m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG02902)
Name
(R)-PFI-2
Synonyms
PFI-2; 1627676-59-8; (R)-PFI-2; CHEMBL3414622; PFI-2 HCl; 8-Fluoro-N-{(2r)-1-Oxo-1-(Pyrrolidin-1-Yl)-3-[3-(Trifluoromethyl)phenyl]propan-2-Yl}-1,2,3,4-Tetrahydroisoquinoline-6-Sulfonamide; 1L8; GTPL8235; C23H25F4N3O3S; MolPort-035-789-712; EX-A1603; s7294; ZINC95920703; BDBM50075073; 2648AH; AKOS030526617; CS-4177; NCGC00351479-01; HY-18627; BC600610; (R)-8-Fluoro-N-(1-oxo-1-(pyrrolidin-1-yl)-3-(3-(trifluoromethyl)phenyl)propan-2-yl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide
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Status
Preclinical
Structure
Formula
C23H25F4N3O3S
InChI
1S/C23H25F4N3O3S/c24-20-13-18(12-16-6-7-28-14-19(16)20)34(32,33)29-21(22(31)30-8-1-2-9-30)11-15-4-3-5-17(10-15)23(25,26)27/h3-5,10,12-13,21,28-29H,1-2,6-9,11,14H2/t21-/m1/s1
InChIKey
JCKGSPAAPQRPBW-OAQYLSRUSA-N
PubChem CID
71300326
TTD Drug ID
D0J6OV
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.
Histone-lysine N-methyltransferase SETD7 (SETD7)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Histone-lysine N-methyltransferase SETD7 (SETD7) is a therapeutic target for (R)-PFI-2. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of (R)-PFI-2 through regulating the expression of Histone-lysine N-methyltransferase SETD7 (SETD7). [1], [2]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Histone-lysine N-methyltransferase SETD7 (SETD7) is a therapeutic target for (R)-PFI-2. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of (R)-PFI-2 through regulating the expression of Histone-lysine N-methyltransferase SETD7 (SETD7). [1], [2]
References
Ref 1 METTL3/YTHDF2 m(6) A axis promotes tumorigenesis by degrading SETD7 and KLF4 mRNAs in bladder cancer. J Cell Mol Med. 2020 Apr;24(7):4092-4104. doi: 10.1111/jcmm.15063. Epub 2020 Mar 3.
Ref 2 Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4). J Med Chem. 2009 Oct 22;52(20):6433-46. doi: 10.1021/jm9009444.