General Information of the Drug (ID: M6APDG00278)
Name
RGB-286638
Synonyms
GPC-286199; RGB-286199; RGB-344064; Non-selective CDK inhibitors, Agennix; Non-selective CDK inhibitors, GPC Biotech; Non-selective cyclin dependent kinase inhibitors, Agennix; Non-selective cyclin dependent kinase inhibitors, GPC Biotech
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Status
Phase 1
Structure
3D MOL
Formula
C29H37Cl2N7O4
InChI
1S/C29H35N7O4.2ClH/c1-39-16-13-34-9-11-35(12-10-34)19-20-5-7-21(8-6-20)26-25-27(32-31-26)22-3-2-4-23(24(22)28(25)37)30-29(38)33-36-14-17-40-18-15-36;;/h2-8H,9-19H2,1H3,(H,31,32)(H2,30,33,38);2*1H
InChIKey
WJVMGQMXUBAAPL-UHFFFAOYSA-N
PubChem CID
11285001
TTD Drug ID
D03DKV
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
Response Summary Cyclin-dependent kinase 1 (CDK1) is a therapeutic target for RGB-286638. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of RGB-286638 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
Response Summary Cyclin-dependent kinase 1 (CDK1) is a therapeutic target for RGB-286638. The Protein virilizer homolog (VIRMA) has potential in affecting the response of RGB-286638 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
Response Summary Cyclin-dependent kinase 2 (CDK2) is a therapeutic target for RGB-286638. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of RGB-286638 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
Response Summary Cyclin-dependent kinase 2 (CDK2) is a therapeutic target for RGB-286638. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of RGB-286638 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
Response Summary Cyclin-dependent kinase 2 (CDK2) is a therapeutic target for RGB-286638. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of RGB-286638 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
Response Summary Cyclin-dependent kinase 4 (CDK4) is a therapeutic target for RGB-286638. The Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1) has potential in affecting the response of RGB-286638 through regulating the expression of Cyclin-dependent kinase 4 (CDK4). [2], [6]
Protein virilizer homolog (VIRMA)
In total 1 mechanisms lead to this potential drug response
Response Summary Cyclin-dependent kinase 4 (CDK4) is a therapeutic target for RGB-286638. The Protein virilizer homolog (VIRMA) has potential in affecting the response of RGB-286638 through regulating the expression of Cyclin-dependent kinase 4 (CDK4). [2], [6]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
Response Summary Cyclin-dependent kinase 4 (CDK4) is a therapeutic target for RGB-286638. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of RGB-286638 through regulating the expression of Cyclin-dependent kinase 4 (CDK4). [2], [5]
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 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66. doi: 10.1038/nrd2907.
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.