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用于发现信号转导抑制剂的新型化学遗传学方法。

Novel chemical genetic approaches to the discovery of signal transduction inhibitors.

作者信息

Shokat Kevan, Velleca Mark

机构信息

Dept of Cellular and Molecular Pharmacology, University of California at San Francisco, San Francisco, CA, USA.

出版信息

Drug Discov Today. 2002 Aug 15;7(16):872-9. doi: 10.1016/s1359-6446(02)02391-7.

Abstract

Concurrent advances in both high-throughput chemistry and genomics have given rise to the field of chemical genetics as a discipline for elucidating and validating drug targets, and generating novel therapeutics. Indeed, chemical genetic approaches to drug discovery have now been applied to several important drug target classes, especially those involved in signal transduction. Chemical genetics is distinct from the broader term "chemogenomics" which is defined as the description of all possible drugs against all possible targets (reviewed in [1]). This review covers several "orthogonal" chemical genetic approaches and focuses on a unique analog sensitive kinase technology and its applications to kinase drug discovery.

摘要

高通量化学和基因组学的同步发展催生了化学遗传学这一学科,用于阐明和验证药物靶点,并开发新型治疗方法。事实上,化学遗传学方法现已应用于多个重要的药物靶点类别,尤其是那些参与信号转导的靶点。化学遗传学与更宽泛的术语“化学基因组学”不同,后者被定义为针对所有可能靶点的所有可能药物的描述(见[1]综述)。本综述涵盖了几种“正交”化学遗传学方法,并重点介绍了一种独特的模拟敏感激酶技术及其在激酶药物发现中的应用。

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