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Structural chemoproteomics and drug discovery

✍ Scribed by Dongkyu Shin; Yong-Seok Heo; Kyung Joo Lee; Cheol Min Kim; Jung Min Yoon; Jae Il Lee; Young-Lan Hyun; Young Ho Jeon; Tae Gyu Lee; Joong Myung Cho; Seonggu Ro

Publisher: Wiley (John Wiley & Sons)
Year: 2005
Tongue: English
Weight: 307 KB
Volume: 80
Category: Article
ISSN: 0006-3525
DOI: 10.1002/bip.20263

No coin nor oath required. For personal study only.

✦ Synopsis

Abstract

Our laboratories have developed several technologies to accelerate drug discovery process on the basis of structural chemoproteomics. They include SPS™ technology for the efficient determination of protein structures, SCP™ technology for the rapid lead generation and SDF™ technology for the productive lead optimization. Using these technologies, we could determine many 3D structures of target proteins bound with biologically active chemicals including the structure of phosphodiesterase 5/Viagra complex and obtain highly potent compounds in animal models of obesity, diabetes, cancer and inflammation. In this paper, we will discuss concepts and applications of structural chemoproteomics for drug discovery. © 2005 Wiley Periodicals, Inc. Biopolymers (Pept Sci), 2005

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