Hubbard Roderick E, Murray James B
Vernalis (R&D) Ltd., Granta Park, Cambridge, United Kingdom; YSBL & HYMS, University of York, Heslington, York, United Kingdom.
Methods Enzymol. 2011;493:509-31. doi: 10.1016/B978-0-12-381274-2.00020-0.
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.
本章总结了Vernalis公司在过去十年中开发和应用基于片段的发现方法于一系列不同靶点的经验。重点将放在不同生物物理技术（表面等离子体共振（SPR）、差示扫描荧光法（DSF）、等温滴定量热法、核磁共振和X射线晶体学）的实际应用方面，这些技术可用于识别与靶点结合的片段，并讨论选择片段并将其发展为先导化合物的标准和策略。
