General Information of the Drug (ID: M6APDG00681)
Name
RGB-286147
Synonyms
pyrazolopyrimidone analog, RGB-286147
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Status
Investigative
Structure
Formula
C23H22Cl2N4O3
InChI
1S/C23H22Cl2N4O3/c1-13(2)20-19-22(29(28-20)21-16(24)4-3-5-17(21)25)26-18(27-23(19)31)12-14-6-8-15(9-7-14)32-11-10-30/h3-9,13,30H,10-12H2,1-2H3,(H,26,27,31)
InChIKey
RSQPNXBTPUXMQN-UHFFFAOYSA-N
PubChem CID
135473382
TTD Drug ID
D0J4ON
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.
Cyclin-dependent kinase 6 (CDK6)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Cyclin-dependent kinase 6 (CDK6) is a therapeutic target for RGB-286147. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of RGB-286147 through regulating the expression of Cyclin-dependent kinase 6 (CDK6). [1], [2]
Glycogen synthase kinase-3 beta (GSK-3B)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Glycogen synthase kinase-3 beta (GSK-3B) is a therapeutic target for RGB-286147. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of RGB-286147 through regulating the expression of Glycogen synthase kinase-3 beta (GSK-3B). [3], [4]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary Glycogen synthase kinase-3 beta (GSK-3B) is a therapeutic target for RGB-286147. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of RGB-286147 through regulating the expression of Glycogen synthase kinase-3 beta (GSK-3B). [4], [5]
References
Ref 1 FTO promotes tumour proliferation in bladder cancer via the FTO/miR-576/CDK6 axis in an m6A-dependent manner. Cell Death Discov. 2021 Nov 1;7(1):329. doi: 10.1038/s41420-021-00724-5.
Ref 2 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. doi: 10.1093/nar/28.1.235.
Ref 3 Vascular Smooth Muscle FTO Promotes Aortic Dissecting Aneurysms via m6A Modification of Klf5. Front Cardiovasc Med. 2020 Nov 20;7:592550. doi: 10.3389/fcvm.2020.592550. eCollection 2020.
Ref 4 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8. doi: 10.1073/pnas.0708800104. Epub 2007 Dec 11.
Ref 5 N6-methyladenosine regulated FGFR4 attenuates ferroptotic cell death in recalcitrant HER2-positive breast cancer. Nat Commun. 2022 May 13;13(1):2672. doi: 10.1038/s41467-022-30217-7.