Fragment-based approaches to enzyme inhibition.

Fragment-based approaches to enzyme inhibition.
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DOI:
10.1016/j.copbio.2007.09.003
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发表时间:
2007-12
影响因子:
7.7
通讯作者:
Abell, Chris
Abell, Chris
中科院分区:
工程技术1区
文献类型:
--
作者:
Ciulli, Alessio;Abell, Chris

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基于片段的方法为小分子药物的发现提供了一个新的范例。该方法是对高通量筛选方法的补充,从低分子复杂性和高配体效率的片段开始,建立更有效的抑制剂。这种方法在很大程度上依赖于许多生物物理技术,现在正被工业界和学术界的更多团体采用。本文描述了该流程的关键方面,并重点介绍了最近的开发和应用。
Fragment-based approaches have provided a new paradigm for small-molecule drug discovery. The methodology is complementary to high-throughput screening approaches, starting from fragments of low molecular complexity and high ligand efficiency, and building up to more potent inhibitors. The approach, which depends heavily on a number of biophysical techniques, is now being taken up by more groups in both industry and academia. This article describes key aspects of the process and highlights recent developments and applications.
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