EXPERIENCES IN FRAGMENT-BASED LEAD DISCOVERY

被引：79

作者：

Hubbard, Roderick E. ^{[1
,2
,3
]}

Murray, James B. ^{[1
]}

机构：

[1] Vernalis R&D Ltd, Cambridge, England

[2] Univ York, YSBL, York YO10 5DD, N Yorkshire, England

[3] Univ York, HYMS, York YO10 5DD, N Yorkshire, England

来源：

FRAGMENT-BASED DRUG DESIGN: TOOLS, PRACTICAL APPROACHES, AND EXAMPLES | 2011年 / 493卷

关键词：

SURFACE-PLASMON RESONANCE; DRUG DISCOVERY; INHIBITORS; DESIGN; PROTEIN; STRATEGIES; CHAPERONE; LIGANDS; FAMILY; NMR;

D O I：

10.1016/B978-0-12-381274-2.00020-0

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

This chapter summarizes the experience at Vernalis over the past decade in developing and applying fragment-based discovery methods across a range of different targets. The emphasis will be on the practical aspects of the different biophysical techniques (surface plasmon resonance (SPR), differential scanning fluorimetry (DSF), isothermal titration calorimetry, nuclear magnetic resonance, and X-ray crystallography) that can be used to identify fragments that bind to targets and a discussion of the criteria and strategies for selecting and evolving fragments to lead compounds.

引用

页码：509 / 531

页数：23

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