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

General Information of Drug (ID: DMKNCVM)

• Drug Name: Dalcetrapib Drug Info
• Synonyms: JTT 705; JTT-705; R-1658; RG-1658; RO-4607381; S-[2-[[1-(2-ethylbutyl)cyclohexanecarbonyl]amino]phenyl] 2-methylpropanethioate

Indication

Disease Entry	ICD 11	Status	REF
Acute coronary syndrome	BA41	Phase 3	[1]
Hyperlipidaemia	5C80	Phase 3	[2]

• Cross-matching ID:
  PubChem CID: 6918540
  ChEBI ID: CHEBI:95001
  CAS Number: CAS 211513-37-0
  TTD Drug ID: DMKNCVM
  INTEDE Drug ID: DR1890

Molecule-Related Drug Atlas

Drug(s) Targeting Cholesteryl ester transfer protein (CETP)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Evacetrapib	DMCDZ15	Cardiovascular disease	BA00-BE2Z	Phase 3	[6]
Anacetrapib	DMP2BFG	Arteriosclerosis	BD40	Phase 3	[7]
JTT-302	DMGLVBI	Lipid metabolism disorder	5C52.Z	Phase 2	[6]
DRL-17822	DMGD3XT	Arteriosclerosis	BD40	Phase 2	[6]
TA-8995	DMAZHT0	Cardiovascular disease	BA00-BE2Z	Phase 2	[8]
BAY-60-5521	DMXIDWE	Arteriosclerosis	BD40	Phase 1	[9]
Torcetrapib	DMDHYM7	Hyperlipidaemia	5C80	Discontinued in Phase 2	[10]
CETi-1	DMUG5OB	Arteriosclerosis	BD40	Discontinued in Phase 2	[11]
CP-800569	DMZ0YU7	Arteriosclerosis	BD40	Discontinued in Phase 1	[12]
R7232	DMETAP8	Dyslipidemia	5C80-5C81	Discontinued in Phase 1	[3]

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Doxorubicin	DMVP5YE	Acute myelogenous leukaemia	2A41	Approved	[13]
Progesterone	DMUY35B	Amenorrhea	GA20.0	Approved	[14]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[15]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[16]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[17]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[18]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[19]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[20]
Prasterone	DM67VKL	Chronic obstructive pulmonary disease	CA22	Approved	[14]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[21]

Drug(s) Affected By Glucocorticoid receptor (NR3C1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[22]
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[23]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[24]
Selenium	DM25CGV	N. A.	N. A.	Approved	[25]
Colchicine	DM2POTE	Acute gout flare	FA25.0	Approved	[26]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[27]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[28]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[29]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[30]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[31]

Drug(s) Affected By Cytochrome b-245 heavy chain (CYBB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[32]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[33]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[34]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[35]
Cisplatin	DMRHGI9	Adenocarcinoma	2D40	Approved	[36]
Triclosan	DMZUR4N	Malaria	1F40-1F45	Approved	[37]
Tamibarotene	DM3G74J	T-cell leukaemia	2A90	Phase 3	[33]
Anacetrapib	DMP2BFG	Arteriosclerosis	BD40	Phase 3	[5]
phorbol 12-myristate 13-acetate	DMJWD62	Acute myeloid leukaemia	2A60	Phase 2	[38]
Benzo(a)pyrene	DMN7J43	N. A.	N. A.	Phase 1	[39]

Drug(s) Affected By Mineralocorticoid receptor (NR3C2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Spironolactone	DM2AQ5N	Chronic heart failure	BD1Z	Approved	[40]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[41]
Triamcinolone	DM98IXF	Acute adrenal insufficiency		Approved	[42]
Aldosterone	DM9S2JW	Hypertension	BA00-BA04	Approved	[43]
Betamethasone	DMAHJEF	Acute adrenal insufficiency		Approved	[42]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[44]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[45]
Hydrocortisone	DMGEMB7	Acne vulgaris	ED80	Approved	[42]
Budesonide	DMJIBAW	Allergic rhinitis	CA08.0	Approved	[42]
Dexamethasone	DMMWZET	Acute adrenal insufficiency		Approved	[46]

Drug(s) Affected By Cytochrome P450 11B1, mitochondrial (CYP11B1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrocortisone	DMGEMB7	Acne vulgaris	ED80	Approved	[47]
FADROZOLE	DM3C5GZ	Breast cancer	2C60-2C65	Approved	[48]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[49]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[45]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[50]
Potassium Chloride	DMMTAJC	Hypokalemia	5C77	Approved	[51]
Mitotane	DMU1GX0	Adrenocortical carcinoma	2D11.Z	Approved	[52]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[53]
Anacetrapib	DMP2BFG	Arteriosclerosis	BD40	Phase 3	[5]
Benzo(a)pyrene	DMN7J43	N. A.	N. A.	Phase 1	[39]

Drug(s) Affected By Cyclic AMP-responsive element-binding protein 1 (CREB1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[54]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[55]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[56]
Selenium	DM25CGV	N. A.	N. A.	Approved	[25]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[57]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[58]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[59]
Isotretinoin	DM4QTBN	Acne vulgaris	ED80	Approved	[59]
Hydroquinone	DM6AVR4	Melasma	ED60.1	Approved	[60]
Ergotidine	DM78IME	Osteoarthritis	FA00-FA05	Approved	[61]

Drug(s) Affected By Cytochrome P450 11B2, mitochondrial (CYP11B2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aldosterone	DM9S2JW	Hypertension	BA00-BA04	Approved	[62]
FADROZOLE	DM3C5GZ	Breast cancer	2C60-2C65	Approved	[48]
Erythromycin	DM4K7GQ	Acne vulgaris	ED80	Approved	[63]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[45]
Potassium Chloride	DMMTAJC	Hypokalemia	5C77	Approved	[51]
Dutasteride	DMQ4TJK	Benign prostatic hyperplasia	GA90	Approved	[64]
Mitotane	DMU1GX0	Adrenocortical carcinoma	2D11.Z	Approved	[65]
Amoxicillin	DMUYNEI	Acute otitis media	AB00	Approved	[63]
Carbamazepine	DMZOLBI	Epilepsy	8A60-8A68	Approved	[66]
Irbesartan	DMTP1DC	Diabetic kidney disease	GB61.Z	Approved	[67]

Drug(s) Affected By Peroxisome proliferator-activated receptor gamma (PPARG)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[68]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[69]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[70]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[71]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[30]
Glucosamine	DM4ZLFD	Osteoarthritis	FA00-FA05	Approved	[72]
Isoniazid	DM5JVS3	Latent tuberculosis infection		Approved	[73]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[74]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[75]
Stavudine	DM6DEK9	Human immunodeficiency virus infection	1C62	Approved	[76]

Drug(s) Affected By Signal transducer and activator of transcription 3 (STAT3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Dexamethasone	DMMWZET	Acute adrenal insufficiency		Approved	[53]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[77]
Sertraline	DM0FB1J	Coronary heart disease	BA80.Z	Approved	[78]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[79]
Trametinib	DM2JGQ3	Melanoma	2C30	Approved	[80]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[81]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[82]
Simvastatin	DM30SGU	Arteriosclerosis	BD40	Approved	[83]
Cladribine	DM3JDRP	Hairy cell leukaemia	2A82.2	Approved	[84]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[85]

Drug(s) Affected By Nuclear receptor subfamily 4 group A member 2 (NR4A2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[86]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[87]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[88]
Hydroquinone	DM6AVR4	Melasma	ED60.1	Approved	[89]
Thalidomide	DM70BU5	Adult T-cell leukemia/lymphoma		Approved	[90]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[91]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[92]
Demecolcine	DMCZQGK	Solid tumour/cancer	2A00-2F9Z	Approved	[93]
Temozolomide	DMKECZD	Adenocarcinoma	2D40	Approved	[94]
Sodium lauryl sulfate	DMLJ634	Constipation	DD91.1	Approved	[95]

Drug(s) Affected By Steroidogenic acute regulatory protein, mitochondrial (STAR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Etretinate	DM2CZFA	Keratosis	ED56	Approved	[96]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[97]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[34]
Lamotrigine	DM8SXYG	Bipolar disorder	6A60	Approved	[98]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[99]
Lindane	DMB8CNL	Infestations of lice and scabies	1G00.Z	Approved	[100]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[66]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[101]
Hydrocortisone	DMGEMB7	Acne vulgaris	ED80	Approved	[102]
Mifepristone	DMGZQEF	Cushing disease	5A70	Approved	[103]

Drug(s) Affected By NADPH oxidase 5 (NOX5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[45]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[104]
Isoflavone	DM7U58J	N. A.	N. A.	Phase 4	[105]
Anacetrapib	DMP2BFG	Arteriosclerosis	BD40	Phase 3	[5]
Benzo(a)pyrene	DMN7J43	N. A.	N. A.	Phase 1	[106]
Torcetrapib	DMDHYM7	Hyperlipidaemia	5C80	Discontinued in Phase 2	[5]
bisphenol A	DM2ZLD7	Discovery agent	N.A.	Investigative	[107]

Drug(s) Affected By NADPH oxidase 4 (NOX4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[108]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[30]
Hydroquinone	DM6AVR4	Melasma	ED60.1	Approved	[109]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[110]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[45]
Capsaicin	DMGMF6V	Back pain	ME84.Z	Approved	[111]
Rosiglitazone	DMILWZR	Chronic kidney disease	GB61	Approved	[112]
Bosentan	DMIOGBU	Pulmonary arterial hypertension	BB01.0	Approved	[113]
Zoledronate	DMIXC7G	Adenocarcinoma	2D40	Approved	[114]
Hesperetin	DMKER83	High blood cholesterol level	5C80.00	Approved	[115]

Drug(s) Affected By NADPH oxidase 1 (NOX1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[116]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[116]
Niclosamide	DMJAGXQ	Cestodes infection	1F70-1F76	Approved	[117]
Arsenic	DMTL2Y1	N. A.	N. A.	Approved	[118]
Anacetrapib	DMP2BFG	Arteriosclerosis	BD40	Phase 3	[5]
(+)-JQ1	DM1CZSJ	Testicular cancer	2C80	Phase 1	[119]
Torcetrapib	DMDHYM7	Hyperlipidaemia	5C80	Discontinued in Phase 2	[5]
Acteoside	DM0YHKB	Nephritis	GB40	Terminated	[120]
U0126	DM31OGF	Discovery agent	N.A.	Investigative	[121]
Nickel chloride	DMI12Y8	Discovery agent	N.A.	Investigative	[122]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cholesteryl ester transfer protein (CETP)	TTFQAYR	CETP_HUMAN	Inhibitor	[3]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4) Main DME	DE4LYSA	CP3A4_HUMAN	Substrate	[4]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Cyclic AMP-responsive element-binding protein 1 (CREB1)	OT1MDLA1	CREB1_HUMAN	Post-Translational Modifications	[5]
Cytochrome b-245 heavy chain (CYBB)	OTGSG868	CY24B_HUMAN	Gene/Protein Processing	[5]
Cytochrome P450 11B1, mitochondrial (CYP11B1)	OTKKL894	C11B1_HUMAN	Gene/Protein Processing	[5]
Cytochrome P450 11B2, mitochondrial (CYP11B2)	OTIOLWYN	C11B2_HUMAN	Gene/Protein Processing	[5]
Glucocorticoid receptor (NR3C1)	OTCI2YDI	GCR_HUMAN	Gene/Protein Processing	[5]
Mineralocorticoid receptor (NR3C2)	OT0F2V2Z	MCR_HUMAN	Gene/Protein Processing	[5]
NADPH oxidase 1 (NOX1)	OTZPJQCC	NOX1_HUMAN	Gene/Protein Processing	[5]
NADPH oxidase 4 (NOX4)	OTTYQ097	NOX4_HUMAN	Gene/Protein Processing	[5]
NADPH oxidase 5 (NOX5)	OTHTH59G	NOX5_HUMAN	Gene/Protein Processing	[5]
Nuclear receptor subfamily 4 group A member 2 (NR4A2)	OT3F9IR2	NR4A2_HUMAN	Gene/Protein Processing	[5]

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] ClinicalTrials.gov (NCT00658515) A Study of RO4607381 in Stable Coronary Heart Disease Patients With Recent Acute Coronary Syndrome. U.S. National Institutes of Health.
• [3] Clinical pipeline report, company report or official report of Roche (2009).
• [4] In vitro and in vivo assessment of the effect of dalcetrapib on a panel of CYP substrates. Curr Med Res Opin. 2009 Apr;25(4):891-902.
• [5] Cholesteryl ester-transfer protein inhibitors stimulate aldosterone biosynthesis in adipocytes through Nox-dependent processes. J Pharmacol Exp Ther. 2015 Apr;353(1):27-34.
• [6] The dyslipidaemia market. Nat Rev Drug Discov. 2014 Nov;13(11):807-8.
• [7] Assessment of a pharmacokinetic and pharmacodynamic interaction between simvastatin and anacetrapib, a potent cholesteryl ester transfer protein (C... Br J Clin Pharmacol. 2009 May;67(5):520-6.
• [8] Amgen To Acquire Privately-Held Dezima Pharma
• [9] Single dose pharmacokinetics, pharmacodynamics, tolerability and safety of BAY 60-5521, a potent inhibitor of cholesteryl ester transfer protein. Br J Clin Pharmacol. 2012 Feb;73(2):210-8.
• [10] Safety and tolerability of dalcetrapib. Am J Cardiol. 2009 Jul 1;104(1):82-91.
• [11] CETi-1. AVANT. Curr Opin Investig Drugs. 2004 Mar;5(3):334-8.
• [12] Pfizer. Product Development Pipeline. March 31 2009.
• [13] Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
• [14] Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
• [15] Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
• [16] Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
• [17] 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.
• [18] Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
• [19] Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
• [20] The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
• [21] Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
• [22] Persistent and non-persistent changes in gene expression result from long-term estrogen exposure of MCF-7 breast cancer cells. J Steroid Biochem Mol Biol. 2011 Feb;123(3-5):140-50.
• [23] Arsenite and cadmium promote the development of mammary tumors. Carcinogenesis. 2020 Jul 14;41(7):1005-1014. doi: 10.1093/carcin/bgz176.
• [24] 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.
• [25] 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.
• [26] Comparative effects of microtubules disruption on glucocorticoid receptor functions in proliferating and quiescent cells. Int J Toxicol. 2010 May-Jun;29(3):326-35. doi: 10.1177/1091581810366486.
• [27] The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
• [28] 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.
• [29] Effects of ciglitazone and troglitazone on the proliferation of human stomach cancer cells. World J Gastroenterol. 2009 Jan 21;15(3):310-20.
• [30] 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.
• [31] Adipocyte differentiation, mitochondrial gene expression and fat distribution: differences between zidovudine and tenofovir after 6 months. Antivir Ther. 2009;14(8):1089-100. doi: 10.3851/IMP1457.
• [32] Dipeptidyl peptidase-4 inhibition prevents vascular aging in mice under chronic stress: Modulation of oxidative stress and inflammation. Chem Biol Interact. 2019 Dec 1;314:108842. doi: 10.1016/j.cbi.2019.108842. Epub 2019 Oct 2.
• [33] 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.
• [34] 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.
• [35] Mechanism of alcohol-induced oxidative stress and neuronal injury. Free Radic Biol Med. 2008 Dec 1;45(11):1542-50.
• [36] 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.
• [37] Transcriptome and DNA methylome dynamics during triclosan-induced cardiomyocyte differentiation toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
• [38] Dexamethasone but not indomethacin inhibits human phagocyte nicotinamide adenine dinucleotide phosphate oxidase activity by down-regulating expression of genes encoding oxidase components. J Immunol. 1998 Nov 1;161(9):4960-7.
• [39] 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.
• [40] The human mineralocorticoid receptor only partially differentiates between different ligands after expression in fission yeast. FEMS Yeast Res. 2005 Apr;5(6-7):627-33. doi: 10.1016/j.femsyr.2004.12.007.
• [41] The synthetic androgen methyltrienolone (r1881) acts as a potent antagonist of the mineralocorticoid receptor. Mol Pharmacol. 2007 Feb;71(2):473-82. doi: 10.1124/mol.106.031112. Epub 2006 Nov 14.
• [42] Transactivation via the human glucocorticoid and mineralocorticoid receptor by therapeutically used steroids in CV-1 cells: a comparison of their glucocorticoid and mineralocorticoid properties. Eur J Endocrinol. 2004 Sep;151(3):397-406. doi: 10.1530/eje.0.1510397.
• [43] Regulation of mineralocorticoid receptor expression during neuronal differentiation of murine embryonic stem cells. Endocrinology. 2010 May;151(5):2244-54. doi: 10.1210/en.2009-0753. Epub 2010 Mar 5.
• [44] 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.
• [45] 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.
• [46] Dexamethasone controls aryl hydrocarbon receptor (AhR)-mediated CYP1A1 and CYP1A2 expression and activity in primary cultures of human hepatocytes. Chem Biol Interact. 2009 May 15;179(2-3):288-96.
• [47] Steroid signalling in the ovarian surface epithelium. Trends Endocrinol Metab. 2005 Sep;16(7):327-33.
• [48] 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.
• [49] Flavonoids exhibit diverse effects on CYP11B1 expression and cortisol synthesis. Toxicol Appl Pharmacol. 2012 Feb 1;258(3):343-50.
• [50] Autophagy as a compensation mechanism participates in ethanol-induced fetal adrenal dysfunction in female rats. Toxicol Appl Pharmacol. 2018 Apr 15;345:36-47.
• [51] Blockade of T-type voltage-dependent Ca2+ channels by benidipine, a dihydropyridine calcium channel blocker, inhibits aldosterone production in human adrenocortical cell line NCI-H295R. Eur J Pharmacol. 2008 Apr 28;584(2-3):424-34. doi: 10.1016/j.ejphar.2008.02.001. Epub 2008 Feb 12.
• [52] Biphasic hormonal responses to the adrenocorticolytic DDT metabolite 3-methylsulfonyl-DDE in human cells. Toxicol Appl Pharmacol. 2010 Feb 1;242(3):281-9.
• [53] 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.
• [54] Association between treatment-emergent suicidal ideation with citalopram and polymorphisms near cyclic adenosine monophosphate response element binding protein in the STAR*D study. Arch Gen Psychiatry. 2007 Jun;64(6):689-97. doi: 10.1001/archpsyc.64.6.689.
• [55] Cannabidiol upregulates melanogenesis through CB1 dependent pathway by activating p38 MAPK and p42/44 MAPK. Chem Biol Interact. 2017 Aug 1;273:107-114. doi: 10.1016/j.cbi.2017.06.005. Epub 2017 Jun 7.
• [56] Oxidative stress modulates theophylline effects on steroid responsiveness. Biochem Biophys Res Commun. 2008 Dec 19;377(3):797-802.
• [57] Distinct genetic profile in peripheral blood mononuclear cells of psoriatic arthritis patients treated with methotrexate and TNF-inhibitors. Clin Rheumatol. 2014 Dec;33(12):1815-21. doi: 10.1007/s10067-014-2807-8. Epub 2014 Oct 24.
• [58] Peroxisome proliferator-activated receptor-gamma ligands suppress fibronectin gene expression in human lung carcinoma cells: involvement of both CRE and Sp1. Am J Physiol Lung Cell Mol Physiol. 2005 Sep;289(3):L419-28. doi: 10.1152/ajplung.00002.2005. Epub 2005 May 20.
• [59] Nonclassical action of retinoic acid on the activation of the cAMP response element-binding protein in normal human bronchial epithelial cells. Mol Biol Cell. 2006 Feb;17(2):566-75. doi: 10.1091/mbc.e05-06-0519. Epub 2005 Nov 9.
• [60] p38 MAPK/PP2Ac/TTP pathway on the connection of TNF- and caspases activation on hydroquinone-induced apoptosis. Carcinogenesis. 2013 Apr;34(4):818-27. doi: 10.1093/carcin/bgs409. Epub 2013 Jan 3.
• [61] Glycyrrhizin attenuates histamine-mediated MUC5AC upregulation, inflammatory cytokine production, and aquaporin 5 downregulation through suppressing the NF-B pathway in human nasal epithelial cells. Chem Biol Interact. 2018 Apr 1;285:21-26. doi: 10.1016/j.cbi.2018.02.010. Epub 2018 Feb 13.
• [62] [Association study between a polymorphism of aldosterone synthetase gene and the pathogenesis of polycystic ovary syndrome]. Zhonghua Fu Chan Ke Za Zhi. 2003 Feb;38(2):94-7.
• [63] Modulation of steroidogenic gene expression and hormone production of H295R cells by pharmaceuticals and other environmentally active compounds. Toxicol Appl Pharmacol. 2007 Dec 1;225(2):142-53.
• [64] Effects of dutasteride on the expression of genes related to androgen metabolism and related pathway in human prostate cancer cell lines. Invest New Drugs. 2007 Oct;25(5):491-7.
• [65] Mitotane alters mitochondrial respiratory chain activity by inducing cytochrome c oxidase defect in human adrenocortical cells. Endocr Relat Cancer. 2013 May 21;20(3):371-81.
• [66] Differential effects of antiepileptic drugs on steroidogenesis in a human in vitro cell model. Acta Neurol Scand Suppl. 2009;(189):14-21.
• [67] Aldosterone synthase (CYP11B2) -344 C/T polymorphism is related to antihypertensive response: result from the Swedish Irbesartan Left Ventricular Hypertrophy Investigation versus Atenolol (SILVHIA) trial. Am J Hypertens. 2002 May;15(5):389-93. doi: 10.1016/s0895-7061(02)02256-2.
• [68] COX-2 and PPAR-gama confer cannabidiol-induced apoptosis of human lung cancer cells. Mol Cancer Ther. 2013 Jan;12(1):69-82.
• [69] 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.
• [70] The effect of quercetin and kaempferol aglycones and glucuronides on peroxisome proliferator-activated receptor-gamma (PPAR-). Food Funct. 2015 Apr;6(4):1098-107. doi: 10.1039/c5fo00076a.
• [71] Induction of solid tumor differentiation by the peroxisome proliferator-activated receptor-gamma ligand troglitazone in patients with liposarcoma. Proc Natl Acad Sci U S A. 1999 Mar 30;96(7):3951-6. doi: 10.1073/pnas.96.7.3951.
• [72] Glucosamine sulfate reduces prostaglandin E(2) production in osteoarthritic chondrocytes through inhibition of microsomal PGE synthase-1. J Rheumatol. 2012 Mar;39(3):635-44. doi: 10.3899/jrheum.110621. Epub 2011 Nov 15.
• [73] Isoniazid suppresses antioxidant response element activities and impairs adipogenesis in mouse and human preadipocytes. Toxicol Appl Pharmacol. 2013 Dec 15;273(3):435-41. doi: 10.1016/j.taap.2013.10.005. Epub 2013 Oct 12.
• [74] Regulatory role of KEAP1 and NRF2 in PPAR expression and chemoresistance in human non-small-cell lung carcinoma cells. Free Radic Biol Med. 2012 Aug 15;53(4):758-68. doi: 10.1016/j.freeradbiomed.2012.05.041. Epub 2012 Jun 7.
• [75] Aspirin inhibits MMP-9 mRNA expression and release via the PPARalpha/gamma and COX-2/mPGES-1-mediated pathways in macrophages derived from THP-1 cells. Biomed Pharmacother. 2010 Feb;64(2):118-23. doi: 10.1016/j.biopha.2009.04.033. Epub 2009 Oct 17.
• [76] Mitochondrial proliferation, DNA depletion and adipocyte differentiation in subcutaneous adipose tissue of HIV-positive HAART recipients. Antivir Ther. 2003 Aug;8(4):323-31.
• [77] 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.
• [78] Immunomodulatory effect of selective serotonin reuptake inhibitors (SSRIs) on human T lymphocyte function and gene expression. Eur Neuropsychopharmacol. 2007 Dec;17(12):774-80.
• [79] Diesel exhaust particulate-induced activation of Stat3 requires activities of EGFR and Src in airway epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2007 Feb;292(2):L422-9. doi: 10.1152/ajplung.00204.2006. Epub 2006 Oct 6.
• [80] Physapubescin B enhances the sensitivity of gastric cancer cells to trametinib by inhibiting the STAT3 signaling pathway. Toxicol Appl Pharmacol. 2020 Dec 1;408:115273. doi: 10.1016/j.taap.2020.115273. Epub 2020 Oct 6.
• [81] Sulindac induces apoptosis and inhibits tumor growth in vivo in head and neck squamous cell carcinoma. Neoplasia. 2007 Mar;9(3):192-9. doi: 10.1593/neo.06781.
• [82] Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
• [83] Simvastatin acts as an inhibitor of interferon gamma-induced cycloxygenase-2 expression in human THP-1 cells, but not in murine RAW264.7 cells. Biocell. 2009 Aug;33(2):107-14.
• [84] Therapeutic potential of cladribine in combination with STAT3 inhibitor against multiple myeloma. BMC Cancer. 2011 Jun 16;11:255. doi: 10.1186/1471-2407-11-255.
• [85] Quercetin exerts anti-melanoma activities and inhibits STAT3 signaling. Biochem Pharmacol. 2014 Feb 1;87(3):424-34. doi: 10.1016/j.bcp.2013.11.008. Epub 2013 Nov 23.
• [86] Identification of NR4A2 as a transcriptional activator of IL-8 expression in human inflammatory arthritis. Mol Immunol. 2009 Oct;46(16):3345-57. doi: 10.1016/j.molimm.2009.07.019. Epub 2009 Sep 3.
• [87] Neuronal and cardiac toxicity of pharmacological compounds identified through transcriptomic analysis of human pluripotent stem cell-derived embryoid bodies. Toxicol Appl Pharmacol. 2021 Dec 15;433:115792. doi: 10.1016/j.taap.2021.115792. Epub 2021 Nov 3.
• [88] Identification of transcriptome signatures and biomarkers specific for potential developmental toxicants inhibiting human neural crest cell migration. Arch Toxicol. 2016 Jan;90(1):159-80.
• [89] 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.
• [90] Polyunsaturated fatty acids synergize with lipid droplet binding thalidomide analogs to induce oxidative stress in cancer cells. Lipids Health Dis. 2010 Jun 2;9:56. doi: 10.1186/1476-511X-9-56.
• [91] 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.
• [92] 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.
• [93] Characterization of formaldehyde's genotoxic mode of action by gene expression analysis in TK6 cells. Arch Toxicol. 2013 Nov;87(11):1999-2012.
• [94] 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.
• [95] Identification of cornifelin and early growth response-1 gene as novel biomarkers for in vitro eye irritation using a 3D reconstructed human cornea model MCTT HCE?. Arch Toxicol. 2015 Sep;89(9):1589-98. doi: 10.1007/s00204-014-1390-8. Epub 2014 Nov 7.
• [96] Retinoids and retinol differentially regulate steroid biosynthesis in ovarian theca cells isolated from normal cycling women and women with polycystic ovary syndrome. J Clin Endocrinol Metab. 2005 Aug;90(8):4858-65. doi: 10.1210/jc.2005-0330. Epub 2005 May 24.
• [97] 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.
• [98] 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.
• [99] Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
• [100] Steroidogenic gene expression in H295R cells and the human adrenal gland: adrenotoxic effects of lindane in vitro. J Appl Toxicol. 2006 Nov-Dec;26(6):484-92.
• [101] Chronic ethanol exposure increases goosecoid (GSC) expression in human embryonic carcinoma cell differentiation. J Appl Toxicol. 2014 Jan;34(1):66-75.
• [102] Glucocorticoid-activation system mediated glucocorticoid-insulin-like growth factor 1 (GC-IGF1) axis programming alteration of adrenal dysfunction induced by prenatal caffeine exposure. Toxicol Lett. 2019 Mar 1;302:7-17.
• [103] Mifepristone induced progesterone withdrawal reveals novel regulatory pathways in human endometrium. Mol Hum Reprod. 2007 Sep;13(9):641-54.
• [104] Molecular mechanism of action of bisphenol and bisphenol A mediated by oestrogen receptor alpha in growth and apoptosis of breast cancer cells. Br J Pharmacol. 2013 May;169(1):167-78.
• [105] Soy isoflavones alter expression of genes associated with cancer progression, including interleukin-8, in androgen-independent PC-3 human prostate cancer cells. J Nutr. 2006 Jan;136(1):75-82.
• [106] Effect of aflatoxin B(1), benzo[a]pyrene, and methapyrilene on transcriptomic and epigenetic alterations in human liver HepaRG cells. Food Chem Toxicol. 2018 Nov;121:214-223. doi: 10.1016/j.fct.2018.08.034. Epub 2018 Aug 26.
• [107] Comparison of transcriptome expression alterations by chronic exposure to low-dose bisphenol A in different subtypes of breast cancer cells. Toxicol Appl Pharmacol. 2019 Dec 15;385:114814. doi: 10.1016/j.taap.2019.114814. Epub 2019 Nov 9.
• [108] Rhizoma Dioscoreae Nipponicae polysaccharides protect HUVECs from H2O2-induced injury by regulating PPAR factor and the NADPH oxidase/ROS-NF-B signal pathway. Toxicol Lett. 2015 Jan 5;232(1):149-58. doi: 10.1016/j.toxlet.2014.10.006. Epub 2014 Oct 8.
• [109] Effects of SIDT2 on the miR-25/NOX4/HuR axis and SIRT3 mRNA stability lead to ROS-mediated TNF- expression in hydroquinone-treated leukemia cells. Cell Biol Toxicol. 2023 Oct;39(5):2207-2225. doi: 10.1007/s10565-022-09705-5. Epub 2022 Mar 18.
• [110] Role of calcitriol and cortisol on human adipocyte proliferation and oxidative and inflammatory stress: a microarray study. J Nutrigenet Nutrigenomics. 2008;1(1-2):30-48. doi: 10.1159/000109873. Epub 2007 Oct 16.
• [111] Capsaicin inhibits cell proliferation by enhancing oxidative stress and apoptosis through SIRT1/NOX4 signaling pathways in HepG2 and HL-7702 cells. J Biochem Mol Toxicol. 2022 Mar;36(3):e22974. doi: 10.1002/jbt.22974. Epub 2021 Dec 23.
• [112] Transcriptomic analysis of untreated and drug-treated differentiated HepaRG cells over a 2-week period. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):27-35.
• [113] Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
• [114] Zoledronate dysregulates fatty acid metabolism in renal tubular epithelial cells to induce nephrotoxicity. Arch Toxicol. 2018 Jan;92(1):469-485.
• [115] Hesperetin relieves cisplatin-induced acute kidney injury by mitigating oxidative stress, inflammation and apoptosis. Chem Biol Interact. 2019 Aug 1;308:269-278.
• [116] Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
• [117] 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.
• [118] Arsenic and chromium in drinking water promote tumorigenesis in a mouse colitis-associated colorectal cancer model and the potential mechanism is ROS-mediated Wnt/-catenin signaling pathway. Toxicol Appl Pharmacol. 2012 Jul 1;262(1):11-21. doi: 10.1016/j.taap.2012.04.014. Epub 2012 Apr 19.
• [119] CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer. J Clin Invest. 2016 Feb;126(2):639-52.
• [120] The inhibitory effect of phenylpropanoid glycosides and iridoid glucosides on free radical production and beta2 integrin expression in human leucocytes. J Pharm Pharmacol. 2006 Jan;58(1):129-35. doi: 10.1211/jpp.58.1.0016.
• [121] Intervention of human breast cell carcinogenesis chronically induced by 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine. Carcinogenesis. 2012 Apr;33(4):876-85. doi: 10.1093/carcin/bgs097. Epub 2012 Feb 3.
• [122] Nickel-induced epithelial-mesenchymal transition by reactive oxygen species generation and E-cadherin promoter hypermethylation. J Biol Chem. 2012 Jul 20;287(30):25292-302.