General Information of the Drug (ID: M6APDG00512)
Name
E-3030
Synonyms
Dual PPAR alpha/gamma agonists, Eisai
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Status
Discontinued in Phase 1
Structure
3D MOL
Formula
C44H44CaCl2F2N2O10
InChI
1S/2C22H23ClFNO5.Ca/c2*1-14(2)30-21(22(26)27)9-15-4-3-5-19(8-15)28-12-18(24)13-29-20-7-6-17(23)10-16(20)11-25;/h2*3-8,10,14,18,21H,9,12-13H2,1-2H3,(H,26,27);/q;;+2/p-2/t2*18-,21-;/m00./s1
InChIKey
QBPOEQDRFVFZRI-ATAMATRTSA-L
PubChem CID
11949481
TTD Drug ID
D06PHO
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Peroxisome proliferator-activated receptor alpha (PPARA)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Peroxisome proliferator-activated receptor alpha (PPARA) is a therapeutic target for E-3030. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of E-3030 through regulating the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [1], [2]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary Peroxisome proliferator-activated receptor alpha (PPARA) is a therapeutic target for E-3030. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of E-3030 through regulating the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [2], [3]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Peroxisome proliferator-activated receptor alpha (PPARA) is a therapeutic target for E-3030. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of E-3030 through regulating the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [2], [4]
Wilms tumor 1-associating protein (WTAP)
In total 1 mechanisms lead to this potential drug response
Response Summary Peroxisome proliferator-activated receptor alpha (PPARA) is a therapeutic target for E-3030. The Wilms tumor 1-associating protein (WTAP) has potential in affecting the response of E-3030 through regulating the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [2], [3]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
Response Summary Peroxisome proliferator-activated receptor alpha (PPARA) is a therapeutic target for E-3030. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of E-3030 through regulating the expression of Peroxisome proliferator-activated receptor alpha (PPARA). [2], [4]
Peroxisome proliferator-activated receptor gamma (PPAR-gamma)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Peroxisome proliferator-activated receptor gamma (PPAR-gamma) is a therapeutic target for E-3030. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of E-3030 through regulating the expression of Peroxisome proliferator-activated receptor gamma (PPAR-gamma). [5], [6]
References
Ref 1 Resveratrol Attenuates High-Fat Diet Induced Hepatic Lipid Homeostasis Disorder and Decreases m(6)A RNA Methylation. Front Pharmacol. 2020 Dec 18;11:568006. doi: 10.3389/fphar.2020.568006. eCollection 2020.
Ref 2 Emerging drugs for non-alcoholic fatty liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):145-58. doi: 10.1517/14728214.13.1.145.
Ref 3 A METTL3-METTL14 complex mediates mammalian nuclear RNA N6-adenosine methylation. Nat Chem Biol. 2014 Feb;10(2):93-5. doi: 10.1038/nchembio.1432. Epub 2013 Dec 6.
Ref 4 Circadian Clock Regulation of Hepatic Lipid Metabolism by Modulation of m(6)A mRNA Methylation. Cell Rep. 2018 Nov 13;25(7):1816-1828.e4. doi: 10.1016/j.celrep.2018.10.068.
Ref 5 The m(6)A demethylase FTO promotes the osteogenesis of mesenchymal stem cells by downregulating PPARG. Acta Pharmacol Sin. 2022 May;43(5):1311-1323. doi: 10.1038/s41401-021-00756-8. Epub 2021 Aug 30.
Ref 6 The novel hypoglycemic agent YM440 improves hepatic insulin resistance in obese Zucker fatty rats. J Pharmacol Sci. 2006 Aug;101(4):311-7. doi: 10.1254/jphs.fp0060360. Epub 2006 Aug 5.