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

General Information of Drug (ID: DMYRUH2)

• Drug Name: I-BET151 Drug Info
• Synonyms: GSK1210151A

Indication

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

• Cross-matching ID:
  PubChem CID: 52912189
  ChEBI ID: CHEMBL2017291
  CAS Number: CAS 1300031-49-5
  TTD Drug ID: DMYRUH2

Molecule-Related Drug Atlas

Drug(s) Targeting Bromodomain-containing protein 4 (BRD4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CPI-0610	DMPXOYJ	Myelofibrosis	2A20.2	Phase 3	[6]
OTX-015	DMI8RG1	Acute myeloid leukaemia	2A60	Phase 1/2	[6]
PLX2853	DMX168L	Acute myeloid leukaemia	2A60	Phase 1/2	[7]
RVX-208	DM1LO8K	Alzheimer disease	8A20	Phase 1/2	[6]
INCB57643	DMBGU7V	Advanced malignancy	2A00-2F9Z	Phase 1/2	[7]
ABBV-744	DMTEA9C	Acute myeloid leukaemia	2A60	Phase 1	[7]
(+)-JQ1	DM1CZSJ	Testicular cancer	2C80	Phase 1	[8]
GSK525762	DMPAWBN	Haematological malignancy	2B33.Y	Phase 1	[6]
TEN010	DM4UOY5	Advanced solid tumour	2A00-2F9Z	Phase 1	[6]
AZD5153	DMW4GM2	Solid tumour/cancer	2A00-2F9Z	Phase 1	[7]

Drug(s) Targeting Bromodomain-containing protein 3 (BRD3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ABBV-744	DMTEA9C	Acute myeloid leukaemia	2A60	Phase 1	[7]
PMID26924192-Compound-104	DM346EU	N. A.	N. A.	Patented	[9]
PMID26924192-Compound-102	DMEJ107	N. A.	N. A.	Patented	[9]
PMID26924192-Compound-103	DMWOCP7	N. A.	N. A.	Patented	[9]
PMID26924192-Compound-105	DMAWLGI	N. A.	N. A.	Patented	[9]
Pyrrolo-pyrrolone derivative 1	DMN4SE5	N. A.	N. A.	Patented	[9]
XD14	DMUMACD	Discovery agent	N.A.	Investigative	[10]
GW841819X	DMRL9IN	Discovery agent	N.A.	Investigative	[11]
PMID24000170C36	DMHUWZS	Discovery agent	N.A.	Investigative	[12]
PMID24000170C38	DMOLRIY	Discovery agent	N.A.	Investigative	[12]

Drug(s) Targeting Bromodomain-containing protein 2 (BRD2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
OTX-015	DMI8RG1	Acute myeloid leukaemia	2A60	Phase 1/2	[6]
ABBV-744	DMTEA9C	Acute myeloid leukaemia	2A60	Phase 1	[7]
PMID26924192-Compound-104	DM346EU	N. A.	N. A.	Patented	[9]
PMID26924192-Compound-102	DMEJ107	N. A.	N. A.	Patented	[9]
PMID26924192-Compound-103	DMWOCP7	N. A.	N. A.	Patented	[9]
PMID26924192-Compound-105	DMAWLGI	N. A.	N. A.	Patented	[9]
Pyrrolo-pyrrolone derivative 1	DMN4SE5	N. A.	N. A.	Patented	[9]
PMID26924192-Compound-106	DM9HRZJ	N. A.	N. A.	Patented	[9]
XD14	DMUMACD	Discovery agent	N.A.	Investigative	[10]
GW841819X	DMRL9IN	Discovery agent	N.A.	Investigative	[11]

Drug(s) Affected By Protein HEXIM1 (HEXIM1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[13]
Leflunomide	DMR8ONJ	Arthritis	FA20	Approved	[14]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[15]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[16]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[17]
Amiodarone	DMUTEX3	Tachyarrhythmias	BC71	Approved	[18]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[19]
Piroxicam	DMTK234	Osteoarthritis	FA00-FA05	Approved	[20]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[21]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[22]

Drug(s) Affected By Cyclin-dependent kinase inhibitor 1B (CDKN1B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[23]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[24]
Prednisone	DM2HG4X	Acute asthma	CA23	Approved	[25]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[26]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[27]
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[28]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[29]
Fluoxetine	DM3PD2C	Bipolar depression		Approved	[30]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[31]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[32]

Drug(s) Affected By Baculoviral IAP repeat-containing protein 5 (BIRC5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[33]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[34]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[35]
Nitric Oxide	DM1RBYG	Hypertension	BA00-BA04	Approved	[36]
Etretinate	DM2CZFA	Keratosis	ED56	Approved	[37]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[38]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[39]
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[40]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[41]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[42]

Drug(s) Affected By Metalloproteinase inhibitor 1 (TIMP1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pentoxifylline	DMU3DNC	Alcoholic hepatitis	DB94.1	Approved	[43]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[44]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[45]
Selenium	DM25CGV	N. A.	N. A.	Approved	[46]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[45]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[47]
obeticholic acid	DM3Q1SM	Primary biliary cholangitis	DB96.1	Approved	[48]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[49]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[50]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[51]

Drug(s) Affected By Myc proto-oncogene protein (MYC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[52]
Sertraline	DM0FB1J	Coronary heart disease	BA80.Z	Approved	[53]
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[54]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[55]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[56]
Selenium	DM25CGV	N. A.	N. A.	Approved	[57]
Ribavirin	DMEYLH9	Hepatitis C virus infection	1E51.1	Approved	[58]
Trametinib	DM2JGQ3	Melanoma	2C30	Approved	[59]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[60]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[61]

Drug(s) Affected By Collagen alpha-1(I) chain (COL1A1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Penicillamine	DM40EF6	Cystinuria	5C60.2	Approved	[43]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[62]
Diazepam	DM08E9O	Alcohol withdrawal		Approved	[63]
Beta-carotene	DM0RXBT	Vitamin deficiency	5B55-5B71	Approved	[64]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[65]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[66]
Ceruletide	DM2WE5K	Caerulein stimulated gastric and pancreatic secretion	5A4Y	Approved	[67]
Dactinomycin	DM2YGNW	Adult kidney Wilms tumor		Approved	[68]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[69]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[70]

Drug(s) Affected By Collagen alpha-2(I) chain (COL1A2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[13]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[71]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[72]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[73]
Aldosterone	DM9S2JW	Hypertension	BA00-BA04	Approved	[74]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[75]
Testosterone enanthate	DMB6871	N. A.	N. A.	Approved	[76]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[16]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[17]
Dexamethasone	DMMWZET	Acute adrenal insufficiency		Approved	[77]

Drug(s) Affected By Protein L-Myc (MYCL)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[78]
Hydroquinone	DM6AVR4	Melasma	ED60.1	Approved	[79]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[80]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[81]
Leflunomide	DMR8ONJ	Arthritis	FA20	Approved	[14]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[82]
Niclosamide	DMJAGXQ	Cestodes infection	1F70-1F76	Approved	[83]
Cupric Sulfate	DMP0NFQ	Fungal infection	1F29-1F2F	Approved	[84]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[85]
Urethane	DM7NSI0	N. A.	N. A.	Phase 4	[86]

Drug(s) Affected By Intercellular adhesion molecule 2 (ICAM2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[13]
Isotretinoin	DM4QTBN	Acne vulgaris	ED80	Approved	[87]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[80]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[88]
Cupric Sulfate	DMP0NFQ	Fungal infection	1F29-1F2F	Approved	[84]
Decitabine	DMQL8XJ	Acute myelogenous leukaemia	2A41	Approved	[89]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[90]
Arsenic	DMTL2Y1	N. A.	N. A.	Approved	[91]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[21]
Urethane	DM7NSI0	N. A.	N. A.	Phase 4	[86]

Drug(s) Affected By Integrin beta-5 (ITGB5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[92]
Methimazole	DM25FL8	Hyperthyroidism	5A02	Approved	[93]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[71]
Propylthiouracil	DM6D7N8	Hyperthyroidism	5A02	Approved	[93]
Liothyronine	DM6IR3P	Congenital hypothyroidism		Approved	[93]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[71]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[17]
Zoledronate	DMIXC7G	Adenocarcinoma	2D40	Approved	[94]
Amiodarone	DMUTEX3	Tachyarrhythmias	BC71	Approved	[93]
Cupric Sulfate	DMP0NFQ	Fungal infection	1F29-1F2F	Approved	[84]

Drug(s) Affected By Collagen alpha-1(V) chain (COL5A1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[95]
Isotretinoin	DM4QTBN	Acne vulgaris	ED80	Approved	[87]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[75]
Testosterone enanthate	DMB6871	N. A.	N. A.	Approved	[76]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[16]
Zoledronate	DMIXC7G	Adenocarcinoma	2D40	Approved	[96]
Dexamethasone	DMMWZET	Acute adrenal insufficiency		Approved	[77]
Ethinyl Estradiol	DMODJ40	Acne vulgaris	ED80	Approved	[97]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[98]
Amphotericin B	DMTAJQE	Acne vulgaris	ED80	Approved	[99]

Drug(s) Affected By Protein-lysine 6-oxidase (LOX)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[100]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[101]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[102]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[13]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[81]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[15]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[82]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[103]
Ampicillin	DMHWE7P	Acute epiglottitis		Approved	[102]
Cupric Sulfate	DMP0NFQ	Fungal infection	1F29-1F2F	Approved	[84]

Drug(s) Affected By Thrombospondin-2 (THBS2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[104]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[105]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[71]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[80]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[73]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[75]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[16]
Ifosfamide	DMCT3I8	Adult central nervous system germ cell tumor		Approved	[106]
Dasatinib	DMJV2EK	Blast phase chronic myelogenous leukemia, BCR-ABL1 positive		Approved	[107]
Temozolomide	DMKECZD	Adenocarcinoma	2D40	Approved	[108]

Drug(s) Affected By Fibrillin-1 (FBN1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Etretinate	DM2CZFA	Keratosis	ED56	Approved	[109]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[110]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[95]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[71]
Leflunomide	DMR8ONJ	Arthritis	FA20	Approved	[14]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[111]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[82]
Zoledronate	DMIXC7G	Adenocarcinoma	2D40	Approved	[112]
Paclitaxel	DMLB81S	Breast carcinoma		Approved	[113]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[22]

Drug(s) Affected By Serine/threonine-protein kinase PLK1 (PLK1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[114]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[115]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[116]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[102]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[110]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[117]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[118]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[119]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[119]
Leflunomide	DMR8ONJ	Arthritis	FA20	Approved	[14]

Drug(s) Affected By Actin, aortic smooth muscle (ACTA2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[120]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[121]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[122]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[123]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[124]
Pirfenidone	DM6VZFQ	Idiopathic pulmonary fibrosis	CB03.4	Approved	[125]
Marinol	DM70IK5	Anorexia nervosa cachexia	6B80	Approved	[126]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[119]
Acocantherin	DM7JT24	Atrial fibrillation	BC81.3	Approved	[127]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[119]

Drug(s) Affected By Lysyl oxidase homolog 1 (LOXL1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[128]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[73]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[16]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[129]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[130]
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[22]
DTI-015	DMXZRW0	Brain cancer	2A00	Approved	[131]
Carbamazepine	DMZOLBI	Epilepsy	8A60-8A68	Approved	[88]
SNDX-275	DMH7W9X	Breast cancer	2C60-2C65	Phase 3	[132]
(+)-JQ1	DM1CZSJ	Testicular cancer	2C80	Phase 1	[3]

Drug(s) Affected By Mitogen-activated protein kinase kinase kinase 1 (MAP3K1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Quercetin	DM3NC4M	Obesity	5B81	Approved	[133]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[122]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[73]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[15]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[16]
Menthol	DMG2KW7	Back pain	ME84.Z	Approved	[134]
Temozolomide	DMKECZD	Adenocarcinoma	2D40	Approved	[108]
Paclitaxel	DMLB81S	Breast carcinoma		Approved	[135]
Cupric Sulfate	DMP0NFQ	Fungal infection	1F29-1F2F	Approved	[84]
Arsenic	DMTL2Y1	N. A.	N. A.	Approved	[136]

Drug(s) Affected By Carbonic anhydrase 9 (CA9)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Acetazolamide	DM1AF5U	Absence epilepsy		Approved	[137]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[101]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[138]
Hydroquinone	DM6AVR4	Melasma	ED60.1	Approved	[79]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[73]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[15]
Ampicillin	DMHWE7P	Acute epiglottitis		Approved	[102]
Temozolomide	DMKECZD	Adenocarcinoma	2D40	Approved	[108]
Bortezomib	DMNO38U	Leukemia		Approved	[139]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[98]

Drug(s) Affected By 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Quercetin	DM3NC4M	Obesity	5B81	Approved	[102]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[140]
Acetic Acid, Glacial	DM4SJ5Y	infection in the ear canal	AA0Y	Approved	[141]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[38]
Leflunomide	DMR8ONJ	Arthritis	FA20	Approved	[14]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[15]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[16]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[17]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[129]
Motexafin gadolinium	DMEJKRF	Brain cancer	2A00	Approved	[141]

Drug(s) Affected By Tumor protein p53-inducible nuclear protein 1 (TP53INP1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[128]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[142]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[102]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[95]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[143]
Hydroquinone	DM6AVR4	Melasma	ED60.1	Approved	[144]
Ibuprofen	DM8VCBE	Dysmenorrhea	GA34.3	Approved	[106]
Clodronate	DM9Y6X7	Hypercalcaemia	5B91.0	Approved	[106]
Cidofovir	DMA13GD	Cytomegalovirus infection	1D82	Approved	[106]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[16]

Drug(s) Affected By Endothelial PAS domain-containing protein 1 (EPAS1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[145]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[61]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[146]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[140]
Panobinostat	DM58WKG	Chronic graft versus host disease		Approved	[71]
Ibuprofen	DM8VCBE	Dysmenorrhea	GA34.3	Approved	[147]
Leflunomide	DMR8ONJ	Arthritis	FA20	Approved	[14]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[15]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[82]
Ketorolac	DMI4EL5	Postoperative inflammation	1A00-CA43.1	Approved	[147]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Bromodomain-containing protein 2 (BRD2)	TTDP48B	BRD2_HUMAN	Inhibitor	[1]
Bromodomain-containing protein 3 (BRD3)	TTHE657	BRD3_HUMAN	Inhibitor	[1]
Bromodomain-containing protein 4 (BRD4)	TTRA6BO	BRD4_HUMAN	Inhibitor	[1]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3)	OT25JBA3	F263_HUMAN	Gene/Protein Processing	[2]
Actin, aortic smooth muscle (ACTA2)	OTEDLG8E	ACTA_HUMAN	Gene/Protein Processing	[3]
Baculoviral IAP repeat-containing protein 5 (BIRC5)	OTILXZYL	BIRC5_HUMAN	Gene/Protein Processing	[4]
Carbonic anhydrase 9 (CA9)	OTNA51XT	CAH9_HUMAN	Gene/Protein Processing	[2]
Collagen alpha-1(I) chain (COL1A1)	OTI31178	CO1A1_HUMAN	Gene/Protein Processing	[3]
Collagen alpha-1(V) chain (COL5A1)	OT24078H	CO5A1_HUMAN	Gene/Protein Processing	[3]
Collagen alpha-2(I) chain (COL1A2)	OTY7G382	CO1A2_HUMAN	Gene/Protein Processing	[3]
Cyclin-dependent kinase inhibitor 1B (CDKN1B)	OTNY5LLZ	CDN1B_HUMAN	Gene/Protein Processing	[5]
Endothelial PAS domain-containing protein 1 (EPAS1)	OTRE3O8U	EPAS1_HUMAN	Gene/Protein Processing	[2]
Fibrillin-1 (FBN1)	OTYCJT63	FBN1_HUMAN	Gene/Protein Processing	[3]

References

• [1] Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature. 2011 Oct 2;478(7370):529-33.
• [2] The BET inhibitor JQ1 selectively impairs tumour response to hypoxia and downregulates CA9 and angiogenesis in triple negative breast cancer. Oncogene. 2017 Jan 5;36(1):122-132. doi: 10.1038/onc.2016.184. Epub 2016 Jun 13.
• [3] BRD4 is a novel therapeutic target for liver fibrosis. Proc Natl Acad Sci U S A. 2015 Dec 22;112(51):15713-8. doi: 10.1073/pnas.1522163112. Epub 2015 Dec 7.
• [4] BET Bromodomain Inhibition as a Therapeutic Strategy in Ovarian Cancer by Downregulating FoxM1. Theranostics. 2016 Jan 1;6(2):219-30. doi: 10.7150/thno.13178. eCollection 2016.
• [5] Synergistic activity of BET protein antagonist-based combinations in mantle cell lymphoma cells sensitive or resistant to ibrutinib. Blood. 2015 Sep 24;126(13):1565-74.
• [6] Targeting bromodomains: epigenetic readers of lysine acetylation.Nat Rev Drug Discov.2014 May;13(5):337-56.
• [7] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [8] Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73.
• [9] BET inhibitors in cancer therapeutics: a patent review.Expert Opin Ther Pat. 2016;26(4):505-22.
• [10] 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading. Angew Chem Int Ed Engl. 2013 Dec 23;52(52):14055-9.
• [11] Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J Med Chem. 2011 Jun 9;54(11):3827-38.
• [12] Naphthyridines as novel BET family bromodomain inhibitors. ChemMedChem. 2014 Mar;9(3):580-9.
• [13] Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
• [14] Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
• [15] 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.
• [16] 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.
• [17] 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.
• [18] Identification by automated screening of a small molecule that selectively eliminates neural stem cells derived from hESCs but not dopamine neurons. PLoS One. 2009 Sep 23;4(9):e7155.
• [19] The thioxotriazole copper(II) complex A0 induces endoplasmic reticulum stress and paraptotic death in human cancer cells. J Biol Chem. 2009 Sep 4;284(36):24306-19.
• [20] Apoptosis induced by piroxicam plus cisplatin combined treatment is triggered by p21 in mesothelioma. PLoS One. 2011;6(8):e23569.
• [21] Gene expression analysis of precision-cut human liver slices indicates stable expression of ADME-Tox related genes. Toxicol Appl Pharmacol. 2011 May 15;253(1):57-69.
• [22] Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
• [23] Therapeutically activating RB: reestablishing cell cycle control in endocrine therapy-resistant breast cancer. Endocr Relat Cancer. 2011 Apr 28;18(3):333-45. doi: 10.1530/ERC-10-0262. Print 2011 Jun.
• [24] Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res. 2006 Jun 1;66(11):5542-8. doi: 10.1158/0008-5472.CAN-05-4620.
• [25] Glucocorticoids induce G1 arrest of lymphoblastic cells through retinoblastoma protein Rb1 dephosphorylation in childhood acute lymphoblastic leukemia in vivo. Cancer Biol Ther. 2004 May;3(5):470-6. doi: 10.4161/cbt.3.5.838. Epub 2004 May 9.
• [26] Methotrexate increases expression of cell cycle checkpoint genes via JNK activation. Arthritis Rheum. 2012 Jun;64(6):1780-9. doi: 10.1002/art.34342. Epub 2011 Dec 19.
• [27] Simvastatin inhibits growth via apoptosis and the induction of cell cycle arrest in human melanoma cells. Melanoma Res. 2008 Apr;18(2):85-94. doi: 10.1097/CMR.0b013e3282f60097.
• [28] The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. Cancer Res. 2005 Jan 1;65(1):18-25.
• [29] Effects of structurally related flavonoids on cell cycle progression of human melanoma cells: regulation of cyclin-dependent kinases CDK2 and CDK1. Biochem Pharmacol. 2001 May 15;61(10):1205-15. doi: 10.1016/s0006-2952(01)00583-4.
• [30] Fluoxetine mediates G0/G1 arrest by inducing functional inhibition of cyclin dependent kinase subunit (CKS)1. Biochem Pharmacol. 2008 May 15;75(10):1924-34. doi: 10.1016/j.bcp.2008.02.013. Epub 2008 Feb 17.
• [31] Induction mechanism of apoptosis by troglitazone through peroxisome proliferator-activated receptor-gamma in gastric carcinoma cells. Anticancer Res. 2003 Jan-Feb;23(1A):267-73.
• [32] Down-regulation of CD44 contributes to the differentiation of HL-60 cells induced by ATRA or HMBA. Cell Mol Immunol. 2007 Feb;4(1):59-63.
• [33] mTOR inhibition reverses acquired endocrine therapy resistance of breast cancer cells at the cell proliferation and gene-expression levels. Cancer Sci. 2008 Oct;99(10):1992-2003. doi: 10.1111/j.1349-7006.2008.00955.x.
• [34] Leptomycin B reduces primary and acquired resistance of gefitinib in lung cancer cells. Toxicol Appl Pharmacol. 2017 Nov 15;335:16-27. doi: 10.1016/j.taap.2017.09.017. Epub 2017 Sep 21.
• [35] Assessment of the cytotoxic, genotoxic, and apoptotic potential of flurbiprofen in HeLa and HepG2 cell lines. J Biochem Mol Toxicol. 2021 Jun;35(6):1-11. doi: 10.1002/jbt.22770. Epub 2021 Mar 11.
• [36] 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.
• [37] Bexarotene activates the p53/p73 pathway in human cutaneous T-cell lymphoma. Br J Dermatol. 2009 Mar;160(3):519-26. doi: 10.1111/j.1365-2133.2008.08931.x. Epub 2008 Nov 25.
• [38] Expression profile analysis of colon cancer cells in response to sulindac or aspirin. Biochem Biophys Res Commun. 2002 Mar 29;292(2):498-512.
• [39] Apoptotic induction by simvastatin in human lung cancer A549 cells via Akt signaling dependent down-regulation of survivin. Invest New Drugs. 2011 Oct;29(5):945-52. doi: 10.1007/s10637-010-9450-2. Epub 2010 May 13.
• [40] Combining lapatinib (GW572016), a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases, with therapeutic anti-ErbB2 antibodies enhances apoptosis of ErbB2-overexpressing breast cancer cells. Oncogene. 2005 Sep 15;24(41):6213-21. doi: 10.1038/sj.onc.1208774.
• [41] Quercetin inhibit human SW480 colon cancer growth in association with inhibition of cyclin D1 and survivin expression through Wnt/beta-catenin signaling pathway. Cancer Invest. 2009 Jul;27(6):604-12. doi: 10.1080/07357900802337191.
• [42] Troglitazone sensitizes tumor cells to TRAIL-induced apoptosis via down-regulation of FLIP and Survivin. Apoptosis. 2006 Sep;11(9):1503-12. doi: 10.1007/s10495-006-8896-3.
• [43] 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.
• [44] Cannabidiol inhibits lung cancer cell invasion and metastasis via intercellular adhesion molecule-1. FASEB J. 2012 Apr;26(4):1535-48. doi: 10.1096/fj.11-198184. Epub 2011 Dec 23.
• [45] Discovery of molecular mechanisms of neuroprotection using cell-based bioassays and oligonucleotide arrays. Physiol Genomics. 2002 Oct 29;11(2):45-52. doi: 10.1152/physiolgenomics.00064.2002.
• [46] Inhibition of invasion and induction of apoptosis by selenium in human malignant brain tumour cells in vitro. Int J Oncol. 2007 May;30(5):1263-71.
• [47] Dietary supplementation with the anti-tumour promoter quercetin: its effects on matrix metalloproteinase gene regulation. Mutat Res. 2001 Sep 1;480-481:269-76. doi: 10.1016/s0027-5107(01)00184-1.
• [48] Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
• [49] 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.
• [50] Arsenic trioxide (As2O3) inhibits invasion of HT1080 human fibrosarcoma cells: role of nuclear factor-kappaB and reactive oxygen species. J Cell Biochem. 2005 Aug 1;95(5):955-69. doi: 10.1002/jcb.20452.
• [51] Aspirin inhibits MMP-2 and MMP-9 expressions and activities through upregulation of PPARalpha/gamma and TIMP gene expressions in ox-LDL-stimulated macrophages derived from human monocytes. Pharmacology. 2009;83(1):18-25. doi: 10.1159/000166183. Epub 2008 Oct 30.
• [52] Acetaminophen-induced proliferation of estrogen-responsive breast cancer cells is associated with increases in c-myc RNA expression and NF-kappaB activity. Toxicol Sci. 2002 Apr;66(2):233-43. doi: 10.1093/toxsci/66.2.233.
• [53] 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.
• [54] Estrogen regulation in human breast cancer cells of new downstream gene targets involved in estrogen metabolism, cell proliferation and cell transformation. J Mol Endocrinol. 2004 Apr;32(2):397-414.
• [55] ZD1839 induces p15INK4b and causes G1 arrest by inhibiting the mitogen-activated protein kinase/extracellular signal-regulated kinase pathway. Mol Cancer Ther. 2007 May;6(5):1579-87. doi: 10.1158/1535-7163.MCT-06-0814.
• [56] Arsenic suppresses gene expression in promyelocytic leukemia cells partly through Sp1 oxidation. Blood. 2005 Jul 1;106(1):304-10.
• [57] Selenite and selenomethionine promote HL-60 cell cycle progression. J Nutr. 2002 Apr;132(4):674-9. doi: 10.1093/jn/132.4.674.
• [58] Ribavirin augments doxorubicin's efficacy in human hepatocellular carcinoma through inhibiting doxorubicin-induced eIF4E activation. J Biochem Mol Toxicol. 2018 Jan;32(1). doi: 10.1002/jbt.22007. Epub 2017 Nov 7.
• [59] Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner. Clin Cancer Res. 2012 Aug 15;18(16):4345-55. doi: 10.1158/1078-0432.CCR-11-3227. Epub 2012 Jun 25.
• [60] Novel detection and differential utilization of a c-myc transcriptional block in colon cancer chemoprevention. Cancer Res. 2002 Nov 1;62(21):6006-10.
• [61] The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
• [62] Investigation of in vitro odonto/osteogenic capacity of cannabidiol on human dental pulp cell. J Dent. 2021 Jun;109:103673. doi: 10.1016/j.jdent.2021.103673. Epub 2021 Apr 16.
• [63] Patterns of some extracellular matrix gene expression are similar in cells from cleft lip-palate patients and in human palatal fibroblasts exposed to diazepam in culture. Toxicology. 2009 Mar 4;257(1-2):10-6. doi: 10.1016/j.tox.2008.12.002. Epub 2008 Dec 9.
• [64] Beta-carotene and apocarotenals promote retinoid signaling in BEAS-2B human bronchioepithelial cells. Arch Biochem Biophys. 2006 Nov 1;455(1):48-60.
• [65] Protective effects of myricitrin against osteoporosis via reducing reactive oxygen species and bone-resorbing cytokines. Toxicol Appl Pharmacol. 2014 Nov 1;280(3):550-60.
• [66] Gene expression profiling of rheumatoid arthritis synovial cells treated with antirheumatic drugs. J Biomol Screen. 2007 Apr;12(3):328-40. doi: 10.1177/1087057107299261. Epub 2007 Mar 22.
• [67] Acinar cell-specific knockout of the PTHrP gene decreases the proinflammatory and profibrotic responses in pancreatitis. Am J Physiol Gastrointest Liver Physiol. 2014 Sep 1;307(5):G533-49. doi: 10.1152/ajpgi.00428.2013. Epub 2014 Jul 17.
• [68] The effects of particulate wear debris, cytokines, and growth factors on the functions of MG-63 osteoblasts. J Bone Joint Surg Am. 2001 Feb;83(2):201-11. doi: 10.2106/00004623-200102000-00007.
• [69] Inhibition of systemic sclerosis dermal fibroblast type I collagen production and gene expression by simvastatin. Arthritis Rheum. 2006 Apr;54(4):1298-308. doi: 10.1002/art.21723.
• [70] Antifibrotic effects of quercetin in primary orbital fibroblasts and orbital fat tissue cultures of Graves' orbitopathy. Invest Ophthalmol Vis Sci. 2012 Aug 31;53(9):5921-9. doi: 10.1167/iovs.12-9646.
• [71] 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.
• [72] Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
• [73] Identification of vitamin D3 target genes in human breast cancer tissue. J Steroid Biochem Mol Biol. 2016 Nov;164:90-97.
• [74] Modelling cardiac fibrosis using three-dimensional cardiac microtissues derived from human embryonic stem cells. J Biol Eng. 2019 Feb 13;13:15. doi: 10.1186/s13036-019-0139-6. eCollection 2019.
• [75] Primary Human Hepatocyte Spheroids as Tools to Study the Hepatotoxic Potential of Non-Pharmaceutical Chemicals. Int J Mol Sci. 2021 Oct 12;22(20):11005. doi: 10.3390/ijms222011005.
• [76] 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.
• [77] Identification of mechanisms of action of bisphenol a-induced human preadipocyte differentiation by transcriptional profiling. Obesity (Silver Spring). 2014 Nov;22(11):2333-43.
• [78] Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
• [79] Keratinocyte-derived IL-36gama plays a role in hydroquinone-induced chemical leukoderma through inhibition of melanogenesis in human epidermal melanocytes. Arch Toxicol. 2019 Aug;93(8):2307-2320.
• [80] The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
• [81] Large-scale in silico and microarray-based identification of direct 1,25-dihydroxyvitamin D3 target genes. Mol Endocrinol. 2005 Nov;19(11):2685-95.
• [82] Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
• [83] Mitochondrial Uncoupling Induces Epigenome Remodeling and Promotes Differentiation in Neuroblastoma. Cancer Res. 2023 Jan 18;83(2):181-194. doi: 10.1158/0008-5472.CAN-22-1029.
• [84] Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
• [85] 17-Estradiol Activates HSF1 via MAPK Signaling in ER-Positive Breast Cancer Cells. Cancers (Basel). 2019 Oct 11;11(10):1533. doi: 10.3390/cancers11101533.
• [86] Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
• [87] 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.
• [88] 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.
• [89] Chemical genomic screening for methylation-silenced genes in gastric cancer cell lines using 5-aza-2'-deoxycytidine treatment and oligonucleotide microarray. Cancer Sci. 2006 Jan;97(1):64-71.
• [90] Low doses of cisplatin induce gene alterations, cell cycle arrest, and apoptosis in human promyelocytic leukemia cells. Biomark Insights. 2016 Aug 24;11:113-21.
• [91] 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.
• [92] Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
• [93] 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.
• [94] Interleukin-19 as a translational indicator of renal injury. Arch Toxicol. 2015 Jan;89(1):101-6.
• [95] Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
• [96] Zoledronate dysregulates fatty acid metabolism in renal tubular epithelial cells to induce nephrotoxicity. Arch Toxicol. 2018 Jan;92(1):469-485.
• [97] The genomic response of a human uterine endometrial adenocarcinoma cell line to 17alpha-ethynyl estradiol. Toxicol Sci. 2009 Jan;107(1):40-55.
• [98] Activation of AIFM2 enhances apoptosis of human lung cancer cells undergoing toxicological stress. Toxicol Lett. 2016 Sep 6;258:227-236.
• [99] Differential expression of microRNAs and their predicted targets in renal cells exposed to amphotericin B and its complex with copper (II) ions. Toxicol Mech Methods. 2017 Sep;27(7):537-543. doi: 10.1080/15376516.2017.1333554. Epub 2017 Jun 8.
• [100] Unique signatures of stress-induced senescent human astrocytes. Exp Neurol. 2020 Dec;334:113466. doi: 10.1016/j.expneurol.2020.113466. Epub 2020 Sep 17.
• [101] NO-sulindac inhibits the hypoxia response of PC-3 prostate cancer cells via the Akt signalling pathway. Int J Cancer. 2009 Jan 1;124(1):223-32. doi: 10.1002/ijc.23934.
• [102] 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.
• [103] Chronic ethanol exposure increases goosecoid (GSC) expression in human embryonic carcinoma cell differentiation. J Appl Toxicol. 2014 Jan;34(1):66-75.
• [104] 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.
• [105] 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.
• [106] Transcriptomics hit the target: monitoring of ligand-activated and stress response pathways for chemical testing. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):7-18.
• [107] Dasatinib reverses cancer-associated fibroblasts (CAFs) from primary lung carcinomas to a phenotype comparable to that of normal fibroblasts. Mol Cancer. 2010 Jun 27;9:168.
• [108] 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.
• [109] The effects of a novel synthetic retinoid, seletinoid G, on the expression of extracellular matrix proteins in aged human skin in vivo. Clin Chim Acta. 2005 Dec;362(1-2):161-9. doi: 10.1016/j.cccn.2005.06.016. Epub 2005 Aug 1.
• [110] Effects of ciglitazone and troglitazone on the proliferation of human stomach cancer cells. World J Gastroenterol. 2009 Jan 21;15(3):310-20.
• [111] Evaluation of a human iPSC-derived BBB model for repeated dose toxicity testing with cyclosporine A as model compound. Toxicol In Vitro. 2021 Jun;73:105112. doi: 10.1016/j.tiv.2021.105112. Epub 2021 Feb 22.
• [112] 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.
• [113] Identification of selective inhibitors of cancer stem cells by high-throughput screening. Cell. 2009 Aug 21;138(4):645-659. doi: 10.1016/j.cell.2009.06.034. Epub 2009 Aug 13.
• [114] Cannabidiol-induced transcriptomic changes and cellular senescence in human Sertoli cells. Toxicol Sci. 2023 Feb 17;191(2):227-238. doi: 10.1093/toxsci/kfac131.
• [115] 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.
• [116] Methotrexate modulates folate phenotype and inflammatory profile in EA.hy 926 cells. Eur J Pharmacol. 2014 Jun 5;732:60-7.
• [117] Effect of retinoic acid on gene expression in human conjunctival epithelium: secretory phospholipase A2 mediates retinoic acid induction of MUC16. Invest Ophthalmol Vis Sci. 2005 Nov;46(11):4050-61.
• [118] PLK1 targets NOTCH1 during DNA damage and mitotic progression. J Biol Chem. 2019 Nov 22;294(47):17941-17950. doi: 10.1074/jbc.RA119.009881. Epub 2019 Oct 9.
• [119] Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
• [120] Editor's Highlight: Modeling Compound-Induced Fibrogenesis In Vitro Using Three-Dimensional Bioprinted Human Liver Tissues. Toxicol Sci. 2016 Dec;154(2):354-367. doi: 10.1093/toxsci/kfw169. Epub 2016 Sep 7.
• [121] Quercetin suppresses pancreatic ductal adenocarcinoma progression via inhibition of SHH and TGF-/Smad signaling pathways. Cell Biol Toxicol. 2021 Jun;37(3):479-496. doi: 10.1007/s10565-020-09562-0. Epub 2020 Oct 17.
• [122] 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.
• [123] Comparison of the antifibrotic effects of the pan-histone deacetylase-inhibitor panobinostat versus the IPF-drug pirfenidone in fibroblasts from patients with idiopathic pulmonary fibrosis. PLoS One. 2018 Nov 27;13(11):e0207915. doi: 10.1371/journal.pone.0207915. eCollection 2018.
• [124] Arsenic trioxide inhibits the differentiation of fibroblasts to myofibroblasts through nuclear factor erythroid 2-like 2 (NFE2L2) protein and the Smad2/3 pathway. J Cell Physiol. 2019 Mar;234(3):2606-2617. doi: 10.1002/jcp.27073. Epub 2018 Oct 14.
• [125] Targeting the myofibroblast genetic switch: inhibitors of myocardin-related transcription factor/serum response factor-regulated gene transcription prevent fibrosis in a murine model of skin injury. J Pharmacol Exp Ther. 2014 Jun;349(3):480-6. doi: 10.1124/jpet.114.213520. Epub 2014 Apr 4.
• [126] THC exposure of human iPSC neurons impacts genes associated with neuropsychiatric disorders. Transl Psychiatry. 2018 Apr 25;8(1):89. doi: 10.1038/s41398-018-0137-3.
• [127] 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.
• [128] 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.
• [129] Gene expression signatures after ethanol exposure in differentiating embryoid bodies. Toxicol In Vitro. 2018 Feb;46:66-76.
• [130] Long-term estrogen exposure promotes carcinogen bioactivation, induces persistent changes in gene expression, and enhances the tumorigenicity of MCF-7 human breast cancer cells. Toxicol Appl Pharmacol. 2009 Nov 1;240(3):355-66.
• [131] Gene expression profile induced by BCNU in human glioma cell lines with differential MGMT expression. J Neurooncol. 2005 Jul;73(3):189-98.
• [132] 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.
• [133] Quercetin potentiates apoptosis by inhibiting nuclear factor-kappaB signaling in H460 lung cancer cells. Biol Pharm Bull. 2013;36(6):944-51. doi: 10.1248/bpb.b12-01004.
• [134] Repurposing L-menthol for systems medicine and cancer therapeutics? L-menthol induces apoptosis through caspase 10 and by suppressing HSP90. OMICS. 2016 Jan;20(1):53-64.
• [135] Involvement of Asp-Glu-Val-Asp-directed, caspase-mediated mitogen-activated protein kinase kinase 1 Cleavage, c-Jun N-terminal kinase activation, and subsequent Bcl-2 phosphorylation for paclitaxel-induced apoptosis in HL-60 cells. Mol Pharmacol. 2001 Feb;59(2):254-62. doi: 10.1124/mol.59.2.254.
• [136] Arsenic and the epigenome: interindividual differences in arsenic metabolism related to distinct patterns of DNA methylation. J Biochem Mol Toxicol. 2013 Feb;27(2):106-15. doi: 10.1002/jbt.21462. Epub 2013 Jan 11.
• [137] Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. J Med Chem. 2011 Oct 13;54(19):6905-18.
• [138] Synergistic effects of arsenic trioxide and silibinin on apoptosis and invasion in human glioblastoma U87MG cell line. Neurochem Res. 2012 Feb;37(2):370-80. doi: 10.1007/s11064-011-0620-1. Epub 2011 Oct 4.
• [139] A phase II trial with pharmacodynamic endpoints of the proteasome inhibitor bortezomib in patients with metastatic colorectal cancer. Clin Cancer Res. 2005 Aug 1;11(15):5526-33. doi: 10.1158/1078-0432.CCR-05-0081.
• [140] Systems analysis of transcriptome and proteome in retinoic acid/arsenic trioxide-induced cell differentiation/apoptosis of promyelocytic leukemia. Proc Natl Acad Sci U S A. 2005 May 24;102(21):7653-8.
• [141] Motexafin gadolinium and zinc induce oxidative stress responses and apoptosis in B-cell lymphoma lines. Cancer Res. 2005 Dec 15;65(24):11676-88.
• [142] Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
• [143] Arsenic trioxide induces apoptosis in NB-4, an acute promyelocytic leukemia cell line, through up-regulation of p73 via suppression of nuclear factor kappa B-mediated inhibition of p73 transcription and prevention of NF-kappaB-mediated induction of XIAP, cIAP2, BCL-XL and survivin. Med Oncol. 2010 Sep;27(3):833-42. doi: 10.1007/s12032-009-9294-9. Epub 2009 Sep 10.
• [144] In vitro effects of aldehydes present in tobacco smoke on gene expression in human lung alveolar epithelial cells. Toxicol In Vitro. 2013 Apr;27(3):1072-81.
• [145] MS4A3-HSP27 target pathway reveals potential for haematopoietic disorder treatment in alimentary toxic aleukia. Cell Biol Toxicol. 2023 Feb;39(1):201-216. doi: 10.1007/s10565-021-09639-4. Epub 2021 Sep 28.
• [146] Flavonoids-induced accumulation of hypoxia-inducible factor (HIF)-1alpha/2alpha is mediated through chelation of iron. J Cell Biochem. 2008 Apr 15;103(6):1989-98. doi: 10.1002/jcb.21588.
• [147] Ibuprofen-mediated reduction of hypoxia-inducible factors HIF-1alpha and HIF-2alpha in prostate cancer cells. Clin Cancer Res. 2003 Aug 1;9(8):3150-7.