General Information of the Drug (ID: M6APDG03389)
Name
CEP-2563
Synonyms
KT-8391; L-Lysyl-beta-alanine 9(S),12(R)-Epoxy-10(S)-methoxy-9-methyl-1-oxo-2,3,9,10,11,12-hexahydro-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-10-ylmethyl ester dihydrochloride
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Status
Discontinued in Phase 1
TTD Drug ID
D0KX1E
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.
Platelet-derived growth factor receptor alpha (PDGFRA)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Platelet-derived growth factor receptor alpha (PDGFRA) is a therapeutic target for CEP-2563. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of CEP-2563 through regulating the expression of Platelet-derived growth factor receptor alpha (PDGFRA). [1], [2]
Platelet-derived growth factor receptor beta (PDGFRB)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Platelet-derived growth factor receptor beta (PDGFRB) is a therapeutic target for CEP-2563. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of CEP-2563 through regulating the expression of Platelet-derived growth factor receptor beta (PDGFRB). [3], [4]
References
Ref 1 METTL3-mediated N (6)-methyladenosine modification governs pericyte dysfunction during diabetes-induced retinal vascular complication. Theranostics. 2022 Jan 1;12(1):277-289. doi: 10.7150/thno.63441. eCollection 2022.
Ref 2 Antitumor activity of SRI 62-834, a cyclic ether analog of ET-18-OCH3. Lipids. 1987 Nov;22(11):884-90. doi: 10.1007/BF02535549.
Ref 3 Mutant NPM1-Regulated FTO-Mediated m(6)A Demethylation Promotes Leukemic Cell Survival via PDGFRB/ERK Signaling Axis. Front Oncol. 2022 Feb 8;12:817584. doi: 10.3389/fonc.2022.817584. eCollection 2022.
Ref 4 Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36. doi: 10.1093/nar/gkr797. Epub 2011 Sep 24.