m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG00652)
Name
AG-024322
Synonyms
AG-24322; N-[[5-[(3E)-3-(4,6-difluorobenzimidazol-2-ylidene)-1,2-dihydroindazol-5-yl]-4-methylpyridin-3-yl]methyl]ethanamine
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Status
Phase 1
Structure
Formula
C23H20F2N6
InChI
1S/C23H20F2N6/c1-3-26-9-14-10-27-11-17(12(14)2)13-4-5-19-16(6-13)21(31-30-19)23-28-20-8-15(24)7-18(25)22(20)29-23/h4-8,10-11,26H,3,9H2,1-2H3,(H,28,29)(H,30,31)
InChIKey
MEKASOQEXYKAKM-UHFFFAOYSA-N
PubChem CID
135413565
TTD Drug ID
D0IX4B
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 1 (CDK1)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 1 (CDK1) is a therapeutic target for AG-024322. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of AG-024322 through regulating the expression of Cyclin-dependent kinase 1 (CDK1). [1], [2]
Protein virilizer homolog (VIRMA)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 1 (CDK1) is a therapeutic target for AG-024322. The Protein virilizer homolog (VIRMA) has potential in affecting the response of AG-024322 through regulating the expression of Cyclin-dependent kinase 1 (CDK1). [2], [3]
Cyclin-dependent kinase 2 (CDK2)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 2 (CDK2) is a therapeutic target for AG-024322. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of AG-024322 through regulating the expression of Cyclin-dependent kinase 2 (CDK2). [2], [4]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 2 (CDK2) is a therapeutic target for AG-024322. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of AG-024322 through regulating the expression of Cyclin-dependent kinase 2 (CDK2). [2], [5]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 2 (CDK2) is a therapeutic target for AG-024322. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of AG-024322 through regulating the expression of Cyclin-dependent kinase 2 (CDK2). [2], [4]
Cyclin-dependent kinase 4 (CDK4)
Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 4 (CDK4) is a therapeutic target for AG-024322. The Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1) has potential in affecting the response of AG-024322 through regulating the expression of Cyclin-dependent kinase 4 (CDK4). [6], [7]
Protein virilizer homolog (VIRMA)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 4 (CDK4) is a therapeutic target for AG-024322. The Protein virilizer homolog (VIRMA) has potential in affecting the response of AG-024322 through regulating the expression of Cyclin-dependent kinase 4 (CDK4). [6], [7]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 4 (CDK4) is a therapeutic target for AG-024322. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of AG-024322 through regulating the expression of Cyclin-dependent kinase 4 (CDK4). [5], [7]
References
Ref 1 CircMETTL3, upregulated in a m6A-dependent manner, promotes breast cancer progression. Int J Biol Sci. 2021 Mar 15;17(5):1178-1190. doi: 10.7150/ijbs.57783. eCollection 2021.
Ref 2 A first in man, phase I dose-escalation study of PHA-793887, an inhibitor of multiple cyclin-dependent kinases (CDK2, 1 and 4) reveals unexpected hepatotoxicity in patients with solid tumors. Cell Cycle. 2011 Mar 15;10(6):963-70. doi: 10.4161/cc.10.6.15075. Epub 2011 Mar 15.
Ref 3 KIAA1429 acts as an oncogenic factor in breast cancer by regulating CDK1 in an N6-methyladenosine-independent manner. Oncogene. 2019 Aug;38(33):6123-6141. doi: 10.1038/s41388-019-0861-z. Epub 2019 Jul 8.
Ref 4 FTO regulates adipogenesis by controlling cell cycle progression via m(6)A-YTHDF2 dependent mechanism. Biochim Biophys Acta Mol Cell Biol Lipids. 2018 Oct;1863(10):1323-1330. doi: 10.1016/j.bbalip.2018.08.008. Epub 2018 Aug 13.
Ref 5 YTHDF1 links hypoxia adaptation and non-small cell lung cancer progression. Nat Commun. 2019 Oct 25;10(1):4892. doi: 10.1038/s41467-019-12801-6.
Ref 6 Identification of pathology-specific regulators of m(6)A RNA modification to optimize lung cancer management in the context of predictive, preventive, and personalized medicine. EPMA J. 2020 Jul 29;11(3):485-504. doi: 10.1007/s13167-020-00220-3. eCollection 2020 Sep.
Ref 7 Liposarcoma: molecular genetics and therapeutics. Sarcoma. 2011;2011:483154. doi: 10.1155/2011/483154. Epub 2010 Dec 27.