General Information of the Drug (ID: M6APDG01595)
Name
MK-2461
Synonyms
MK 2461
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Status
Phase 1/2
Structure
Formula
C24H25N5O5S
InChI
1S/C24H25N5O5S/c1-28-13-18(12-26-28)17-9-22-23(25-11-17)6-4-16-3-5-19(10-21(16)24(22)30)27-35(31,32)29(2)14-20-15-33-7-8-34-20/h3-6,9-13,20,27H,7-8,14-15H2,1-2H3/t20-/m1/s1
InChIKey
JGEBLDKNWBUGRZ-HXUWFJFHSA-N
PubChem CID
44137946
TTD Drug ID
D00DRL
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 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 MK-2461. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of MK-2461 through regulating the expression of Platelet-derived growth factor receptor beta (PDGFRB). [1], [2]
Proto-oncogene c-Met (MET)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Proto-oncogene c-Met (MET) is a therapeutic target for MK-2461. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of MK-2461 through regulating the expression of Proto-oncogene c-Met (MET). [3], [4]
Tyrosine-protein kinase Mer (MERTK)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Tyrosine-protein kinase Mer (MERTK) is a therapeutic target for MK-2461. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of MK-2461 through regulating the expression of Tyrosine-protein kinase Mer (MERTK). [5], [6]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
Response Summary Tyrosine-protein kinase Mer (MERTK) is a therapeutic target for MK-2461. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of MK-2461 through regulating the expression of Tyrosine-protein kinase Mer (MERTK). [5], [6]
References
Ref 1 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 2 Company report (Neuronova)
Ref 3 RNA m(6) A methylation regulates uveal melanoma cell proliferation, migration, and invasion by targeting c-Met. J Cell Physiol. 2020 Oct;235(10):7107-7119. doi: 10.1002/jcp.29608. Epub 2020 Feb 4.
Ref 4 ClinicalTrials.gov (NCT03638206) Autologous CAR-T/TCR-T Cell Immunotherapy for Malignancies
Ref 5 A dynamic N(6)-methyladenosine methylome regulates intrinsic and acquired resistance to tyrosine kinase inhibitors. Cell Res. 2018 Nov;28(11):1062-1076. doi: 10.1038/s41422-018-0097-4. Epub 2018 Oct 8.
Ref 6 Clinical pipeline report, company report or official report of Ono Pharmaceutical.