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

General Information of Drug (ID: DMPL2KM)

Drug Name
GW-501516 Drug Info
Synonyms
317318-70-0; GW501516; GW 501516; Endurobol; GW-501516; GSK-516; UNII-7I2HA1NU22; GW1516; GW 1516; 2-(2-Methyl-4-(((4-methyl-2-(4-(trifluoromethyl)phenyl)thiazol-5-yl)methyl)thio)phenoxy)acetic acid; GW-516; GW-1516; CHEMBL38943; 2-(2-methyl-4-((4-methyl-2-(4-(trifluoromethyl)phenyl)thiazol-5-yl)methylthio)phenoxy)acetic acid; 2-(4-((2-(4-(Trifluoromethyl)phenyl)-4-methylthiazol-5-yl)methylthio)-2-methylphenoxy)acetic acid; 7I2HA1NU22
Indication
Disease Entry ICD 11 Status REF
Type-1 diabetes 5A10 Discontinued in Phase 4 [1]
Cross-matching ID
PubChem CID
9803963
ChEBI ID
CHEBI:73726
CAS Number
CAS 317318-70-0
TTD Drug ID
DMPL2KM

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Patented Agent(s)
Discontinued Drug(s)
Approved Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Peroxisome proliferator-activated receptor delta (PPARD)
Drug Name Drug ID Indication ICD 11 Highest Status REF
GFT-505 DM7ZOAE Non-alcoholic steatohepatitis DB92.1 Phase 3 [8]
MBX-8025 DMNTCV4 Obesity 5B81 Phase 2/3 [9]
T3D-959 DMR3245 Alzheimer disease 8A20 Phase 2 [10]
T3D-959 DMR3245 Alzheimer disease 8A20 Phase 2 [11]
KD3010 DMNFDYE Metabolic disorder 5C50-5D2Z Phase 1 [12]
SAR351034 DM15PG9 Dyslipidemia 5C80-5C81 Phase 1 [13]
CER-002 DMLBKZV Dyslipidemia 5C80-5C81 Phase 1 [14]
PMID25416646-Compound-Figure5-C DM17FKL N. A. N. A. Patented [15]
Sodelglitazar DMJ816F Hyperlipidaemia 5C80 Discontinued in Phase 2 [16]
Indeglitazar DMS56UD Type-2 diabetes 5A11 Discontinued in Phase 2 [17]
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Drug(s) Affected By Phospholipid-transporting ATPase ABCA1 (ABCA1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [18]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [19]
Quercetin DM3NC4M Obesity 5B81 Approved [20]
Fluoxetine DM3PD2C Bipolar depression Approved [21]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [22]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [23]
Omeprazole DM471KJ Cystic fibrosis CA25 Approved [24]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [25]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [26]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [27]
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Drug(s) Affected By Prostaglandin G/H synthase 2 (PTGS2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Eicosapentaenoic acid/docosa-hexaenoic acid DMMUCG4 Hypertriglyceridemia 5C80.1 Approved [28]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [29]
Gamolenic acid DMQN30Z Allergy 4A80-4A85 Approved [30]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [31]
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [32]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [33]
Ibandronate DM0QZBN Hypercalcaemia 5B91.0 Approved [34]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [35]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [36]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [37]
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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 [31]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [38]
Quercetin DM3NC4M Obesity 5B81 Approved [39]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [40]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [41]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [42]
Isoniazid DM5JVS3 Latent tuberculosis infection Approved [43]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [44]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [45]
Stavudine DM6DEK9 Human immunodeficiency virus infection 1C62 Approved [46]
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Drug(s) Affected By CX3C chemokine receptor 1 (CX3CR1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [47]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [48]
Lindane DMB8CNL Infestations of lice and scabies 1G00.Z Approved [49]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [50]
Rosiglitazone DMILWZR Chronic kidney disease GB61 Approved [4]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [51]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [52]
Phenobarbital DMXZOCG Cluster headache 8A81.0 Approved [53]
SNDX-275 DMH7W9X Breast cancer 2C60-2C65 Phase 3 [54]
Benzo(a)pyrene DMN7J43 N. A. N. A. Phase 1 [55]
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Drug(s) Affected By Oxysterols receptor LXR-beta (NR1H2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tretinoin DM49DUI Acne vulgaris ED80 Approved [48]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [56]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [57]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [50]
Gemfibrozil DMD8Q3J Hyperlipidaemia 5C80 Approved [5]
Fenofibrate DMFKXDY Coronary atherosclerosis Approved [5]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [58]
Temozolomide DMKECZD Adenocarcinoma 2D40 Approved [59]
Pioglitazone DMKJ485 Amyotrophic lateral sclerosis 8B60.0 Approved [5]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [60]
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Drug(s) Affected By Peroxisome proliferator-activated receptor alpha (PPARA)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [61]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [62]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [41]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [63]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [45]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [64]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [65]
Testosterone DM7HUNW Hot flushes GA30 Approved [66]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [67]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [68]
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Drug(s) Affected By Oxysterols receptor LXR-alpha (NR1H3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tretinoin DM49DUI Acne vulgaris ED80 Approved [69]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [68]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [70]
Gemfibrozil DMD8Q3J Hyperlipidaemia 5C80 Approved [5]
Ethanol DMDRQZU Chronic pain MG30 Approved [71]
Fenofibrate DMFKXDY Coronary atherosclerosis Approved [5]
Rosiglitazone DMILWZR Chronic kidney disease GB61 Approved [72]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [58]
Temozolomide DMKECZD Adenocarcinoma 2D40 Approved [59]
Pioglitazone DMKJ485 Amyotrophic lateral sclerosis 8B60.0 Approved [73]
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Drug(s) Affected By kinase isozyme 4, mitochondrial (PDK4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Quercetin DM3NC4M Obesity 5B81 Approved [74]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [75]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [76]
Liothyronine DM6IR3P Congenital hypothyroidism Approved [77]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [78]
Clodronate DM9Y6X7 Hypercalcaemia 5B91.0 Approved [78]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [78]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [68]
Testosterone enanthate DMB6871 N. A. N. A. Approved [79]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [80]
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Drug(s) Affected By Perilipin-2 (PLIN2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Methotrexate DM2TEOL Anterior urethra cancer Approved [81]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [82]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [69]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [83]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [84]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [78]
Leflunomide DMR8ONJ Arthritis FA20 Approved [85]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [86]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [70]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [87]
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Drug(s) Affected By Angiopoietin-related protein 4 (ANGPTL4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aspirin DM672AH Acute coronary syndrome BA41 Approved [88]
Quercetin DM3NC4M Obesity 5B81 Approved [20]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [89]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [90]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [78]
Leflunomide DMR8ONJ Arthritis FA20 Approved [85]
Clodronate DM9Y6X7 Hypercalcaemia 5B91.0 Approved [78]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [78]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [91]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [70]
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Drug(s) Affected By Peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PPARGC1A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Quercetin DM3NC4M Obesity 5B81 Approved [20]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [92]
Fructose DM43AN2 Vomiting MD90 Approved [93]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [94]
Isoniazid DM5JVS3 Latent tuberculosis infection Approved [95]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [84]
Ketotifen DM74XKS Allergic conjunctivitis 9A60.02 Approved [96]
Riboflavin DM8YMWE Acne vulgaris ED80 Approved [7]
Leflunomide DMR8ONJ Arthritis FA20 Approved [85]
Glutathione DMAHMT9 Human immunodeficiency virus infection 1C62 Approved [7]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Peroxisome proliferator-activated receptor delta (PPARD) TT2JWF6 PPARD_HUMAN Modulator [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Angiopoietin-related protein 4 (ANGPTL4) OTQL5SPX ANGL4_HUMAN Gene/Protein Processing [3]
CX3C chemokine receptor 1 (CX3CR1) OTIM9XT8 CX3C1_HUMAN Gene/Protein Processing [4]
kinase isozyme 4, mitochondrial (PDK4) OTCMHMBZ PDK4_HUMAN Gene/Protein Processing [3]
Oxysterols receptor LXR-alpha (NR1H3) OT54YZ9I NR1H3_HUMAN Gene/Protein Processing [5]
Oxysterols receptor LXR-beta (NR1H2) OT4APA60 NR1H2_HUMAN Gene/Protein Processing [5]
Perilipin-2 (PLIN2) OTRXJ9UN PLIN2_HUMAN Gene/Protein Processing [6]
Peroxisome proliferator-activated receptor alpha (PPARA) OTK095PP PPARA_HUMAN Gene/Protein Processing [5]
Peroxisome proliferator-activated receptor gamma (PPARG) OTHMARHO PPARG_HUMAN Gene/Protein Processing [5]
Peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PPARGC1A) OTHCDQ22 PRGC1_HUMAN Gene/Protein Processing [7]
Phospholipid-transporting ATPase ABCA1 (ABCA1) OT94G6BQ ABCA1_HUMAN Gene/Protein Processing [5]

References

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18 Atheroprotective effects of methotrexate on reverse cholesterol transport proteins and foam cell transformation in human THP-1 monocyte/macrophages. Arthritis Rheum. 2008 Dec;58(12):3675-83.
19 Combining simvastatin with the farnesyltransferase inhibitor tipifarnib results in an enhanced cytotoxic effect in a subset of primary CD34+ acute myeloid leukemia samples. Clin Cancer Res. 2009 May 1;15(9):3076-83. doi: 10.1158/1078-0432.CCR-08-3004. Epub 2009 Apr 21.
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21 Screening autism-associated environmental factors in differentiating human neural progenitors with fractional factorial design-based transcriptomics. Sci Rep. 2023 Jun 29;13(1):10519. doi: 10.1038/s41598-023-37488-0.
22 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
23 Differential effects of peroxisome proliferator-activated receptor activators on the mRNA levels of genes involved in lipid metabolism in primary human monocyte-derived macrophages. Metabolism. 2003 May;52(5):652-7. doi: 10.1053/meta.2003.50100.
24 Proton pump inhibitor lansoprazole is a nuclear liver X receptor agonist. Biochem Pharmacol. 2010 May 1;79(9):1310-6. doi: 10.1016/j.bcp.2009.12.018. Epub 2010 Jan 8.
25 Repression of hepatocyte nuclear factor 4 alpha by AP-1 underlies dyslipidemia associated with retinoic acid. J Lipid Res. 2019 Apr;60(4):794-804. doi: 10.1194/jlr.M088880. Epub 2019 Feb 1.
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28 Docosahexaenoic acid regulates gene expression in HUVEC cells treated with polycyclic aromatic hydrocarbons. Toxicol Lett. 2015 Jul 16;236(2):75-81.
29 Etoposide induces necrosis through p53-mediated antiapoptosis in human kidney proximal tubule cells. Toxicol Sci. 2015 Nov;148(1):204-19.
30 Conjugated linoleic acid, unlike other unsaturated fatty acids, strongly induces glutathione synthesis without any lipoperoxidation. Br J Nutr. 2006 Nov;96(5):811-9.
31 COX-2 and PPAR-gama confer cannabidiol-induced apoptosis of human lung cancer cells. Mol Cancer Ther. 2013 Jan;12(1):69-82.
32 Mitochondrial involvement in schizophrenia and other functional psychoses. Neurochem Res. 1996 Sep;21(9):995-1004.
33 Immunomodulatory effect of selective serotonin reuptake inhibitors (SSRIs) on human T lymphocyte function and gene expression. Eur Neuropsychopharmacol. 2007 Dec;17(12):774-80.
34 Stimulation of cyclooxygenase-2 expression by bone-derived transforming growth factor-beta enhances bone metastases in breast cancer. Cancer Res. 2006 Feb 15;66(4):2067-73.
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36 An in vitro coculture system of human peripheral blood mononuclear cells with hepatocellular carcinoma-derived cells for predicting drug-induced liver injury. Arch Toxicol. 2021 Jan;95(1):149-168. doi: 10.1007/s00204-020-02882-4. Epub 2020 Aug 20.
37 A2E selectively induces cox-2 in ARPE-19 and human neural cells. Curr Eye Res. 2006 Mar;31(3):259-63.
38 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.
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43 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.
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48 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.
49 Transcriptome-based functional classifiers for direct immunotoxicity. Arch Toxicol. 2014 Mar;88(3):673-89.
50 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.
51 Blood transcript immune signatures distinguish a subset of people with elevated serum ALT from others given acetaminophen. Clin Pharmacol Ther. 2016 Apr;99(4):432-41.
52 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.
53 Dose- and time-dependent effects of phenobarbital on gene expression profiling in human hepatoma HepaRG cells. Toxicol Appl Pharmacol. 2009 Feb 1;234(3):345-60.
54 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.
55 Identification of a transcriptomic signature of food-relevant genotoxins in human HepaRG hepatocarcinoma cells. Food Chem Toxicol. 2020 Jun;140:111297. doi: 10.1016/j.fct.2020.111297. Epub 2020 Mar 28.
56 Arsenic trioxide suppresses liver X receptor and enhances cholesteryl ester transfer protein expression without affecting the liver X receptor in HepG2 cells. Chem Biol Interact. 2016 Oct 25;258:288-96. doi: 10.1016/j.cbi.2016.09.009. Epub 2016 Sep 10.
57 Carotenoid transport is decreased and expression of the lipid transporters SR-BI, NPC1L1, and ABCA1 is downregulated in Caco-2 cells treated with ezetimibe. J Nutr. 2005 Oct;135(10):2305-12. doi: 10.1093/jn/135.10.2305.
58 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
59 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.
60 Regulation of Hepatic Cholesteryl Ester Transfer Protein Expression and Reverse Cholesterol Transport by Inhibition of DNA Topoisomerase II. J Biol Chem. 2015 Jun 5;290(23):14418-29. doi: 10.1074/jbc.M115.643015. Epub 2015 Apr 25.
61 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
62 The ligands/activators for peroxisome proliferator-activated receptor alpha (PPARalpha) and PPARgamma increase Cu2+,Zn2+-superoxide dismutase and decrease p22phox message expressions in primary endothelial cells. Metabolism. 2001 Jan;50(1):3-11.
63 Arsenic trioxide promotes senescence and regulates the balance of adipogenic and osteogenic differentiation in human mesenchymal stem cells. Acta Biochim Biophys Sin (Shanghai). 2011 Mar;43(3):204-9. doi: 10.1093/abbs/gmq130. Epub 2011 Jan 21.
64 Modulation of receptor phosphorylation contributes to activation of peroxisome proliferator activated receptor alpha by dehydroepiandrosterone and other peroxisome proliferators. Mol Pharmacol. 2008 Mar;73(3):968-76. doi: 10.1124/mol.107.036780. Epub 2007 Dec 13.
65 (9)-THC modulation of fatty acid 2-hydroxylase (FA2H) gene expression: possible involvement of induced levels of PPARalpha in MDA-MB-231 breast cancer cells. Toxicology. 2014 Dec 4;326:18-24.
66 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
67 Cross-talk between vitamin D receptor (VDR)- and peroxisome proliferator-activated receptor (PPAR)-signaling in melanoma cells. Anticancer Res. 2009 Sep;29(9):3647-58.
68 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.
69 Retinoic acid-induced downmodulation of telomerase activity in human cancer cells. Exp Mol Pathol. 2005 Oct;79(2):108-17.
70 Integrated 'omics analysis reveals new drug-induced mitochondrial perturbations in human hepatocytes. Toxicol Lett. 2018 Jun 1;289:1-13.
71 The potential effects of HECTD4 variants on fasting glucose and triglyceride levels in relation to prevalence of type 2 diabetes based on alcohol intake. Arch Toxicol. 2022 Sep;96(9):2487-2499. doi: 10.1007/s00204-022-03325-y. Epub 2022 Jun 17.
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