m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG02828)
Name
GSK2816126
Synonyms
GSK 126; GSK-126
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Status
Phase 1
Structure
Formula
C31H38N6O2
InChI
1S/C31H38N6O2/c1-6-22(5)37-18-20(3)29-25(30(38)34-17-26-19(2)13-21(4)35-31(26)39)14-24(15-27(29)37)23-7-8-28(33-16-23)36-11-9-32-10-12-36/h7-8,13-16,18,22,32H,6,9-12,17H2,1-5H3,(H,34,38)(H,35,39)/t22-/m0/s1
InChIKey
FKSFKBQGSFSOSM-QFIPXVFZSA-N
PubChem CID
68210102
TTD Drug ID
D05FIJ
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.
Enhancer of zeste homolog 2 (EZH2)
Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Enhancer of zeste homolog 2 (EZH2) is a therapeutic target for GSK2816126. The Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1) has potential in affecting the response of GSK2816126 through regulating the expression of Enhancer of zeste homolog 2 (EZH2). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Enhancer of zeste homolog 2 (EZH2) is a therapeutic target for GSK2816126. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of GSK2816126 through regulating the expression of Enhancer of zeste homolog 2 (EZH2). [2], [3]
References
Ref 1 IGF2BP1 Promotes Proliferation of Neuroendocrine Neoplasms by Post-Transcriptional Enhancement of EZH2. Cancers (Basel). 2022 Apr 24;14(9):2121. doi: 10.3390/cancers14092121.
Ref 2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 3 METTL3 Accelerates Breast Cancer Progression via Regulating EZH2 m(6)A Modification. J Healthc Eng. 2022 Mar 29;2022:5794422. doi: 10.1155/2022/5794422. eCollection 2022.