General Information of the Drug (ID: M6APDG02131)
Name
GSK525762
Synonyms
GSK-525762
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Status
Phase 1
Structure
Formula
C22H22ClN5O2
InChI
1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1
InChIKey
AAAQFGUYHFJNHI-SFHVURJKSA-N
PubChem CID
46943432
TTD Drug ID
D07OFM
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.
Bromodomain-containing protein 4 (BRD4)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Bromodomain-containing protein 4 (BRD4) is a therapeutic target for GSK525762. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of GSK525762 through regulating the expression of Bromodomain-containing protein 4 (BRD4). [1], [2]
References
Ref 1 mRNA circularization by METTL3-eIF3h enhances translation and promotes oncogenesis. Nature. 2018 Sep;561(7724):556-560. doi: 10.1038/s41586-018-0538-8. Epub 2018 Sep 19.
Ref 2 Targeting bromodomains: epigenetic readers of lysine acetylation. Nat Rev Drug Discov. 2014 May;13(5):337-56. doi: 10.1038/nrd4286. Epub 2014 Apr 22.