Discovery of Novel and Potent Cdc25 Phosphatase Inhibitors Based on the Structure-Based De Novo Design

Cdc25 phosphatases have been considered as attractive drug targets for anticancer therapy due to the correlation of their overexpression with a wide variety of cancers. We have been able to identify five novel Cdc25 phosphatase inhibitors with micromolar activity by means of a structure-based de nov...

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Bibliographic Details
Published in:Bulletin of the Korean Chemical Society 2009, 30(6), , pp.1313-1316
Main Authors: 박황서, Suk-Kyeong Jung, Young Jae Bahn, Dae Gwin Jeong, 류성언, 김승준
Format: Article
Language:English
Subjects:
화학
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Summary:Cdc25 phosphatases have been considered as attractive drug targets for anticancer therapy due to the correlation of their overexpression with a wide variety of cancers. We have been able to identify five novel Cdc25 phosphatase inhibitors with micromolar activity by means of a structure-based de novo design method with a known inhibitor scaffold. Because the newly discovered inhibitors are structurally diverse and have desirable physicochemical properties as a drug candidate, they deserve further investigation as anticancer drugs. The differences in binding modes of the identified inhibitors in the active sites of Cdc25A and B are addressed in detail. KCI Citation Count: 2
ISSN:0253-2964
1229-5949
DOI:10.5012/bkcs.2009.30.6.1313