Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 이철훈 | - |
dc.date.accessioned | 2019-07-02T02:39:41Z | - |
dc.date.available | 2019-07-02T02:39:41Z | - |
dc.date.issued | 2007-10 | - |
dc.identifier.citation | JOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY, v. 17, No. 10, Page. 1712-1716 | en_US |
dc.identifier.issn | 1017-7825 | - |
dc.identifier.issn | 1738-8872 | - |
dc.identifier.uri | http://kiss.kstudy.com/thesis/thesis-view.asp?key=2644691 | - |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/107000 | - |
dc.description.abstract | To 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.iso | ko_KR | en_US |
dc.publisher | KOREAN SOC MICROBIOLOGY & BIOTECHNOLOGY | en_US |
dc.subject | CR229 | en_US |
dc.subject | CDK inhibitor | en_US |
dc.subject | structure-based drug screening | en_US |
dc.title | Discovery of cyclin-dependent kinase inhibitor, CR229, using structure-based drug screening | en_US |
dc.type | Article | en_US |
dc.relation.journal | JOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY | - |
dc.contributor.googleauthor | Kim, Min Kyoung | - |
dc.contributor.googleauthor | Min, Jaeki | - |
dc.contributor.googleauthor | Ch, Bu-Young | - |
dc.contributor.googleauthor | Lim, Haeyoung | - |
dc.contributor.googleauthor | Cho, Youl-Hee | - |
dc.contributor.googleauthor | Lee, Chul-Hoon | - |
dc.relation.code | 2007205425 | - |
dc.sector.campus | E | - |
dc.sector.daehak | COLLEGE OF PHARMACY[E] | - |
dc.sector.department | DEPARTMENT OF PHARMACY | - |
dc.identifier.pid | chhlee | - |
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