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Non-kinase targets of protein kinase inhibitors
Nature Reviews Drug Discovery ( IF 122.7 ) Pub Date : 2017-03-10 00:00:00 , DOI: 10.1038/nrd.2016.266
Lenka Munoz

Inhibition of proteins other than the intended target by small molecules can lead to the incorrect assignment of biological functions to particular proteins and wasted drug development efforts. Potential inhibition of off-target kinases by kinase inhibitors is often investigated, but kinase inhibitors can also inhibit non-kinases. Munoz examines the growing number of examples of this issue and suggests a systematic strategy to verify which protein is responsible for the effects of a given small molecule.

中文翻译:

蛋白激酶抑制剂的非激酶靶标

小分子对非预期目标蛋白质的抑制会导致将生物学功能错误分配给特定蛋白质,并浪费了药物开发的精力。经常研究激酶抑制剂对脱靶激酶的潜在抑制作用,但是激酶抑制剂也可以抑制非激酶。Munoz研究了这个问题的越来越多的例子,并提出了一种系统的策略来验证哪种蛋白质负责给定小分子的作用。
更新日期:2017-04-06
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