Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMEQH6J)

• Drug Name: flavone Drug Info
• Synonyms: Flavone; FLAVONE; 525-82-6; 2-Phenylchromone; 2-Phenyl-4H-chromen-4-one; 2-Phenyl-4-chromone; Asmacoril; 2-Phenyl-4H-1-benzopyran-4-one; 2-Phenyl-4-benzopyron; 4H-1-Benzopyran-4-one, 2-phenyl-; Chromocor; Cromaril; 2-phenylchromen-4-one; Phenylchromone; 2-Phenyl-chromen-4-one; 2-Phenyl-gamma-benzopyrone; 2-Phenylbenzopyran-4-one; Cromarile; 2-Phenyl-4H-benzopyran-4-one; Flavon; 2-Phenylchrome; UNII-S2V45N7G3B; NSC 19028; 2-Phenyl-4H-chromen-4-on; CCRIS 4288; NSC19028; EINECS 208-383-8; NSC-19028; BRN 0157598

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 10680
  ChEBI ID: CHEBI:42491
  CAS Number: CAS 525-82-6
  TTD Drug ID: DMEQH6J
  INTEDE Drug ID: DR2144

Molecule-Related Drug Atlas

Drug(s) Targeting Aromatase (CYP19A1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Anastrozole	DMNP60F	Breast cancer	2C60-2C65	Approved	[16]
Letrozole	DMH07Y3	Estrogen-receptor positive breast cancer		Approved	[17]
Exemestane	DM9HPW3	Hormonally-responsive breast cancer	2C60-2C65	Approved	[17]
Aminoglutethimide	DMWFHMZ	Cushing disease	5A70	Approved	[18]
FADROZOLE	DM3C5GZ	Breast cancer	2C60-2C65	Approved	[19]
Testolactone	DMVY4GN	Breast cancer	2C60-2C65	Approved	[20]
LIAROZOLE	DM4OYXE	Dermatological disease	DA24.Y	Phase 2/3	[4]
Coumate	DMVKW0N	Breast cancer	2C60-2C65	Phase 2	[21]
BGS-649	DMO4MNQ	Endometriosis	GA10	Phase 2	[22]
NARINGENIN	DMHAZLM	N. A.	N. A.	Phase 1	[4]
Letrozole	DMH07Y3	Estrogen-receptor positive breast cancer		Approved	[99]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[100]
Sertraline	DM0FB1J	Coronary heart disease	BA80.Z	Approved	[101]
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[102]
Citalopram	DM2G9AE	Acute coronary syndrome	BA41	Approved	[101]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[73]
FADROZOLE	DM3C5GZ	Breast cancer	2C60-2C65	Approved	[103]
Bifonazole	DM3KN7V	Fungal infection	1F29-1F2F	Approved	[104]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[105]
Fluoxetine	DM3PD2C	Bipolar depression		Approved	[101]

Drug(s) Targeting Adenosine A3 receptor (ADORA3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
IB-MECA	DM9G5XD	Psoriasis vulgaris	EA90	Phase 3	[23]
Tonapofylline	DMBH316	Acute and chronic heart failure	BD1Z	Phase 2	[24]
NITD609	DMQHBSX	Malaria	1F40-1F45	Phase 2	[25]
CF102	DMP56WJ	Hepatocellular carcinoma	2C12.02	Phase 2	[26]
SCH-442416	DMQ2K1V	N. A.	N. A.	Phase 1	[27]
AST-004	DM5WMG7	Stroke	8B20	Phase 1	[28]
BEMESETRON	DMSPJX9	N. A.	N. A.	Discontinued in Phase 3	[29]
BAY 60-6583	DMTEJV1	Myocardial ischemia	BA6Z	Preclinical	[30]
CF602	DM0ULO2	Inflammation	1A00-CA43.1	Preclinical	[26]
CF502	DMQSJ20	Inflammation	1A00-CA43.1	Preclinical	[26]

Drug(s) Targeting Androgen receptor messenger RNA (AR mRNA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dihydrotestosterone	DM3S8XC	Prostate hyperplasia	GA90	Phase 4	[31]
BAY 86-5044	DMRZLU4	Breast cancer	2C60-2C65	Phase 2	[32]
TRC-253	DMXI8CD	Prostate cancer	2C82.0	Phase 1/2	[33]
IONIS-AR-2.5Rx	DMF2DMS	Prostate cancer	2C82.0	Phase 1/2	[34]
ISIS-AR	DM8P3N5	Prostate cancer	2C82.0	Phase 1	[35]
EZN-4176	DMNPS59	Prostate cancer	2C82.0	Phase 1	[36]
EUGENOL	DM7US1H	Discovery agent	N.A.	Patented	[37]
RU-58841	DMMEAZ2	Acne vulgaris	ED80	Discontinued in Phase 1	[38]
APIGENIN	DMI3491	Discovery agent	N.A.	Investigative	[3]
KAEMPFEROL	DMHEMUB	Discovery agent	N.A.	Investigative	[3]

Drug(s) Targeting GABA(A) receptor alpha-1 (GABRA1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[39]
Zolpidem	DMWOSKJ	Insomnia	7A00-7A0Z	Approved	[40]
Methoxyflurane	DML0RAE	Anaesthesia	9A78.6	Approved	[39]
Nitrazepam	DMEGIQ6	Epilepsy	8A60-8A68	Approved	[39]
Allopregnanolone	DMNLHAC	Depression	6A70-6A7Z	approved	[41]
Clobazam - Lundbeck	DMW1OQ0	Anxiety disorder	6B00-6B0Z	Approved	[39]
Hexobarbital	DMQ314B	Anaesthesia	9A78.6	Approved	[39]
THIOCOLCHICOSIDE	DMEPWYA	Muscle spasm	MB47.3	Approved	[42]
Meprobamate	DMHM93Y	Anxiety		Approved	[39]
Zaleplon	DMGFWSM	Insomnia	7A00-7A0Z	Approved	[43]

Drug(s) Targeting Gamma-aminobutyric acid receptor (GAR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Phenobarbital	DMXZOCG	Cluster headache	8A81.0	Approved	[39]
Allopregnanolone	DMNLHAC	Depression	6A70-6A7Z	approved	[44]
THIOCOLCHICOSIDE	DMEPWYA	Muscle spasm	MB47.3	Approved	[42]
Clonazepam	DMTO13J	Absence epilepsy		Approved	[45]
Piperazine	DMTY9LU	Ascariasis	1F62	Approved	[46]
Alpidem	DMN7Y9K	Anxiety disorder	6B00-6B0Z	Approved	[47]
Moxidectin	DMYGHX5	Onchocerciasis	1F6A	Approved	[48]
DP-VPA	DMGOXPQ	Bipolar disorder	6A60	Approved	[49]
ANDROSTERONE	DMITJAK	N. A.	N. A.	Phase 3	[44]
ZK-93423	DMFWMKZ	Epileptic seizures	8A61-8A6Z	Phase 3	[50]

Drug(s) Targeting Adenosine A2b receptor (ADORA2B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Adenosine	DMM2NSK	Paroxysmal supraventricular tachycardia	BC81.Z	Approved	[43]
Vidarabine	DM0N85H	Hepatosplenic T-cell lymphoma		Approved	[43]
A295	DM55GO2	Aggressive cancer	2A00-2F9Z	IND submitted	[51]
Tonapofylline	DMBH316	Acute and chronic heart failure	BD1Z	Phase 2	[24]
YT-146	DM3YVKQ	Hypertension	BA00-BA04	Phase 2	[52]
AB928	DMDOXMN	Metastatic colorectal cancer	2B91	Phase 1/2	[33]
KF-17837	DMQ6DLZ	Parkinson disease	8A00.0	Phase 1	[53]
Xanthine	DMFBOQ7	Apnea	MD11.0	Phase 1	[54]
CVT-6883	DMY84TW	Asthma	CA23	Phase 1	[55]
PBF-1129	DMOPGXM	Non-small-cell lung cancer	2C25.Y	Phase 1	[33]

Drug(s) Targeting Adenosine A1 receptor (ADORA1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Caffeine	DMKBJWP	Allergic rhinitis	CA08.0	Approved	[56]
Rolofylline	DMSZPR3	Heart failure	BD10-BD13	Phase 3	[57]
Tonapofylline	DMBH316	Acute and chronic heart failure	BD1Z	Phase 2	[24]
AMP-579	DMJ4GPR	Hyperlipidaemia	5C80	Phase 2	[58]
SELODENOSON	DMQM3IX	Cardiac arrhythmias	BC9Z	Phase 2	[59]
Apaxifylline	DMQMV9F	Cognitive impairment	6D71	Phase 2	[60]
SLV320	DM867BJ	Heart failure	BD10-BD13	Phase 2	[61]
DTI-0009	DMV84OK	Atrial fibrillation	BC81.3	Phase 2	[59]
Capadenoson	DMYWO62	Atrial fibrillation	BC81.3	Phase 2	[62]
BAY 1067197	DM4JGNH	Heart failure	BD10-BD13	Phase 2	[63]

Drug(s) Metabolized By Cytochrome P450 2A6 (CYP2A6)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[64]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[65]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[66]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[67]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[65]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[68]
Metronidazole	DMTIVEN	Abscess		Approved	[69]
Propofol	DMB4OLE	Anaesthesia	9A78.6	Approved	[70]
Nicotine	DMWX5CO	Lung cancer	2C25.0	Approved	[71]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[65]

Drug(s) Metabolized By Biphenyl dioxygenase (bphC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Isoflavone	DM7U58J	N. A.	N. A.	Phase 4	[8]
AUS-131	DMUXO3Z	Hot flushes	GA30	Phase 2	[8]
Flavanone	DMNWIYM	Discovery agent	N.A.	Investigative	[8]

Drug(s) Metabolized By Naphthalene dioxygenase (doxB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Isoflavone	DM7U58J	N. A.	N. A.	Phase 4	[8]

Drug(s) Affected By Steroid hormone receptor ERR1 (ESRRA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[72]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[73]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[74]
Lindane	DMB8CNL	Infestations of lice and scabies	1G00.Z	Approved	[75]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[76]
Bortezomib	DMNO38U	Leukemia		Approved	[77]
Dinoprostone	DMTYOPD	Medical abortion	JA00.1Z	Approved	[78]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[79]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[79]
DTI-015	DMXZRW0	Brain cancer	2A00	Approved	[80]

Drug(s) Affected By Multidrug resistance-associated protein 1 (ABCC1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[81]
Folic Acid	DMEMBJC	Colorectal carcinoma		Approved	[82]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[83]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[84]
Docetaxel	DMDI269	Advanced cancer	2A00-2F9Z	Approved	[85]
Irinotecan	DMP6SC2	Adenocarcinoma	2D40	Approved	[86]
Epirubicin	DMPDW6T	Solid tumour/cancer	2A00-2F9Z	Approved	[87]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[88]
Colchicine	DM2POTE	Acute gout flare	FA25.0	Approved	[89]
Dactinomycin	DM2YGNW	Adult kidney Wilms tumor		Approved	[89]

Drug(s) Affected By Serum paraoxonase/arylesterase 1 (PON1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Primidone	DM0WX6I	Epilepsy	8A60-8A68	Approved	[90]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[91]
Methimazole	DM25FL8	Hyperthyroidism	5A02	Approved	[92]
Ciprofloxacin XR	DM2NLS9	Acute gonococcal cervicitis		Approved	[93]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[94]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[95]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[96]
Rifampicin	DM5DSFZ	Non-insulin dependent diabetes	5A11	Approved	[97]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[98]
Gabapentin	DM6T924	Complex partial seizure	8A68.0	Approved	[90]

Drug(s) Affected By Cytochrome P450 1A1 (CYP1A1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amodiaquine	DME4RA8	Malaria	1F40-1F45	Approved	[106]
Riluzole	DMECBWN	Amyotrophic lateral sclerosis	8B60.0	Approved	[107]
Flutamide	DMK0O7U	Prostate cancer	2C82.0	Approved	[108]
Menadione	DMSJDTY	Vitamin K deficiency	5B59	Approved	[109]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[110]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[111]
Ethacrynic acid	DM60QMR	Edema	MG29	Approved	[112]
Marinol	DM70IK5	Anorexia nervosa cachexia	6B80	Approved	[113]
Ethinyl Estradiol	DMODJ40	Acne vulgaris	ED80	Approved	[114]
Clofibrate	DMPC1J7	Dysbetalipoproteinemia	5C80.2	Approved	[115]

Drug(s) Affected By Cytochrome P450 1B1 (CYP1B1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Flutamide	DMK0O7U	Prostate cancer	2C82.0	Approved	[107]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[116]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[117]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[118]
Estrone	DM5T6US	Acne vulgaris	ED80	Approved	[119]
Melatonin	DMKWFBT	Depression	6A70-6A7Z	Approved	[120]
Vitamin A	DMJ2AH4	Night blindness	9D45	Approved	[121]
Amodiaquine	DME4RA8	Malaria	1F40-1F45	Approved	[122]
Daunorubicin	DMQUSBT	Acute monocytic leukemia		Approved	[123]
Pantothenic acid	DM091H2	Vitamin deficiency	5B55-5B71	Approved	[124]

Drug(s) Affected By Cytochrome P450 1A2 (CYP1A2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Zolmitriptan	DM1IB4Q	Migraine	8A80	Approved	[125]
Rofecoxib	DM3P5DA	Osteoarthritis	FA00-FA05	Approved	[125]
Etoricoxib	DM6A4NW	Rheumatoid arthritis	FA20	Approved	[125]
Capsaicin	DMGMF6V	Back pain	ME84.Z	Approved	[126]
Hesperetin	DMKER83	High blood cholesterol level	5C80.00	Approved	[127]
Stiripentol	DMMSDOY	Dravet syndrome	8A61.11	Approved	[128]
Nifedipine	DMSVOZT	Angina pectoris	BA40	Approved	[129]
Zileuton	DMVRIC2	Allergic asthma	CA23.0	Approved	[130]
Nicotine	DMWX5CO	Lung cancer	2C25.0	Approved	[131]
Clonidine	DM6RZ9Q	Attention deficit hyperactivity disorder	6A05.Z	Approved	[132]

Drug(s) Affected By Amine oxidase A (MAOA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[133]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[134]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[135]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[136]
Cyclophosphamide	DM4O2Z7	Advanced cancer	2A00-2F9Z	Approved	[137]
Selegiline	DM6034S	Major depressive disorder	6A70.3	Approved	[138]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[139]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[140]
Clorgyline	DMCEUJD	Parkinson disease	8A00.0	Approved	[141]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[142]

Drug(s) Affected By Suppressor of cytokine signaling 3 (SOCS3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[102]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[143]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[144]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[145]
Rofecoxib	DM3P5DA	Osteoarthritis	FA00-FA05	Approved	[146]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[147]
Fedratinib	DM4ZBK6	Myelofibrosis	2A20.2	Approved	[148]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[96]
Pyrimethamine	DM5X7VY	Malaria	1F40-1F45	Approved	[148]
Ibuprofen	DM8VCBE	Dysmenorrhea	GA34.3	Approved	[146]

Drug(s) Affected By Apoptotic protease-activating factor 1 (APAF1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[149]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[133]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[150]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[151]
Cyclophosphamide	DM4O2Z7	Advanced cancer	2A00-2F9Z	Approved	[152]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[153]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[154]
Acocantherin	DM7JT24	Atrial fibrillation	BC81.3	Approved	[155]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[156]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[157]

Drug(s) Affected By Keratin, type I cytoskeletal 18 (KRT18)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Beta-carotene	DM0RXBT	Vitamin deficiency	5B55-5B71	Approved	[158]
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[159]
Selenium	DM25CGV	N. A.	N. A.	Approved	[160]
Colchicine	DM2POTE	Acute gout flare	FA25.0	Approved	[161]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[162]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[9]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[151]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[96]
Nevirapine	DM6HX9B	Human immunodeficiency virus infection	1C62	Approved	[163]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[164]

Drug(s) Affected By Keratin, type II cytoskeletal 8 (KRT8)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Beta-carotene	DM0RXBT	Vitamin deficiency	5B55-5B71	Approved	[158]
Selenium	DM25CGV	N. A.	N. A.	Approved	[160]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[162]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[165]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[135]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[158]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[96]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[166]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[167]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[168]

Drug(s) Affected By ATP-dependent translocase ABCB1 (ABCB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Flupentixol	DM0DJ9O	Schizophrenia	6A20	Approved	[169]
Sertraline	DM0FB1J	Coronary heart disease	BA80.Z	Approved	[170]
Crizotinib	DM4F29C	Non-small-cell lung cancer	2C25.Y	Approved	[171]
Lamotrigine	DM8SXYG	Bipolar disorder	6A60	Approved	[172]
Cepharanthine	DM9Y5JB	N. A.	N. A.	Approved	[173]
Itraconazole	DMCR1MV	Aspergillosis	1F20	Approved	[174]
Clozapine	DMFC71L	Schizophrenia	6A20	Approved	[175]
Midostaurin	DMI6E0R	Acute myeloid leukaemia	2A60	Approved	[176]
Trifluoperazine	DMKBYWI	Anxiety		Approved	[177]
Olanzapine	DMPFN6Y	Bipolar depression		Approved	[175]

Drug(s) Affected By Cytochrome P450 3A4 (CYP3A4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Eplerenone	DMF0NQR	Heart failure	BD10-BD13	Approved	[178]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[179]
Isotretinoin	DM4QTBN	Acne vulgaris	ED80	Approved	[180]
Voriconazole	DMAOL2S	Aspergillosis	1F20	Approved	[181]
Proguanil	DMBL79I	Malaria	1F40-1F45	Approved	[182]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[182]
Loratadine	DMF3AN7	Allergy	4A80-4A85	Approved	[183]
Nelfinavir mesylate	DMFX6G8	N. A.	N. A.	Approved	[184]
Capsaicin	DMGMF6V	Back pain	ME84.Z	Approved	[185]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[186]

Drug(s) Affected By Poly polymerase 1 (PARP1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[187]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[188]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[189]
Nitric Oxide	DM1RBYG	Hypertension	BA00-BA04	Approved	[190]
Citalopram	DM2G9AE	Acute coronary syndrome	BA41	Approved	[191]
Ciprofloxacin XR	DM2NLS9	Acute gonococcal cervicitis		Approved	[192]
Imipramine	DM2NUH3	Depression	6A70-6A7Z	Approved	[191]
Colchicine	DM2POTE	Acute gout flare	FA25.0	Approved	[193]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[194]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[195]

Drug(s) Affected By Heat shock 70 kDa protein 1A (HSPA1A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Carbamazepine	DMZOLBI	Epilepsy	8A60-8A68	Approved	[196]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[197]
Sertraline	DM0FB1J	Coronary heart disease	BA80.Z	Approved	[198]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[199]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[116]
Selenium	DM25CGV	N. A.	N. A.	Approved	[160]
Etretinate	DM2CZFA	Keratosis	ED56	Approved	[200]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[73]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[134]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[111]

Drug(s) Affected By 60 kDa heat shock protein, mitochondrial (HSPD1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[201]
Etretinate	DM2CZFA	Keratosis	ED56	Approved	[200]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[144]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[9]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[111]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[202]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[203]
Isotretinoin	DM4QTBN	Acne vulgaris	ED80	Approved	[204]
Acetic Acid, Glacial	DM4SJ5Y	infection in the ear canal	AA0Y	Approved	[205]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[206]

Drug(s) Affected By C-C motif chemokine 2 (CCL2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Indinavir	DM0T3YH	Human immunodeficiency virus infection	1C62	Approved	[207]
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[102]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[208]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[209]
Imiquimod	DM1TMA3	Alopecia areata	ED70.2	Approved	[210]
Methimazole	DM25FL8	Hyperthyroidism	5A02	Approved	[211]
TECFIDERA	DM2OVDT	Multiple sclerosis	8A40	Approved	[212]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[73]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[213]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[214]

Drug(s) Affected By Leukocyte elastase inhibitor (SERPINB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[143]
Etretinate	DM2CZFA	Keratosis	ED56	Approved	[200]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[215]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[133]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[134]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[216]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[139]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[217]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[218]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[219]

Drug(s) Affected By Prohibitin 1 (PHB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[220]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[221]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[202]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[217]
Marinol	DM70IK5	Anorexia nervosa cachexia	6B80	Approved	[222]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[202]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[140]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[223]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[157]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[224]

Drug(s) Affected By Aryl hydrocarbon receptor (AHR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[102]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[225]
Citalopram	DM2G9AE	Acute coronary syndrome	BA41	Approved	[226]
Colchicine	DM2POTE	Acute gout flare	FA25.0	Approved	[227]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[228]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[229]
Omeprazole	DM471KJ	Cystic fibrosis	CA25	Approved	[230]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[136]
Rifampicin	DM5DSFZ	Non-insulin dependent diabetes	5A11	Approved	[231]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[98]

Drug(s) Affected By Caspase-3 (CASP3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sevoflurane	DMC9O43	Anaesthesia	9A78.6	Approved	[232]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[233]
Lovastatin	DM9OZWQ	Arteriosclerosis	BD40	Approved	[234]
Cidofovir	DMA13GD	Cytomegalovirus infection	1D82	Approved	[235]
Docetaxel	DMDI269	Advanced cancer	2A00-2F9Z	Approved	[236]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[237]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[238]
Mannitol	DMSCDY9	Bronchiectasis	CA24	Approved	[239]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[240]
Aprepitant	DM053KT	Depression	6A70-6A7Z	Approved	[241]

Drug(s) Affected By 3-ketoacyl-CoA thiolase, mitochondrial (ACAA2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Selenium	DM25CGV	N. A.	N. A.	Approved	[160]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[73]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[134]
obeticholic acid	DM3Q1SM	Primary biliary cholangitis	DB96.1	Approved	[242]
Isotretinoin	DM4QTBN	Acne vulgaris	ED80	Approved	[204]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[139]
Acocantherin	DM7JT24	Atrial fibrillation	BC81.3	Approved	[243]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[140]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[142]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[157]

Drug(s) Affected By 26S proteasome regulatory subunit 4 (PSMC1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Selenium	DM25CGV	N. A.	N. A.	Approved	[160]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[157]
Benzatropine	DMF7EXL	Parkinsonian disorder		Approved	[220]
Cupric Sulfate	DMP0NFQ	Fungal infection	1F29-1F2F	Approved	[244]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[245]
Tocopherol	DMBIJZ6	N. A.	N. A.	Phase 2	[160]
TAK-243	DM4GKV2	Solid tumour/cancer	2A00-2F9Z	Phase 1	[246]
PMID28460551-Compound-2	DM4DOUB	N. A.	N. A.	Patented	[247]
MG-132	DMKA2YS	N. A.	N. A.	Preclinical	[248]
bisphenol A	DM2ZLD7	Discovery agent	N.A.	Investigative	[159]

Drug(s) Affected By Lamin-B2 (LMNB2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[219]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[142]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[157]
Cupric Sulfate	DMP0NFQ	Fungal infection	1F29-1F2F	Approved	[244]
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[249]
Aminoglutethimide	DMWFHMZ	Cushing disease	5A70	Approved	[250]
Genistein	DM0JETC	Menopause symptom	GA30.0	Phase 2/3	[251]
DNCB	DMDTVYC	Immune System disease	4A01-4B41	Phase 2	[252]
GSK2110183	DMZHB37	leukaemia	2A60-2B33	Phase 2	[253]
Benzo(a)pyrene	DMN7J43	N. A.	N. A.	Phase 1	[254]

Drug(s) Affected By Nuclear receptor subfamily 1 group I member 3 (NR1I3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[255]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[256]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[257]
Artemether	DM48QOT	Malaria	1F40-1F45	Approved	[258]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[259]
Nefazodone	DM4ZS8M	Major depressive disorder	6A70.3	Approved	[260]
Rifampicin	DM5DSFZ	Non-insulin dependent diabetes	5A11	Approved	[231]
Estrone	DM5T6US	Acne vulgaris	ED80	Approved	[261]
Leflunomide	DMR8ONJ	Arthritis	FA20	Approved	[262]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[140]

Drug(s) Affected By Synaptonemal complex protein 1 (SYCP1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[142]
Decitabine	DMQL8XJ	Acute myelogenous leukaemia	2A41	Approved	[263]
Arsenic	DMTL2Y1	N. A.	N. A.	Approved	[264]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[265]
Benzo(a)pyrene	DMN7J43	N. A.	N. A.	Phase 1	[266]

Drug(s) Affected By Estrogen receptor beta (ESR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[102]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[267]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[268]
Estrone	DM5T6US	Acne vulgaris	ED80	Approved	[269]
Tibolone	DM78XFG	Anabolic metabolism	5C50-5C8Z	Approved	[270]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[271]
Lindane	DMB8CNL	Infestations of lice and scabies	1G00.Z	Approved	[272]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[273]
Mestranol	DMG3F94	Contraception	QA21	Approved	[274]
Flutamide	DMK0O7U	Prostate cancer	2C82.0	Approved	[275]

Drug(s) Affected By DNA repair protein RAD50 (RAD50)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[276]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[9]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[111]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[216]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[277]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[140]
Testosterone enanthate	DMB6871	N. A.	N. A.	Approved	[278]
Clorgyline	DMCEUJD	Parkinson disease	8A00.0	Approved	[279]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[168]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[157]

Drug(s) Affected By Centromere protein J (CENPJ)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[280]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[134]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[151]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[281]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[281]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[140]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[168]
Temozolomide	DMKECZD	Adenocarcinoma	2D40	Approved	[282]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[265]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[117]

Drug(s) Affected By Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[283]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[283]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[284]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[132]
Rosuvastatin	DMMIQ7G	Arteriosclerosis	BD40	Approved	[285]
Ciprofloxacin XR	DM2NLS9	Acute gonococcal cervicitis		Approved	[286]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[162]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[287]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[288]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[289]

Drug(s) Affected By Unconventional myosin-Va (MYO5A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Quercetin	DM3NC4M	Obesity	5B81	Approved	[290]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[291]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[142]
Temozolomide	DMKECZD	Adenocarcinoma	2D40	Approved	[282]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[292]
Arsenic	DMTL2Y1	N. A.	N. A.	Approved	[264]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[265]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[293]
Vorinostat	DMWMPD4	Adult acute monocytic leukemia		Approved	[294]
Carbamazepine	DMZOLBI	Epilepsy	8A60-8A68	Approved	[295]

Drug(s) Affected By Centrosomal protein of 83 kDa (CEP83)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Quercetin	DM3NC4M	Obesity	5B81	Approved	[134]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[151]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[142]
Cupric Sulfate	DMP0NFQ	Fungal infection	1F29-1F2F	Approved	[244]
Benzo(a)pyrene	DMN7J43	N. A.	N. A.	Phase 1	[140]
bisphenol A	DM2ZLD7	Discovery agent	N.A.	Investigative	[159]
ORG2058	DMH1M6N	Discovery agent	N.A.	Investigative	[296]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Adenosine A1 receptor (ADORA1)	TTK25J1	AA1R_HUMAN	Antagonist	[2]
Adenosine A2b receptor (ADORA2B)	TTNE7KG	AA2BR_HUMAN	Antagonist	[2]
Adenosine A3 receptor (ADORA3)	TTJFY5U	AA3R_HUMAN	Antagonist	[2]
Androgen receptor messenger RNA (AR mRNA)	TTKPW01	ANDR_HUMAN	Inhibitor	[3]
Aromatase (CYP19A1)	TTSZLWK	CP19A_HUMAN	Inhibitor	[4]
GABA(A) receptor alpha-1 (GABRA1)	TT1MPAY	GBRA1_HUMAN	Inhibitor	[5]
Gamma-aminobutyric acid receptor (GAR)	TTNJYV2	NOUNIPROTAC	Inhibitor	[6]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 2A6 (CYP2A6)	DEJVYAZ	CP2A6_HUMAN	Substrate	[7]
Naphthalene dioxygenase (doxB)	DEE76YZ	NDOB_PSEU8	Substrate	[8]
Biphenyl dioxygenase (bphC)	DEUX61H	BPHC_PSEFK	Substrate	[8]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
26S proteasome regulatory subunit 4 (PSMC1)	OTLHD56E	PRS4_HUMAN	Gene/Protein Processing	[9]
3-ketoacyl-CoA thiolase, mitochondrial (ACAA2)	OTGLVWOP	THIM_HUMAN	Gene/Protein Processing	[9]
60 kDa heat shock protein, mitochondrial (HSPD1)	OTTO1Y11	CH60_HUMAN	Gene/Protein Processing	[9]
Amine oxidase A (MAOA)	OT8NIWMQ	AOFA_HUMAN	Gene/Protein Processing	[10]
Apoptotic protease-activating factor 1 (APAF1)	OTJWIVY0	APAF_HUMAN	Gene/Protein Processing	[9]
Aromatase (CYP19A1)	OTZ6XF74	CP19A_HUMAN	Gene/Protein Processing	[11]
Aryl hydrocarbon receptor (AHR)	OTFE4EYE	AHR_HUMAN	Protein Interaction/Cellular Processes	[12]
ATP-dependent translocase ABCB1 (ABCB1)	OTEJROBO	MDR1_HUMAN	Gene/Protein Processing	[13]
Broad substrate specificity ATP-binding cassette transporter ABCG2 (ABCG2)	OTW8V2V1	ABCG2_HUMAN	Gene/Protein Processing	[14]
C-C motif chemokine 2 (CCL2)	OTAD2HEL	CCL2_HUMAN	Gene/Protein Processing	[15]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 409).
• [2] Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. J Med Chem. 1996 Jun 7;39(12):2293-301.
• [3] Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4706-10.
• [4] Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19). Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64.
• [5] Synthesis of halogenated/nitrated flavone derivatives and evaluation of their affinity for the central benzodiazepine receptor, Bioorg. Med. Chem. Lett. 7(15):2003-2008 (1997).
• [6] Refinement and evaluation of a pharmacophore model for flavone derivatives binding to the benzodiazepine site of the GABA(A) receptor. J Med Chem. 2002 Sep 12;45(19):4188-201.
• [7] Site-specific oxidation of flavanone and flavone by cytochrome P450 2A6 in human liver microsomes. Xenobiotica. 2019 Jul;49(7):791-802.
• [8] Flavonoids biotransformation by bacterial non-heme dioxygenases, biphenyl and naphthalene dioxygenase. Appl Microbiol Biotechnol. 2011 Jul;91(2):219-28.
• [9] Identification of biomarkers for the initiation of apoptosis in human preneoplastic colonocytes by proteome analysis. Int J Cancer. 2004 Mar 20;109(2):220-9. doi: 10.1002/ijc.11692.
• [10] Evaluation of the inhibitory effects of quercetin-related flavonoids and tea catechins on the monoamine oxidase-A reaction in mouse brain mitochondria. J Agric Food Chem. 2012 Oct 17;60(41):10270-7.
• [11] Induction and inhibition of aromatase (CYP19) activity by natural and synthetic flavonoid compounds in H295R human adrenocortical carcinoma cells. Toxicol Sci. 2004 Nov;82(1):70-9.
• [12] Xeno-oestrogens and phyto-oestrogens are alternative ligands for the androgen receptor. Asian J Androl. 2010 Jul;12(4):535-47. doi: 10.1038/aja.2010.14. Epub 2010 May 3.
• [13] Structure-activity relationship and mechanism of flavonoids on the inhibitory activity of P-glycoprotein (P-gp)-mediated transport of rhodamine123 and daunorubicin in P-gp overexpressed human mouth epidermal carcinoma (KB/MDR) cells. Food Chem Toxicol. 2021 Sep;155:112381. doi: 10.1016/j.fct.2021.112381. Epub 2021 Jul 1.
• [14] Phytochemicals induce breast cancer resistance protein in Caco-2 cells and enhance the transport of benzo[a]pyrene-3-sulfate. Toxicol Sci. 2007 Apr;96(2):227-36. doi: 10.1093/toxsci/kfl147. Epub 2006 Oct 31.
• [15] Flavanoids induce expression of the suppressor of cytokine signalling 3 (SOCS3) gene and suppress IL-6-activated signal transducer and activator of transcription 3 (STAT3) activation in vascular endothelial cells. Biochem J. 2013 Sep 1;454(2):283-93. doi: 10.1042/BJ20130481.
• [16] Effective aromatase inhibition by anastrozole in a patient with gonadotropin-independent precocious puberty in McCune-Albright syndrome. J Pediatr Endocrinol Metab. 2002;15 Suppl 3:945-8.
• [17] Aromatase inhibitors--theoretical concept and present experiences in the treatment of endometriosis. Zentralbl Gynakol. 2003 Jul-Aug;125(7-8):247-51.
• [18] Aminoglutethimide-induced protein free radical formation on myeloperoxidase: a potential mechanism of agranulocytosis. Chem Res Toxicol. 2007 Jul;20(7):1038-45.
• [19] Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach. J Med Chem. 2005 Nov 17;48(23):7282-9.
• [20] Aromatase inhibitors for male infertility. J Urol. 2002 Feb;167(2 Pt 1):624-9.
• [21] Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template. J Med Chem. 2010 Mar 11;53(5):2155-70.
• [22] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032111)
• [23] A role for central A3-adenosine receptors. Mediation of behavioral depressant effects. FEBS Lett. 1993 Dec 20;336(1):57-60.
• [24] 2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. Bioorg Med Chem. 2010 Mar 15;18(6):2195-2203.
• [25] Spiroindolones, a potent compound class for the treatment of malaria. Science. 2010 Sep 3;329(5996):1175-80.
• [26] 2011 Pipeline of Can-Fite BioPharm.
• [27] Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5690-4.
• [28] Adenosine A1R/A3R (Adenosine A1 and A3 Receptor) Agonist AST-004 Reduces Brain Infarction in a Nonhuman Primate Model of Stroke. Stroke. 2022 Jan;53(1):238-248.
• [29] 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacolog... J Med Chem. 2005 Nov 3;48(22):6887-96.
• [30] Protein kinase C protects preconditioned rabbit hearts by increasing sensitivity of adenosine A2b-dependent signaling during early reperfusion. J Mol Cell Cardiol. 2007 Sep;43(3):262-71.
• [31] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 628).
• [32] Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. J Med Chem. 2000 Dec 28;43(26):5010-6.
• [33] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [34] Perspectives on the current and emerging chemical androgen receptor antagonists for the treatment of prostate cancer. Expert Opin Pharmacother. 2019 Feb;20(2):163-172.
• [35] Clinical pipeline report, company report or official report of ISIS Pharmaceuticals.
• [36] 2011 Pipeline of Santaris Pharma.
• [37] Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2111-4.
• [38] Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen recepto... J Med Chem. 2008 Nov 13;51(21):7010-4.
• [39] DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
• [40] Zolpidem, a selective GABA(A) receptor alpha1 subunit agonist, induces comparable Fos expression in oxytocinergic neurons of the hypothalamic paraventricular and accessory but not supraoptic nuclei in the rat.Brain Res Bull.2006 Dec 11;71(1-3):200-7.
• [41] Neurosteroid analogues. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (... J Med Chem. 2005 Apr 21;48(8):3051-9.
• [42] 3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7.
• [43] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [44] Neurosteroid analogues. 11. Alternative ring system scaffolds: gamma-aminobutyric acid receptor modulation and anesthetic actions of benz[f]indenes. J Med Chem. 2006 Jul 27;49(15):4595-605.
• [45] Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
• [46] Cyclooctadepsipeptides--an anthelmintically active class of compounds exhibiting a novel mode of action. Int J Antimicrob Agents. 2003 Sep;22(3):318-31.
• [47] Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new se... J Med Chem. 1997 Sep 12;40(19):3109-18.
• [48] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [49] DP-VPA D-Pharm. Curr Opin Investig Drugs. 2002 Jun;3(6):921-3.
• [50] Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carbolin... J Med Chem. 1990 Mar;33(3):1062-9.
• [51] Clinical pipeline report, company report or official report of Klus Pharma
• [52] Identification of adenosine A2 receptor-cAMP system in human aortic endothelial cells. Biochem Biophys Res Commun. 1994 Mar 15;199(2):905-10.
• [53] Photoisomerization of a potent and selective adenosine A2 antagonist, (E)-1,3-Dipropyl-8-(3,4-dimethoxystyryl)-7-methylxanthine. J Med Chem. 1993 Nov 12;36(23):3731-3.
• [54] Role of adenosine in asthma. Drug Dev Res. 1996;39:333-6.
• [55] GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse. J Pharmacol Exp Ther. 2012 Dec;343(3):587-95.
• [56] Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72.
• [57] Association between the PDE4D gene and ischaemic stroke in the Chinese Han population. Clin Sci (Lond). 2009 Aug 17;117(7):265-72.
• [58] Adenosine A1/A2a receptor agonist AMP-579 induces acute and delayed preconditioning against in vivo myocardial stunning. Am J Physiol Heart Circ Physiol. 2004 Dec;287(6):H2746-53.
• [59] Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May;1808(5):1290-308.
• [60] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004779)
• [61] Role of matrix metalloproteinases and their tissue inhibitors as potential biomarkers of left ventricular remodelling in the athlete's heart. Clin Sci (Lond). 2009 Jul 16;117(4):157-64.
• [62] A1 adenosine receptor agonists and their potential therapeutic applications. Expert Opin Investig Drugs. 2008 Dec;17(12):1901-10.
• [63] Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Current Issue vol. 111 no. 12 Celine Valant, 4614-4619.
• [64] Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
• [65] Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
• [66] Genotoxicity of tamoxifen, tamoxifen epoxide and toremifene in human lymphoblastoid cells containing human cytochrome P450s. Carcinogenesis. 1994 Jan;15(1):5-9.
• [67] Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
• [68] Psychotropic drug interactions with valproate. Clin Neuropharmacol. 2005 Mar-Apr;28(2):96-101.
• [69] The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94.
• [70] Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
• [71] CYP2A6- and CYP2A13-catalyzed metabolism of the nicotine delta-5'(1')iminium ion. J Pharmacol Exp Ther. 2012 Nov;343(2):307-15.
• [72] Regulation of ERRalpha gene expression by estrogen receptor agonists and antagonists in SKBR3 breast cancer cells: differential molecular mechanisms mediated by g protein-coupled receptor GPR30/GPER-1. Mol Endocrinol. 2010 May;24(5):969-80. doi: 10.1210/me.2009-0148. Epub 2010 Mar 8.
• [73] The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
• [74] Troglitazone induces cytotoxicity in part by promoting the degradation of peroxisome proliferator-activated receptor co-activator-1 protein. Br J Pharmacol. 2010 Oct;161(4):771-81. doi: 10.1111/j.1476-5381.2010.00900.x.
• [75] Plasmatic concentration of organochlorine lindane acts as metabolic disruptors in HepG2 liver cell line by inducing mitochondrial disorder. Toxicol Appl Pharmacol. 2013 Oct 15;272(2):325-34.
• [76] Antiepileptic drugs are endocrine disruptors for the human fetal testis ex vivo. Toxicol Sci. 2023 Sep 28;195(2):169-183. doi: 10.1093/toxsci/kfad076.
• [77] The proapoptotic effect of zoledronic acid is independent of either the bone microenvironment or the intrinsic resistance to bortezomib of myeloma cells and is enhanced by the combination with arsenic trioxide. Exp Hematol. 2011 Jan;39(1):55-65.
• [78] Estrogen receptor-related receptor alpha mediates up-regulation of aromatase expression by prostaglandin E2 in prostate stromal cells. Mol Endocrinol. 2010 Jun;24(6):1175-86.
• [79] [Regulation of orphan receptor ERR alpha by estrogen and progesterone in endometrial carcinoma cell line]. Beijing Da Xue Xue Bao Yi Xue Ban. 2005 Jun 18;37(3):281-3.
• [80] Gene expression profile induced by BCNU in human glioma cell lines with differential MGMT expression. J Neurooncol. 2005 Jul;73(3):189-98.
• [81] Characterization of multidrug transporter-mediated efflux of avermectins in human and mouse neuroblastoma cell lines. Toxicol Lett. 2015 Jun 15;235(3):189-98. doi: 10.1016/j.toxlet.2015.04.005. Epub 2015 Apr 9.
• [82] Folate concentration dependent transport activity of the Multidrug Resistance Protein 1 (ABCC1). Biochem Pharmacol. 2004 Apr 15;67(8):1541-8.
• [83] Methotrexate normalizes up-regulated folate pathway genes in rheumatoid arthritis. Arthritis Rheum. 2013 Nov;65(11):2791-802.
• [84] Influence of redox-active compounds and PXR-activators on human MRP1 and MRP2 gene expression. Toxicology. 2002 Feb 28;171(2-3):137-46.
• [85] Enhanced in vitro invasiveness and drug resistance with altered gene expression patterns in a human lung carcinoma cell line after pulse selection with anticancer drugs. Int J Cancer. 2004 Sep 10;111(4):484-93. doi: 10.1002/ijc.20230.
• [86] Clinical determinants of response to irinotecan-based therapy derived from cell line models. Clin Cancer Res. 2008 Oct 15;14(20):6647-55.
• [87] Co-encapsulation of chrysophsin-1 and epirubicin in PEGylated liposomes circumvents multidrug resistance in HeLa cells. Chem Biol Interact. 2015 Dec 5;242:13-23. doi: 10.1016/j.cbi.2015.08.023. Epub 2015 Sep 1.
• [88] Upregulation of multi drug resistance genes in doxorubicin resistant human acute myelogeneous leukemia cells and reversal of the resistance. Hematology. 2007 Dec;12(6):511-7. doi: 10.1080/10245330701562535.
• [89] Functional analysis of MRP1 cloned from bovine. FEBS Lett. 2002 Jun 19;521(1-3):211-3. doi: 10.1016/s0014-5793(02)02816-8.
• [90] Antiepileptic drugs: impacts on human serum paraoxonase-1. J Biochem Mol Toxicol. 2017 Jun;31(6).
• [91] Beneficial effect of oleoylated lipids on paraoxonase 1: protection against oxidative inactivation and stabilization. Biochem J. 2003 Oct 15;375(Pt 2):275-85.
• [92] Serum paraoxonase activity before and after treatment of thyrotoxicosis. Clin Endocrinol (Oxf). 2004 Jan;60(1):75-80.
• [93] Effects of some antibiotics on paraoxonase from human serum in vitro and from mouse serum and liver in vivo. Biol Pharm Bull. 2006 Aug;29(8):1559-63.
• [94] Simvastatin modulates expression of the PON1 gene and increases serum paraoxonase: a role for sterol regulatory element-binding protein-2. Arterioscler Thromb Vasc Biol. 2003 Nov 1;23(11):2083-9. doi: 10.1161/01.ATV.0000096207.01487.36. Epub 2003 Sep 18.
• [95] Dietary polyphenols increase paraoxonase 1 gene expression by an aryl hydrocarbon receptor-dependent mechanism. Mol Cell Biol. 2004 Jun;24(12):5209-22.
• [96] A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
• [97] Transcriptional regulation of human paraoxonase 1 by PXR and GR in human hepatoma cells. Toxicol In Vitro. 2015 Dec 25;30(1 Pt B):348-54.
• [98] Induction of paraoxonase 1 and apolipoprotein A-I gene expression by aspirin. J Lipid Res. 2008 Oct;49(10):2142-8.
• [99] Aromatase inhibition: translation into a successful therapeutic approach. Clin Cancer Res. 2005 Apr 15;11(8):2809-21. doi: 10.1158/1078-0432.CCR-04-2187.
• [100] Cannabidiol (CBD) but not tetrahydrocannabinol (THC) dysregulate in vitro decidualization of human endometrial stromal cells by disruption of estrogen signaling. Reprod Toxicol. 2020 Apr;93:75-82. doi: 10.1016/j.reprotox.2020.01.003. Epub 2020 Jan 14.
• [101] Effects of selective serotonin reuptake inhibitors on three sex steroids in two versions of the aromatase enzyme inhibition assay and in the H295R cell assay. Toxicol In Vitro. 2015 Oct;29(7):1729-35.
• [102] Arsenite and cadmium promote the development of mammary tumors. Carcinogenesis. 2020 Jul 14;41(7):1005-1014. doi: 10.1093/carcin/bgz176.
• [103] Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase. J Med Chem. 2005 Mar 10;48(5):1563-75.
• [104] Comparative assessment of the inhibition of recombinant human CYP19 (aromatase) by azoles used in agriculture and as drugs for humans. Endocr Res. 2004 Aug;30(3):387-94.
• [105] Estrogen synthesis in human colon cancer epithelial cells. J Steroid Biochem Mol Biol. 1999 Dec 31;71(5-6):223-30.
• [106] Cytochrome P450 1A1/2 induction by antiparasitic drugs: dose-dependent increase in ethoxyresorufin O-deethylase activity and mRNA caused by quinine, primaquine and albendazole in HepG2 cells. Eur J Clin Pharmacol. 2002 Nov;58(8):537-42.
• [107] Association of CYP1A1 and CYP1B1 inhibition in in vitro assays with drug-induced liver injury. J Toxicol Sci. 2021;46(4):167-176. doi: 10.2131/jts.46.167.
• [108] Anti-androgenic effect of 6-formylindolo[3,2-b]carbazole (FICZ) in LNCaP cells is mediated by the aryl hydrocarbon-androgen receptors cross-talk. Steroids. 2020 Jan;153:108508. doi: 10.1016/j.steroids.2019.108508. Epub 2019 Oct 3.
• [109] Pharmacologic profiling of human and rat cytochrome P450 1A1 and 1A2 induction and competition. Arch Toxicol. 2008 Dec;82(12):909-21.
• [110] Effect of CYP1A1 gene polymorphisms on estrogen metabolism and bone density. J Bone Miner Res. 2005 Feb;20(2):232-9. doi: 10.1359/JBMR.041110. Epub 2004 Nov 16.
• [111] Increased sensitivity for troglitazone-induced cytotoxicity using a human in vitro co-culture model. Toxicol In Vitro. 2009 Oct;23(7):1387-95.
• [112] Isoform-specific induction of a human aldo-keto reductase by polycyclic aromatic hydrocarbons (PAHs), electrophiles, and oxidative stress: implications for the alternative pathway of PAH activation catalyzed by human dihydrodiol dehydrogenase. Cancer Res. 1999 Feb 1;59(3):607-14.
• [113] Gene expression changes in human small airway epithelial cells exposed to Delta9-tetrahydrocannabinol. Toxicol Lett. 2005 Aug 14;158(2):95-107.
• [114] The metallohormone cadmium modulates AhR-associated gene expression in the small intestine of rats similar to ethinyl-estradiol. Arch Toxicol. 2013 Apr;87(4):633-43.
• [115] Evidence for a new human CYP1A1 regulation pathway involving PPAR-alpha and 2 PPRE sites. Gastroenterology. 2004 Nov;127(5):1436-45.
• [116] Gene expression after treatment with hydrogen peroxide, menadione, or t-butyl hydroperoxide in breast cancer cells. Cancer Res. 2002 Nov 1;62(21):6246-54.
• [117] Convergent transcriptional profiles induced by endogenous estrogen and distinct xenoestrogens in breast cancer cells. Carcinogenesis. 2006 Aug;27(8):1567-78.
• [118] Gene expression in endometrial cancer cells (Ishikawa) after short time high dose exposure to progesterone. Steroids. 2008 Jan;73(1):116-28.
• [119] In vitro aromatic bioactivation of the weak estrogen E(2)alpha and genesis of DNA adducts. Steroids. 2005 Mar;70(3):161-72. doi: 10.1016/j.steroids.2004.11.004.
• [120] Metabolism of melatonin by human cytochromes p450. Drug Metab Dispos. 2005 Apr;33(4):489-94.
• [121] Metabolism of retinoids and arachidonic acid by human and mouse cytochrome P450 1b1. Drug Metab Dispos. 2004 Aug;32(8):840-7.
• [122] Apoptosis contributes to the cytotoxicity induced by amodiaquine and its major metabolite N-desethylamodiaquine in hepatic cells. Toxicol In Vitro. 2020 Feb;62:104669. doi: 10.1016/j.tiv.2019.104669. Epub 2019 Oct 16.
• [123] Genetic variants contributing to daunorubicin-induced cytotoxicity. Cancer Res. 2008 May 1;68(9):3161-8. doi: 10.1158/0008-5472.CAN-07-6381.
• [124] Calcium pantothenate modulates gene expression in proliferating human dermal fibroblasts. Exp Dermatol. 2009 Nov;18(11):969-78. doi: 10.1111/j.1600-0625.2009.00884.x. Epub 2009 Apr 8.
• [125] In vitro inhibition of CYP1A2 by model inhibitors, anti-inflammatory analgesics and female sex steroids: predictability of in vivo interactions. Basic Clin Pharmacol Toxicol. 2008 Aug;103(2):157-65.
• [126] Effects of capsaicin and dihydrocapsaicin on human and rat liver microsomal CYP450 enzyme activities in vitro and in vivo. J Asian Nat Prod Res. 2012;14(4):382-95.
• [127] Drug interaction study of flavonoids toward CYP3A4 and their quantitative structure activity relationship (QSAR) analysis for predicting potential effects. Toxicol Lett. 2018 Sep 15;294:27-36.
• [128] Stiripentol. Expert Opin Investig Drugs. 2005 Jul;14(7):905-11.
• [129] Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: prediction of in vivo drug-drug interactions. Eur J Clin Pharmacol. 2000 Feb-Mar;55(11-12):843-52.
• [130] Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor. Drug Metab Dispos. 2003 Nov;31(11):1352-60.
• [131] Predictive three-dimensional quantitative structure-activity relationship of cytochrome P450 1A2 inhibitors. J Med Chem. 2005 Jun 2;48(11):3808-15.
• [132] ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
• [133] Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
• [134] Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
• [135] Effects of ciglitazone and troglitazone on the proliferation of human stomach cancer cells. World J Gastroenterol. 2009 Jan 21;15(3):310-20.
• [136] Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
• [137] Comparative gene expression analysis of a chronic myelogenous leukemia cell line resistant to cyclophosphamide using oligonucleotide arrays and response to tyrosine kinase inhibitors. Leuk Res. 2007 Nov;31(11):1511-20.
• [138] Characterizing fucoxanthin as a selective dopamine D(3)/D(4) receptor agonist: Relevance to Parkinson's disease. Chem Biol Interact. 2019 Sep 1;310:108757. doi: 10.1016/j.cbi.2019.108757. Epub 2019 Jul 16.
• [139] Arsenic suppresses gene expression in promyelocytic leukemia cells partly through Sp1 oxidation. Blood. 2005 Jul 1;106(1):304-10.
• [140] Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
• [141] Synthesis and study of a series of 3-arylcoumarins as potent and selective monoamine oxidase B inhibitors. J Med Chem. 2011 Oct 27;54(20):7127-37.
• [142] Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
• [143] Global gene expression analysis reveals differences in cellular responses to hydroxyl- and superoxide anion radical-induced oxidative stress in caco-2 cells. Toxicol Sci. 2010 Apr;114(2):193-203. doi: 10.1093/toxsci/kfp309. Epub 2009 Dec 31.
• [144] Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
• [145] Simvastatin inhibits IL-17 secretion by targeting multiple IL-17-regulatory cytokines and by inhibiting the expression of IL-17 transcription factor RORC in CD4+ lymphocytes. J Immunol. 2008 May 15;180(10):6988-96. doi: 10.4049/jimmunol.180.10.6988.
• [146] Rofecoxib modulates multiple gene expression pathways in a clinical model of acute inflammatory pain. Pain. 2007 Mar;128(1-2):136-47.
• [147] Retinoic acid and its 4-oxo metabolites are functionally active in human skin cells in vitro. J Invest Dermatol. 2005 Jul;125(1):143-53.
• [148] The antimicrobial drug pyrimethamine inhibits STAT3 transcriptional activity by targeting the enzyme dihydrofolate reductase. J Biol Chem. 2022 Feb;298(2):101531. doi: 10.1016/j.jbc.2021.101531. Epub 2021 Dec 23.
• [149] Cannabidiol Modulates the Immunophenotype and Inhibits the Activation of the Inflammasome in Human Gingival Mesenchymal Stem Cells. Front Physiol. 2016 Nov 24;7:559. doi: 10.3389/fphys.2016.00559. eCollection 2016.
• [150] Integrated assessment by multiple gene expression analysis of quercetin bioactivity on anticancer-related mechanisms in colon cancer cells in vitro. Eur J Nutr. 2005 Mar;44(3):143-56. doi: 10.1007/s00394-004-0503-1. Epub 2004 Apr 30.
• [151] Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
• [152] Comparison of Drug Metabolism and Its Related Hepatotoxic Effects in HepaRG, Cryopreserved Human Hepatocytes, and HepG2 Cell Cultures. Biol Pharm Bull. 2018 May 1;41(5):722-732. doi: 10.1248/bpb.b17-00913. Epub 2018 Feb 14.
• [153] Endoplasmic reticulum stress contributes to arsenic trioxide-induced intrinsic apoptosis in human umbilical and bone marrow mesenchymal stem cells. Environ Toxicol. 2016 Mar;31(3):314-28.
• [154] Lunasin, a novel seed peptide, sensitizes human breast cancer MDA-MB-231 cells to aspirin-arrested cell cycle and induced apoptosis. Chem Biol Interact. 2010 Jul 30;186(2):127-34. doi: 10.1016/j.cbi.2010.04.027. Epub 2010 May 21.
• [155] Ouabain induces apoptotic cell death in human prostate DU 145 cancer cells through DNA damage and TRAIL pathways. Environ Toxicol. 2019 Dec;34(12):1329-1339. doi: 10.1002/tox.22834. Epub 2019 Aug 21.
• [156] From transient transcriptome responses to disturbed neurodevelopment: role of histone acetylation and methylation as epigenetic switch between reversible and irreversible drug effects. Arch Toxicol. 2014 Jul;88(7):1451-68.
• [157] Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
• [158] Beta-carotene and apocarotenals promote retinoid signaling in BEAS-2B human bronchioepithelial cells. Arch Biochem Biophys. 2006 Nov 1;455(1):48-60.
• [159] DNA methylome-wide alterations associated with estrogen receptor-dependent effects of bisphenols in breast cancer. Clin Epigenetics. 2019 Oct 10;11(1):138. doi: 10.1186/s13148-019-0725-y.
• [160] Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
• [161] The stability of cytokeratin 18 in human liver cells during colchicine-induced microtubule disruption. Food Chem Toxicol. 2001 Jan;39(1):85-9. doi: 10.1016/s0278-6915(00)00113-7.
• [162] Proteomic identification of differentially expressed proteins associated with the multiple drug resistance in methotrexate-resistant human breast cancer cells. Int J Oncol. 2014 Jul;45(1):448-58.
• [163] Nevirapine restores androgen signaling in hormone-refractory human prostate carcinoma cells both in vitro and in vivo. Prostate. 2009 May 15;69(7):744-54. doi: 10.1002/pros.20923.
• [164] Identification of vitamin D3 target genes in human breast cancer tissue. J Steroid Biochem Mol Biol. 2016 Nov;164:90-97.
• [165] The effects of quercetin on SW480 human colon carcinoma cells: a proteomic study. Nutr J. 2005 Mar 4;4:11.
• [166] Proteomics-based identification of differentially abundant proteins from human keratinocytes exposed to arsenic trioxide. J Proteomics Bioinform. 2014 Jul;7(7):166-178.
• [167] Proteomics investigations of drug-induced hepatotoxicity in HepG2 cells. Toxicol Sci. 2011 Mar;120(1):109-22.
• [168] Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
• [169] Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. Cancer Res. 1994 Feb 1;54(3):730-7.
• [170] Michaelis-Menten kinetic analysis of drugs of abuse to estimate their affinity to human P-glycoprotein. Toxicol Lett. 2013 Feb 27;217(2):137-42. doi: 10.1016/j.toxlet.2012.12.012. Epub 2012 Dec 27.
• [171] Editor's Highlight: PlacentalDisposition and Effects of Crizotinib: An Ex Vivo Study in the Isolated Dual-Side Perfused Human Cotyledon. Toxicol Sci. 2017 Jun 1;157(2):500-509. doi: 10.1093/toxsci/kfx063.
• [172] Functional evaluation of polymorphisms in the human ABCB1 gene and the impact on clinical responses of antiepileptic drugs. Pharmacogenet Genomics. 2008 May;18(5):390-402. doi: 10.1097/FPC.0b013e3282f85e36.
• [173] Cepharanthine potently enhances the sensitivity of anticancer agents in K562 cells. Cancer Sci. 2005 Jun;96(6):372-6. doi: 10.1111/j.1349-7006.2005.00057.x.
• [174] Clinical pharmacokinetic monitoring of itraconazole is warranted in only a subset of patients. Ther Drug Monit. 2005 Jun;27(3):322-33. doi: 10.1097/01.ftd.0000150135.22645.ea.
• [175] Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein. Psychopharmacology (Berl). 2006 Sep;187(4):415-23. doi: 10.1007/s00213-006-0437-9. Epub 2006 Jun 30.
• [176] Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002 Feb;87(2):167-76.
• [177] Characterization of the ATPase activity of the Mr 170,000 to 180,000 membrane glycoprotein (P-glycoprotein) associated with multidrug resistance in K562/ADM cells. Cancer Res. 1988 Sep 1;48(17):4926-32.
• [178] The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
• [179] Characterization of the structural determinants required for potent mechanism-based inhibition of human cytochrome P450 1A1 by cannabidiol. Chem Biol Interact. 2014 May 25;215:62-8.
• [180] Retinoids activate the RXR/SXR-mediated pathway and induce the endogenous CYP3A4 activity in Huh7 human hepatoma cells. Toxicol Sci. 2006 Jul;92(1):51-60.
• [181] The novel azole R126638 is a selective inhibitor of ergosterol synthesis in Candida albicans, Trichophyton spp., and Microsporum canis. Antimicrob Agents Chemother. 2004 Sep;48(9):3272-8.
• [182] Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. Drug Metab Dispos. 2001 Jan;29(1):30-5.
• [183] Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5591-4.
• [184] Mechanism-based inactivation of CYP3A by HIV protease inhibitors. J Pharmacol Exp Ther. 2005 Feb;312(2):583-91.
• [185] Studies of the toxicological potential of capsinoids, XIII: inhibitory effects of capsaicin and capsinoids on cytochrome P450 3A4 in human liver microsomes. Int J Toxicol. 2010 Mar;29(2 Suppl):22S-6S.
• [186] Investigation of the effects of axitinib on the pharmacokinetics of loperamide and its main metabolite N-demethylated loperamide in rats by UPLC-MS/MS. Chem Biol Interact. 2019 Sep 1;310:108744. doi: 10.1016/j.cbi.2019.108744. Epub 2019 Jul 9.
• [187] Cannabidiol enhances cytotoxicity of anti-cancer drugs in human head and neck squamous cell carcinoma. Sci Rep. 2020 Nov 26;10(1):20622. doi: 10.1038/s41598-020-77674-y.
• [188] Evidence of securin-mediated resistance to gefitinib-induced apoptosis in human cancer cells. Chem Biol Interact. 2013 Apr 25;203(2):412-22. doi: 10.1016/j.cbi.2013.03.011. Epub 2013 Mar 22.
• [189] Cigarette smoke and asbestos activate poly-ADP-ribose polymerase in alveolar epithelial cells. J Investig Med. 2001 Jan;49(1):68-76. doi: 10.2310/6650.2001.34092.
• [190] Apoptotic signaling pathways induced by nitric oxide in human lymphoblastoid cells expressing wild-type or mutant p53. Cancer Res. 2004 May 1;64(9):3022-9. doi: 10.1158/0008-5472.can-03-1880.
• [191] The antidepressants imipramine, clomipramine, and citalopram induce apoptosis in human acute myeloid leukemia HL-60 cells via caspase-3 activation. J Biochem Mol Toxicol. 1999;13(6):338-47. doi: 10.1002/(sici)1099-0461(1999)13:6<338::aid-jbt8>3.0.co;2-7.
• [192] Ciprofloxacin mediated cell growth inhibition, S/G2-M cell cycle arrest, and apoptosis in a human transitional cell carcinoma of the bladder cell line. Clin Cancer Res. 2000 Mar;6(3):891-900.
• [193] Investigation of molecular mechanisms underlying the antiproliferative effects of colchicine against PC3 prostate cancer cells. Toxicol In Vitro. 2021 Jun;73:105138. doi: 10.1016/j.tiv.2021.105138. Epub 2021 Mar 6.
• [194] Sulindac enhances adenoviral vector expressing mda-7/IL-24-mediated apoptosis in human lung cancer. Mol Cancer Ther. 2005 Feb;4(2):291-304.
• [195] Methotrexate induces poly(ADP-ribose) polymerase-dependent, caspase 3-independent apoptosis in subsets of proliferating CD4+ T cells. Clin Exp Immunol. 2007 May;148(2):288-95. doi: 10.1111/j.1365-2249.2007.03335.x. Epub 2007 Feb 7.
• [196] Serious carbamazepine-induced hypersensitivity reactions associated with the HSP70 gene cluster. Pharmacogenet Genomics. 2006 Apr;16(4):287-96. doi: 10.1097/01.fpc.0000189800.88596.7a.
• [197] Inhibiting Heat Shock Proteins Can Potentiate the Cytotoxic Effect of Cannabidiol in Human Glioma Cells. Anticancer Res. 2015 Nov;35(11):5827-37.
• [198] Sertraline induces endoplasmic reticulum stress in hepatic cells. Toxicology. 2014 Aug 1;322:78-88. doi: 10.1016/j.tox.2014.05.007. Epub 2014 May 24.
• [199] Reactive metabolite of gefitinib activates inflammasomes: implications for gefitinib-induced idiosyncratic reaction. J Toxicol Sci. 2020;45(11):673-680. doi: 10.2131/jts.45.673.
• [200] Consequences of the natural retinoid/retinoid X receptor ligands action in human breast cancer MDA-MB-231 cell line: Focus on functional proteomics. Toxicol Lett. 2017 Nov 5;281:26-34. doi: 10.1016/j.toxlet.2017.09.001. Epub 2017 Sep 5.
• [201] Comparative gene expression profiling reveals partially overlapping but distinct genomic actions of different antiestrogens in human breast cancer cells. J Cell Biochem. 2006 Aug 1;98(5):1163-84.
• [202] Comparison of the gene expression profiles of monocytic versus granulocytic lineages of HL-60 leukemia cell differentiation by DNA microarray analysis. Life Sci. 2003 Aug 15;73(13):1705-19. doi: 10.1016/s0024-3205(03)00515-0.
• [203] Lon protease and eiF2 are involved in acute, but not prolonged, antiretroviral induced stress response in HepG2 cells. Chem Biol Interact. 2016 May 25;252:82-6. doi: 10.1016/j.cbi.2016.03.021. Epub 2016 Apr 1.
• [204] Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
• [205] Motexafin gadolinium and zinc induce oxidative stress responses and apoptosis in B-cell lymphoma lines. Cancer Res. 2005 Dec 15;65(24):11676-88.
• [206] Darinaparsin induces a unique cellular response and is active in an arsenic trioxide-resistant myeloma cell line. Mol Cancer Ther. 2009 May;8(5):1197-206.
• [207] Some HIV antiretrovirals increase oxidative stress and alter chemokine, cytokine or adiponectin production in human adipocytes and macrophages. Antivir Ther. 2007;12(4):489-500.
• [208] Crosstalk between alveolar macrophages and alveolar epithelial cells/fibroblasts contributes to the pulmonary toxicity of gefitinib. Toxicol Lett. 2021 Mar 1;338:1-9. doi: 10.1016/j.toxlet.2020.11.011. Epub 2020 Nov 25.
• [209] Oxidative Stress Alters miRNA and Gene Expression Profiles in Villous First Trimester Trophoblasts. Biomed Res Int. 2015;2015:257090. doi: 10.1155/2015/257090. Epub 2015 Aug 3.
• [210] Cannabidiol selectively modulates interleukin (IL)-1 and IL-6 production in toll-like receptor activated human peripheral blood monocytes. Toxicology. 2021 Dec;464:153016. doi: 10.1016/j.tox.2021.153016. Epub 2021 Nov 2.
• [211] Monitoring of deiodinase deficiency based on transcriptomic responses in SH-SY5Y cells. Arch Toxicol. 2013 Jun;87(6):1103-13. doi: 10.1007/s00204-013-1018-4. Epub 2013 Feb 10.
• [212] Dimethyl Fumarate Inhibits the Nuclear Factor B Pathway in Breast Cancer Cells by Covalent Modification of p65 Protein. J Biol Chem. 2016 Feb 12;291(7):3639-47. doi: 10.1074/jbc.M115.679704. Epub 2015 Dec 18.
• [213] Simvastatin reduces expression of cytokines interleukin-6, interleukin-8, and monocyte chemoattractant protein-1 in circulating monocytes from hypercholesterolemic patients. Arterioscler Thromb Vasc Biol. 2002 Jul 1;22(7):1194-9. doi: 10.1161/01.atv.0000022694.16328.cc.
• [214] Plant polyphenols differentially modulate inflammatory responses of human keratinocytes by interfering with activation of transcription factors NFB and AhR and EGFR-ERK pathway. Toxicol Appl Pharmacol. 2011 Sep 1;255(2):138-49.
• [215] p21(WAF1/cip1) is an important determinant of intestinal cell response to sulindac in vitro and in vivo. Cancer Res. 2001 Aug 15;61(16):6297-302.
• [216] Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
• [217] DNA array analysis of the effects of aspirin on colon cancer cells: involvement of Rac1. Carcinogenesis. 2004 Jul;25(7):1293-8.
• [218] 1,25-Dihydroxyvitamin D3 suppresses gene expression of eukaryotic translation initiation factor 2 in human promyelocytic leukemia HL-60 cells. Cell Struct Funct. 2005;30(1):1-6. doi: 10.1247/csf.30.1.
• [219] Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
• [220] Cannabidiol Displays Proteomic Similarities to Antipsychotics in Cuprizone-Exposed Human Oligodendrocytic Cell Line MO3.13. Front Mol Neurosci. 2021 May 28;14:673144. doi: 10.3389/fnmol.2021.673144. eCollection 2021.
• [221] Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
• [222] Genomic and proteomic analysis of the effects of cannabinoids on normal human astrocytes. Brain Res. 2008 Jan 29;1191:1-11.
• [223] Integrated 'omics analysis reveals new drug-induced mitochondrial perturbations in human hepatocytes. Toxicol Lett. 2018 Jun 1;289:1-13.
• [224] Effects of acute ethanol treatment on NCCIT cells and NCCIT cell-derived embryoid bodies (EBs). Toxicol In Vitro. 2010 Sep;24(6):1696-704. doi: 10.1016/j.tiv.2010.05.017. Epub 2010 May 26.
• [225] Oxidative stress modulates expression of immune checkpoint genes via activation of AhR signaling. Toxicol Appl Pharmacol. 2022 Dec 15;457:116314. doi: 10.1016/j.taap.2022.116314. Epub 2022 Nov 9.
• [226] Profiling of enantiopure drugs towards aryl hydrocarbon (AhR), glucocorticoid (GR) and pregnane X (PXR) receptors in human reporter cell lines. Chem Biol Interact. 2014 Feb 5;208:64-76. doi: 10.1016/j.cbi.2013.11.018. Epub 2013 Dec 6.
• [227] Involvement of cytoskeleton in AhR-dependent CYP1A1 expression. Curr Drug Metab. 2006 Apr;7(3):301-13. doi: 10.2174/138920006776359310.
• [228] Sulindac and its metabolites induce carcinogen metabolizing enzymes in human colon cancer cells. Int J Cancer. 2008 Mar 1;122(5):990-8.
• [229] Quercetin, quercetin glycosides and taxifolin differ in their ability to induce AhR activation and CYP1A1 expression in HepG2 cells. Phytother Res. 2012 Nov;26(11):1746-52.
• [230] Omeprazole inhibits pancreatic cancer cell invasion through a nongenomic aryl hydrocarbon receptor pathway. Chem Res Toxicol. 2015 May 18;28(5):907-18.
• [231] Expression and inducibility of cytochrome P450s (CYP1A1, 2B6, 2E1, 3A4) in human cord blood CD34(+) stem cell-derived differentiating neuronal cells. Toxicol Sci. 2012 Oct;129(2):392-410.
• [232] Different apoptosis ratios and gene expressions in two human cell lines after sevoflurane anaesthesia. Acta Anaesthesiol Scand. 2009 Oct;53(9):1192-9. doi: 10.1111/j.1399-6576.2009.02036.x. Epub 2009 Jun 30.
• [233] [Mechanisms underlying the effect of arsenic trioxide on proliferation inhibition and apoptosis induction in myeloma cell line u266]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2007 Oct;15(5):982-5.
• [234] Lovastatin lactone elicits human lung cancer cell apoptosis via a COX-2/PPAR-dependent pathway. Oncotarget. 2016 Mar 1;7(9):10345-62. doi: 10.18632/oncotarget.7213.
• [235] Induction of apoptosis by cidofovir in human papillomavirus (HPV)-positive cells. Oncol Res. 2000;12(9-10):397-408. doi: 10.3727/096504001108747855.
• [236] Comparison of burst of reactive oxygen species and activation of caspase-3 in apoptosis of K562 and HL-60 cells induced by docetaxel. Cancer Lett. 2004 Oct 8;214(1):103-13. doi: 10.1016/j.canlet.2004.03.047.
• [237] Induction of mitochondrial manganese superoxide dismutase confers resistance to apoptosis in acute myeloblastic leukaemia cells exposed to etoposide. Br J Haematol. 2000 Mar;108(3):574-81. doi: 10.1046/j.1365-2141.2000.01852.x.
• [238] Cisplatin-enhanced sensitivity of glioblastoma multiforme U251 cells to adenovirus-delivered TRAIL in vitro. Tumour Biol. 2010 Dec;31(6):613-22. doi: 10.1007/s13277-010-0077-x. Epub 2010 Jul 11.
• [239] Insulin-like growth factor I is the key growth factor in serum that protects neuroblastoma cells from hyperosmotic-induced apoptosis. J Cell Physiol. 2000 Jan;182(1):24-32. doi: 10.1002/(SICI)1097-4652(200001)182:1<24::AID-JCP3>3.0.CO;2-6.
• [240] mRNA expression analysis of a variety of apoptosis-related genes, including the novel gene of the BCL2-family, BCL2L12, in HL-60 leukemia cells after treatment with carboplatin and doxorubicin. Biol Chem. 2004 Nov;385(11):1099-103. doi: 10.1515/BC.2004.143.
• [241] Neurokinin-1 receptor (NK1R) inhibition sensitizes APL cells to anti-tumor effect of arsenic trioxide via restriction of NF-B axis: Shedding new light on resistance to Aprepitant. Int J Biochem Cell Biol. 2018 Oct;103:105-114. doi: 10.1016/j.biocel.2018.08.010. Epub 2018 Aug 23.
• [242] Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
• [243] Proteomics analysis of the proliferative effect of low-dose ouabain on human endothelial cells. Biol Pharm Bull. 2007 Feb;30(2):247-53. doi: 10.1248/bpb.30.247.
• [244] Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
• [245] Expression Profiling of Human Pluripotent Stem Cell-Derived Cardiomyocytes Exposed to Doxorubicin-Integration and Visualization of Multi-Omics Data. Toxicol Sci. 2018 May 1;163(1):182-195. doi: 10.1093/toxsci/kfy012.
• [246] Inhibiting ubiquitination causes an accumulation of SUMOylated newly synthesized nuclear proteins at PML bodies. J Biol Chem. 2019 Oct 18;294(42):15218-15234. doi: 10.1074/jbc.RA119.009147. Epub 2019 Jul 8.
• [247] Cell-based two-dimensional morphological assessment system to predict cancer drug-induced cardiotoxicity using human induced pluripotent stem cell-derived cardiomyocytes. Toxicol Appl Pharmacol. 2019 Nov 15;383:114761. doi: 10.1016/j.taap.2019.114761. Epub 2019 Sep 15.
• [248] Proteasome inhibition creates a chromatin landscape favorable to RNA Pol II processivity. J Biol Chem. 2020 Jan 31;295(5):1271-1287. doi: 10.1074/jbc.RA119.011174. Epub 2019 Dec 5.
• [249] New insights into the mechanisms underlying 5-fluorouracil-induced intestinal toxicity based on transcriptomic and metabolomic responses in human intestinal organoids. Arch Toxicol. 2021 Aug;95(8):2691-2718. doi: 10.1007/s00204-021-03092-2. Epub 2021 Jun 20.
• [250] Proteomic profile of aminoglutethimide-induced apoptosis in HL-60 cells: role of myeloperoxidase and arylamine free radicals. Chem Biol Interact. 2015 Sep 5;239:129-38.
• [251] Quantitative proteomics and transcriptomics addressing the estrogen receptor subtype-mediated effects in T47D breast cancer cells exposed to the phytoestrogen genistein. Mol Cell Proteomics. 2011 Jan;10(1):M110.002170.
• [252] Proteomic analysis of the cellular response to a potent sensitiser unveils the dynamics of haptenation in living cells. Toxicology. 2020 Dec 1;445:152603. doi: 10.1016/j.tox.2020.152603. Epub 2020 Sep 28.
• [253] Novel ATP-competitive Akt inhibitor afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6(11):2646-2659. doi: 10.1002/cam4.1179. Epub 2017 Sep 27.
• [254] Exome-wide mutation profile in benzo[a]pyrene-derived post-stasis and immortal human mammary epithelial cells. Mutat Res Genet Toxicol Environ Mutagen. 2014 Dec;775-776:48-54. doi: 10.1016/j.mrgentox.2014.10.011. Epub 2014 Nov 4.
• [255] Identification of HMG-CoA reductase inhibitors as activators for human, mouse and rat constitutive androstane receptor. Drug Metab Dispos. 2005 Jul;33(7):924-9.
• [256] Bioactive terpenoids and flavonoids from Ginkgo biloba extract induce the expression of hepatic drug-metabolizing enzymes through pregnane X receptor, constitutive androstane receptor, and aryl hydrocarbon receptor-mediated pathways. Pharm Res. 2009 Apr;26(4):872-82.
• [257] Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes. Chem Biol Interact. 2009 Apr 15;179(1):17-24.
• [258] Fetal bovine serum and human constitutive androstane receptor: evidence for activation of the SV23 splice variant by artemisinin, artemether, and arteether in a serum-free cell culture system. Toxicol Appl Pharmacol. 2014 Jun 1;277(2):221-30. doi: 10.1016/j.taap.2014.03.023. Epub 2014 Apr 12.
• [259] Constitutive androstane/active receptor is a target of retinoic acid receptor in humans. Biochem Pharmacol. 2010 Jul 1;80(1):129-35. doi: 10.1016/j.bcp.2010.02.023. Epub 2010 Mar 6.
• [260] Robustness testing and optimization of an adverse outcome pathway on cholestatic liver injury. Arch Toxicol. 2020 Apr;94(4):1151-1172. doi: 10.1007/s00204-020-02691-9. Epub 2020 Mar 10.
• [261] Agonistic effects of diverse xenobiotics on the constitutive androstane receptor as detected in a recombinant yeast-cell assay. Toxicol In Vitro. 2018 Feb;46:335-349. doi: 10.1016/j.tiv.2017.09.014. Epub 2017 Sep 18.
• [262] Teriflunomide is an indirect human constitutive androstane receptor (CAR) activator interacting with epidermal growth factor (EGF) signaling. Front Pharmacol. 2018 Oct 11;9:993.
• [263] The DNA demethylating agent 5-aza-2'-deoxycytidine activates NY-ESO-1 antigenicity in orthotopic human glioma. Int J Cancer. 2008 Jun 1;122(11):2542-53. doi: 10.1002/ijc.23407.
• [264] Prenatal arsenic exposure and the epigenome: identifying sites of 5-methylcytosine alterations that predict functional changes in gene expression in newborn cord blood and subsequent birth outcomes. Toxicol Sci. 2015 Jan;143(1):97-106. doi: 10.1093/toxsci/kfu210. Epub 2014 Oct 10.
• [265] Predictive toxicology using systemic biology and liver microfluidic "on chip" approaches: application to acetaminophen injury. Toxicol Appl Pharmacol. 2012 Mar 15;259(3):270-80.
• [266] Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.
• [267] Combined tamoxifen and gefitinib in non-small cell lung cancer shows antiproliferative effects. Biomed Pharmacother. 2010 Feb;64(2):88-92. doi: 10.1016/j.biopha.2009.06.010. Epub 2009 Oct 23.
• [268] Quercetin exerts bidirectional regulation effects on the efficacy of tamoxifen in estrogen receptor-positive breast cancer therapy: An in vitro study. Environ Toxicol. 2020 Nov;35(11):1179-1193. doi: 10.1002/tox.22983. Epub 2020 Jun 12.
• [269] Comparison of an array of in vitro assays for the assessment of the estrogenic potential of natural and synthetic estrogens, phytoestrogens and xenoestrogens. Toxicology. 2001 Sep 14;166(1-2):79-89. doi: 10.1016/s0300-483x(01)00437-1.
• [270] Estrogenic effects of natural and synthetic compounds including tibolone assessed in Saccharomyces cerevisiae expressing the human estrogen alpha and beta receptors. FASEB J. 2006 Jul;20(9):1552-4. doi: 10.1096/fj.05-5413fje. Epub 2006 May 23.
• [271] Comparison of relative binding affinities to fish and mammalian estrogen receptors: the regulatory implications. Toxicol Lett. 2010 Feb 15;192(3):298-315. doi: 10.1016/j.toxlet.2009.11.004. Epub 2009 Nov 12.
• [272] Screening for estrogen and androgen receptor activities in 200 pesticides by in vitro reporter gene assays using Chinese hamster ovary cells. Environ Health Perspect. 2004 Apr;112(5):524-31. doi: 10.1289/ehp.6649.
• [273] Valproic acid and its derivatives enhanced estrogenic activity but not androgenic activity in a structure dependent manner. Reprod Toxicol. 2013 Dec;42:49-57. doi: 10.1016/j.reprotox.2013.07.019. Epub 2013 Jul 26.
• [274] Relationship between estrogen receptor-binding and estrogenic activities of environmental estrogens and suppression by flavonoids. Biosci Biotechnol Biochem. 2002 Jul;66(7):1479-87. doi: 10.1271/bbb.66.1479.
• [275] Arylpiperazines for management of benign prostatic hyperplasia: design, synthesis, quantitative structure-activity relationships, and pharmacokinetic studies. J Med Chem. 2011 Jan 13;54(1):302-11. doi: 10.1021/jm101163m. Epub 2010 Dec 3.
• [276] Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802.
• [277] Arsenic trioxide induces different gene expression profiles of genes related to growth and apoptosis in glioma cells dependent on the p53 status. Mol Biol Rep. 2008 Sep;35(3):421-9.
• [278] Transcriptional profiling of testosterone-regulated genes in the skeletal muscle of human immunodeficiency virus-infected men experiencing weight loss. J Clin Endocrinol Metab. 2007 Jul;92(7):2793-802. doi: 10.1210/jc.2006-2722. Epub 2007 Apr 17.
• [279] Anti-oncogenic and pro-differentiation effects of clorgyline, a monoamine oxidase A inhibitor, on high grade prostate cancer cells. BMC Med Genomics. 2009 Aug 20;2:55. doi: 10.1186/1755-8794-2-55.
• [280] Minimal peroxide exposure of neuronal cells induces multifaceted adaptive responses. PLoS One. 2010 Dec 17;5(12):e14352. doi: 10.1371/journal.pone.0014352.
• [281] Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
• [282] Temozolomide induces activation of Wnt/-catenin signaling in glioma cells via PI3K/Akt pathway: implications in glioma therapy. Cell Biol Toxicol. 2020 Jun;36(3):273-278. doi: 10.1007/s10565-019-09502-7. Epub 2019 Nov 22.
• [283] Localization of breast cancer resistance protein (Bcrp) in endocrine organs and inhibition of its transport activity by steroid hormones. Cell Tissue Res. 2012 Aug;349(2):551-63. doi: 10.1007/s00441-012-1417-5. Epub 2012 May 13.
• [284] Pharmacogenetics of ABCG2 and adverse reactions to gefitinib. J Natl Cancer Inst. 2006 Dec 6;98(23):1739-42.
• [285] ABCG2 polymorphism is associated with the low-density lipoprotein cholesterol response to rosuvastatin. Clin Pharmacol Ther. 2010 May;87(5):558-62.
• [286] Ciprofloxacin mediates cancer stem cell phenotypes in lung cancer cells through caveolin-1-dependent mechanism. Chem Biol Interact. 2016 Apr 25;250:1-11.
• [287] Activation of beta-catenin signalling by GSK-3 inhibition increases p-glycoprotein expression in brain endothelial cells. J Neurochem. 2008 Aug;106(4):1855-65. doi: 10.1111/j.1471-4159.2008.05537.x. Epub 2008 Jul 4.
• [288] Differential gene expression in human hepatocyte cell lines exposed to the antiretroviral agent zidovudine. Arch Toxicol. 2014 Mar;88(3):609-23. doi: 10.1007/s00204-013-1169-3. Epub 2013 Nov 30.
• [289] Chronic imatinib mesylate exposure leads to reduced intracellular drug accumulation by induction of the ABCG2 (BCRP) and ABCB1 (MDR1) drug transport pumps. Cancer Biol Ther. 2005 Jul;4(7):747-52.
• [290] Protein expression profiling identifies molecular targets of quercetin as a major dietary flavonoid in human colon cancer cells. Proteomics. 2004 Jul;4(7):2160-74.
• [291] Synergistic effects of retinoic acid and tamoxifen on human breast cancer cells: proteomic characterization. Exp Cell Res. 2007 Jan 15;313(2):357-68. doi: 10.1016/j.yexcr.2006.10.016. Epub 2006 Oct 25.
• [292] Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
• [293] Identification of novel low-dose bisphenol a targets in human foreskin fibroblast cells derived from hypospadias patients. PLoS One. 2012;7(5):e36711. doi: 10.1371/journal.pone.0036711. Epub 2012 May 4.
• [294] Definition of transcriptome-based indices for quantitative characterization of chemically disturbed stem cell development: introduction of the STOP-Toxukn and STOP-Toxukk tests. Arch Toxicol. 2017 Feb;91(2):839-864.
• [295] Gene Expression Regulation and Pathway Analysis After Valproic Acid and Carbamazepine Exposure in a Human Embryonic Stem Cell-Based Neurodevelopmental Toxicity Assay. Toxicol Sci. 2015 Aug;146(2):311-20. doi: 10.1093/toxsci/kfv094. Epub 2015 May 15.
• [296] The antiproliferative effects of progestins in T47D breast cancer cells are tempered by progestin induction of the ETS transcription factor Elf5. Mol Endocrinol. 2010 Jul;24(7):1380-92. doi: 10.1210/me.2009-0516. Epub 2010 Jun 2.