title: [Progress in the fragment-based drug discovery].
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.
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Ren
authors.forename: Jian
authors.initials: J
authors.lastname: Li
authors.forename: Feng
authors.initials: F
authors.lastname: Shi
authors.forename: Xin
authors.initials: X
authors.lastname: Wang
authors.forename: Jian-Hua
authors.initials: JH
authors.lastname: He
authors.forename: Ye-Chun
authors.initials: YC
authors.lastname: Xu
authors.forename: Nai-Xia
authors.initials: NX
authors.lastname: Zhang
authors.forename: Bing
authors.initials: B
authors.lastname: Xiong
authors.forename: Jing-Kang
authors.initials: JK
authors.lastname: Shen
mesh_terms: D017076:Computer-Aided Design; D018360:Crystallography, X-Ray; D055808:Drug Discovery / Q000379:methods*; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D010446:Peptide Fragments / Q000138:chemical synthesis* / Q000737:chemistry; D011487:Protein Conformation; D054852:Small Molecule Libraries; D020349:Surface Plasmon Resonance
chemical_list: D008024:Ligands; D010446:Peptide Fragments; D054852:Small Molecule Libraries