Progress in the fragment-based drug discovery
Ren, J.; Li, J.; Shi, F.; Wang, X.; He, J-Hua.; Xu, Y-Chun.; Zhang, N-Xia.; Xiong, B.; Shen, J-Kang.
Yao Xue Xue Bao 48(1): 14-24
2013
ISSN/ISBN: 0513-4870 PMID: 23600136 Document Number: 669497
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.