Progress in the fragment-based drug discovery.
- Author:
Jing REN
;
Jian LI
;
Feng SHI
;
Xin WANG
;
Jianhua HE
;
Yechun XU
;
Naixia ZHANG
;
Bing XIONG
;
Jingkang SHEN
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2013;48(1):14-24
- CountryChina
- 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.
