Acta Pharmaceutica Sinica 2013;48(1):14-24

Progress in the fragment-based drug discovery.

Jing REN 1 ; Jian LI ; Feng SHI ; Xin WANG ; Jian-Hua HE ; Ye-Chun XU ; Nai-Xia ZHANG ; Bing XIONG ; Jing-Kang SHEN

Affiliations

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Country

China

Language

Chinese

Abstract

As an extension of the structure-based drug discovery, fragment-based drug discovery is matured increasingly, and plays an important role in drug development. Fragments in a small library, with lower molecular mass and high "ligand efficiency", are detected by SPR, MS, NMR, X-ray crystallography technologies and other biophysical methods. Then they are considered as starting points for chemical optimization with the guidance of structural biology methods to get good "drug-like" lead and candidate compounds. In this article, we reviewed the current progress of fragment-based drug discovery and detailed a number of examples to illustrate the novel strategies.