m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG03326)
Name
Roscovitine
Synonyms
Seliciclib; roscovitine; 186692-46-6; R-Roscovitine; (R)-roscovitine; CYC202; CYC-202; CYC 202; 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine; UNII-0ES1C2KQ94; Roscovitine (Seliciclib,CYC202); NSC 701554; AL-39256; Roscovitine; CHEMBL14762; 0ES1C2KQ94; CHEBI:45307; NSC701554; NSC-701554; (2R)-2-[[6-(benzylamino)-9-isopropyl-purin-2-yl]amino]butan-1-ol; (R)-2-((6-(Benzylamino)-9-isopropyl-9H-purin-2-yl)amino)butan-1-ol; (2R)-2-[[6-(benzylamino)-9-propan-2-ylpurin-2-yl]amino]butan-1-ol; RRC; Rosco; M02443; BMK1-E12; CYC202, Seliciclib, R-roscovitine, Roscovitine; (2r)-2-{[6-(benzylamino)-9-isopropyl-9h-purin-2-yl]amino}-1-butanol; 2-(R)-[[9-(1-Methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-1-butanol; 2-[[9-(1-Methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-(R)-1-butanol; 6-(Benzylamino)-2(R)-[[1-(hydroxymethyl)propyl]amino]-9-isopropylpurine
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Status
Phase 2
Structure
Formula
C19H26N6O
InChI
1S/C19H26N6O/c1-4-15(11-26)22-19-23-17(20-10-14-8-6-5-7-9-14)16-18(24-19)25(12-21-16)13(2)3/h5-9,12-13,15,26H,4,10-11H2,1-3H3,(H2,20,22,23,24)/t15-/m1/s1
InChIKey
BTIHMVBBUGXLCJ-OAHLLOKOSA-N
PubChem CID
160355
TTD Drug ID
D05ADP
VARIDT Drug ID
DR01494
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 Roscovitine. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Roscovitine 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 Roscovitine. The Protein virilizer homolog (VIRMA) has potential in affecting the response of Roscovitine 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 Roscovitine. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of Roscovitine 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 Roscovitine. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of Roscovitine 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 Roscovitine. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of Roscovitine through regulating the expression of Cyclin-dependent kinase 2 (CDK2). [2], [4]
P-glycoprotein 1 (ABCB1)
Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary P-glycoprotein 1 (ABCB1) is a therapeutic target for Roscovitine. The Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3) has potential in affecting the response of Roscovitine through regulating the expression of P-glycoprotein 1 (ABCB1). [6], [7]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary P-glycoprotein 1 (ABCB1) is a therapeutic target for Roscovitine. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Roscovitine through regulating the expression of P-glycoprotein 1 (ABCB1). [7], [8]
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 comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
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 Binding of RNA m6A by IGF2BP3 triggers chemoresistance of HCT8 cells via upregulation of ABCB1. Am J Cancer Res. 2021 Apr 15;11(4):1428-1445. eCollection 2021.
Ref 7 ATP-binding cassette B1 transports seliciclib (R-roscovitine), a cyclin-dependent kinase inhibitor. Drug Metab Dispos. 2010 Nov;38(11):2000-6.
Ref 8 METTL3 promotes adriamycin resistance in MCF-7 breast cancer cells by accelerating pri-microRNA-221-3p maturation in a m6A-dependent manner. Exp Mol Med. 2021 Jan;53(1):91-102. doi: 10.1038/s12276-020-00510-w. Epub 2021 Jan 8.