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dc.contributor.author이철훈-
dc.date.accessioned2019-07-02T02:39:41Z-
dc.date.available2019-07-02T02:39:41Z-
dc.date.issued2007-10-
dc.identifier.citationJOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY, v. 17, No. 10, Page. 1712-1716en_US
dc.identifier.issn1017-7825-
dc.identifier.issn1738-8872-
dc.identifier.urihttp://kiss.kstudy.com/thesis/thesis-view.asp?key=2644691-
dc.identifier.urihttps://repository.hanyang.ac.kr/handle/20.500.11754/107000-
dc.description.abstractTo generate new scaffold candidates as highly selective and potent cyclin-dependent kinase (CDK) inhibitors, structure-based drug screening was performed utilizing 3D pharmacophore conformations of known potent inhibitors. As a result, CR229 (6-bromo-2,3,4,9-tetrahydro-carbolin-1-one) was generated as the hit-compound. A computational docking study using the X-ray crystallographic structure of CDK2 in complex with CR229 was evaluated. This predicted binding mode study of CR229 with CDK2 demonstrated that CR229 interacted effectively with the Leu83 and Glu81 residues in the ATP-binding pocket of CDK2 for the possible hydrogen bond formation. Furthermore, biochemical studies on inhibitory effects of CR229 on various kinases in the human cervical cancer HeLa cells demonstrated that CR229 was a potent inhibitor of CDK2 (IC50: 3 mu M), CDK1 (IC50: 4.9 mu M), and CDK4 (IC50: 3 9 mu M), yet had much less inhibitory effect (IC50: >20 mu M) on other kinases, such as casein kinase 2-alpha 1 (CK2-alpha 1), protein kinase A (PKA), and protein kinase C (PKC). Accordingly, these data demonstrate that CR229 is a potent CDK inhibitor with anticancer efficacy.en_US
dc.language.isoko_KRen_US
dc.publisherKOREAN SOC MICROBIOLOGY & BIOTECHNOLOGYen_US
dc.subjectCR229en_US
dc.subjectCDK inhibitoren_US
dc.subjectstructure-based drug screeningen_US
dc.titleDiscovery of cyclin-dependent kinase inhibitor, CR229, using structure-based drug screeningen_US
dc.typeArticleen_US
dc.relation.journalJOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY-
dc.contributor.googleauthorKim, Min Kyoung-
dc.contributor.googleauthorMin, Jaeki-
dc.contributor.googleauthorCh, Bu-Young-
dc.contributor.googleauthorLim, Haeyoung-
dc.contributor.googleauthorCho, Youl-Hee-
dc.contributor.googleauthorLee, Chul-Hoon-
dc.relation.code2007205425-
dc.sector.campusE-
dc.sector.daehakCOLLEGE OF PHARMACY[E]-
dc.sector.departmentDEPARTMENT OF PHARMACY-
dc.identifier.pidchhlee-
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COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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