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

General Information of Drug (ID: DMEAIQC)

• Drug Name: GW2433 Drug Info
• Synonyms: GW 2433; GW-2433

Indication

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

• Cross-matching ID:
  PubChem CID: 1517
  TTD Drug ID: DMEAIQC

Molecule-Related Drug Atlas

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	[4]
MBX-8025	DMNTCV4	Obesity	5B81	Phase 2/3	[5]
T3D-959	DMR3245	Alzheimer disease	8A20	Phase 2	[6]
T3D-959	DMR3245	Alzheimer disease	8A20	Phase 2	[7]
KD3010	DMNFDYE	Metabolic disorder	5C50-5D2Z	Phase 1	[8]
SAR351034	DM15PG9	Dyslipidemia	5C80-5C81	Phase 1	[9]
CER-002	DMLBKZV	Dyslipidemia	5C80-5C81	Phase 1	[10]
PMID25416646-Compound-Figure5-C	DM17FKL	N. A.	N. A.	Patented	[11]
GW-501516	DMPL2KM	Type-1 diabetes	5A10	Discontinued in Phase 4	[12]
Sodelglitazar	DMJ816F	Hyperlipidaemia	5C80	Discontinued in Phase 2	[13]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[14]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[15]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[16]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[17]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[18]
Hydroquinone	DM6AVR4	Melasma	ED60.1	Approved	[19]
Marinol	DM70IK5	Anorexia nervosa cachexia	6B80	Approved	[20]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[21]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[22]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[23]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

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

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Peroxisome proliferator-activated receptor delta (PPARD)	OTI4WTOP	PPARD_HUMAN	Protein Interaction/Cellular Processes	[3]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2716).
• [2] Identification of peroxisome proliferator-activated receptor ligands from a biased chemical library. Chem Biol. 1997 Dec;4(12):909-18.
• [3] A widely used retinoic acid receptor antagonist induces peroxisome proliferator-activated receptor-gamma activity. Mol Pharmacol. 2007 May;71(5):1251-7. doi: 10.1124/mol.106.033662. Epub 2007 Feb 8.
• [4] Dual peroxisome proliferator-activated receptor / agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects.Diabetes Care.2013 Oct;36(10):2923-30.
• [5] ClinicalTrials.gov (NCT00701883) Safety and Benefit of MBX-8025 With and Without Commonly Used Statins in Moderately Overweight Patients With High Cholesterol. U. S. National Institute of Health. 2008.
• [6] Phrma report (2013 Alzheimers disease)
• [7] T3D-959: A Multi-Faceted Disease Remedial Drug Candidate for the Treatment of Alzheimer's Disease. J Alzheimers Dis. 2016;51(1):123-38.
• [8] Kalypsys nearing completion of phase Ia study of KD3010 for metabolic disorders. Kalypsys. 2007.
• [9] Addressing Unmet Medical Needs in Type 2 Diabetes: A Narrative Review of Drugs under Development. Curr Diabetes Rev. 2015 March; 11(1): 17-31.
• [10] Fibrates, glitazones, and peroxisome proliferator-activated receptors. Arterioscler Thromb Vasc Biol. 2010 May; 30(5): 894-899.
• [11] PPAR ligands and their therapeutic applications: a patent review (2008 - 2014).Expert Opin Ther Pat. 2015 Feb;25(2):175-91.
• [12] Lipid effects of peroxisome proliferator-activated receptor- agonist GW501516 in subjects with low high-density lipoprotein cholesterol: characteristics of metabolic syndrome.Arterioscler Thromb Vasc Biol.2012 Sep;32(9):2289-94.
• [13] Docking and molecular dynamics simulations of peroxisome proliferator activated receptors interacting with pan agonist sodelglitazar. Protein Pept Lett. 2011 Oct;18(10):1021-7.
• [14] Cannabidiol induces antioxidant pathways in keratinocytes by targeting BACH1. Redox Biol. 2020 Jan;28:101321. doi: 10.1016/j.redox.2019.101321. Epub 2019 Sep 5.
• [15] Functional characterization of peroxisome proliferator-activated receptor-/ expression in colon cancer. Mol Carcinog. 2011 Nov;50(11):884-900. doi: 10.1002/mc.20757. Epub 2011 Mar 11.
• [16] The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
• [17] Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
• [18] Aspirin-induced apoptosis in jurkat cells is not mediated by peroxisome proliferator-activated receptor delta. Mol Cell Biochem. 2004 Nov;266(1-2):57-63. doi: 10.1023/b:mcbi.0000049138.67699.7b.
• [19] 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.
• [20] (9)-Tetrahydrocannabinol upregulates fatty acid 2-hydroxylase (FA2H) via PPAR induction: A possible evidence for the cancellation of PPAR/-mediated inhibition of PPAR in MDA-MB-231?cells. Arch Biochem Biophys. 2019 Feb 15;662:219-225. doi: 10.1016/j.abb.2018.12.011. Epub 2018 Dec 13.
• [21] 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.
• [22] 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.
• [23] Integrated 'omics analysis reveals new drug-induced mitochondrial perturbations in human hepatocytes. Toxicol Lett. 2018 Jun 1;289:1-13.