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Park, Cheol-Min
Synthetic & Medicinal Chemistry Lab
Research Interests
  • Organic synthesis, medicinal chemistry, chemical biology

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Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR

Cited 29 times inthomson ciCited 27 times inthomson ci
Title
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR
Author
Petros, Andrew M.Huth, Jeffrey R.Oost, ThorstenPark, Cheol-MinDing, HongWang, XiluZhang, HaichaoNimmer, PaulMendoza, RenaldoSun, ChaohongMack, JameyWalter, KarlDorwin, SarahGramling, EmilyLadror, UriRosenberg, Saul H.Elmore, Steven W.Fesik, Stephen W.Hajduk, Philip J.
Issue Date
2010-11
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.20, no.22, pp.6587 - 6591
Abstract
The Bcl-2 family of proteins plays a major role in the regulation of apoptosis, or programmed cell death. Overexpression of the anti-apoptotic members of this family (Bcl-2, Bcl-xL, and Mcl-1) can render cancer cells resistant to chemotherapeutic agents and therefore these proteins are important targets for the development of new anti-cancer agents. Here we describe the discovery of a potent, highly selective, Bcl-2 inhibitor using SAR by NMR and structure-based drug design which could serve as a starting point for the development of a Bcl-2 selective anti-cancer agent. Such an agent would potentially overcome the Bcl-xL mediated thrombocytopenia observed with ABT-263.
URI
https://scholarworks.unist.ac.kr/handle/201301/8541
URL
http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=77958048793
DOI
10.1016/j.bmcl.2010.09.033
ISSN
0960-894X
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CHM_Journal Papers
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