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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 저널정보
- 한국미생물생명공학회 Journal of Microbiology and Biotechnology Journal of Microbiology and Biotechnology 제17권 제10호
- 발행연도
- 2007.1
- 수록면
- 1,712 - 1,716 (5page)
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To generate new scaffold candidates as highlyselective and potent cyclin-dependent kinase (CDK) inhibitors,structure-based drug screening was performed utilizing 3Dpharmacophore conformations of known potent inhibitors. Asa result, CR229 (6-bromo-2,3,4,9-tetrahydro-carbolin-1-one)was generated as the hit-compound. A computational dockingstudy using the X-ray crystalographicstructure of CDK2 incomplex with CR229 was evaluated. This predicted bindingmode study of CR229 with CDK2 demonstrated that CR229interacted effectively with the Leu83 and Glu81 residues in theATP-binding pocket of CDK2 for the posible hydrogen bondformation. Furthermore, biochemical studies on inhibitoryeffects of CR229 on various kinases in the human cervicalcancer HeLa cells demonstrated that CR229 was a potentinhibitor of CDK2 (IC50: 3M), CDK1 (IC50: 4.9M), andCDK4 (IC50: 3M), yet had much less inhibitory effect (IC50:>20 M) on other kinases, such as casein kinase 2-α1 (CK2-α1), protein kinase A (PKA), and protein kinase C (PKC).Acordingly, these data demonstrate that CR229 is a potentCDK inhibitor with anticancer efficacy.
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참고문헌 (27)
참고문헌 신청
Choi, Y. H / 2000 / p53- independent induction of p21 (WAF1/CIP1), reduction of cyclin B1 and G2/M arrest by the isoflavone genistein in human prostate carcinoma cells 91 : 1
Davis, S. T / 2001 / Prevention of chemotherapyinduced alopecia in rats by CDK inhibitors 291 : 134 ~ 137
Desjarlais, R. L / 1997 / Generation and use of threedimensional databases for drug discovery : 73 ~ 104
Doerig, C / 2002 / Protein kinases as drug targets in parasitic protozoa 18 : 366 ~ 371
Gray, N / 1999 / ATPsite directed inhibitors of cyclin-dependent kinases 6 : 859 ~ 875
Davis, S. T / 2001 / Prevention of chemotherapyinduced alopecia in rats by CDK inhibitors 291 : 134 ~ 137
Desjarlais, R. L / 1997 / Generation and use of threedimensional databases for drug discovery : 73 ~ 104
Doerig, C / 2002 / Protein kinases as drug targets in parasitic protozoa 18 : 366 ~ 371
Gray, N / 1999 / ATPsite directed inhibitors of cyclin-dependent kinases 6 : 859 ~ 875
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