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Structural chemoproteomics and drug discovery.

Shin D, Heo YS, Lee KJ, Kim CM, Yoon JM, Lee JI, Hyun YL, Jeon YH, Lee TG, Cho JM, Ro S

CrystalGenomics, Inc., Asian Institute for Life Sciences, 388-1 Pungnap-dong, Songpa-gu, Seoul, 138-736, Korea.

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.

Published 25 April 2005 in Biopolymers, 80(2): 258-63.
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