General Information of the Drug (ID: M6APDG02301)
Name
I-BET151
Synonyms
GSK1210151A
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Status
Investigative
Structure
Formula
C23H21N5O3
InChI
1S/C23H21N5O3/c1-12-21(14(3)31-27-12)16-9-18-15(10-20(16)30-4)22-19(11-25-18)26-23(29)28(22)13(2)17-7-5-6-8-24-17/h5-11,13H,1-4H3,(H,26,29)/t13-/m1/s1
InChIKey
VUVUVNZRUGEAHB-CYBMUJFWSA-N
PubChem CID
52912189
TTD Drug ID
D0WU1S
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 I-BET151. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of I-BET151 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 Down-regulation of NF-KappaB transcriptional activity in HIV-associated kidney disease by BRD4 inhibition. J Biol Chem. 2012 Aug 17;287(34):28840-51. doi: 10.1074/jbc.M112.359505. Epub 2012 May 29.