筛选蛋白激酶和抑制剂的分析方法,包括动力学评估

IF 11.8 1区 化学 Q1 CHEMISTRY, ANALYTICAL
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引用次数: 0

摘要

蛋白激酶促进细胞生长和增殖等细胞过程,肿瘤细胞和健康细胞的情况类似。药物研究旨在开发能抑制肿瘤生长的小分子药物,这些药物能与特定蛋白激酶的 ATP 结合袋结合。要了解抑制剂的特异性,激酶-抑制剂结合过程的热力学和动力学数据非常重要。有多种分析方法可以研究蛋白激酶与抑制剂之间的相互作用。然而,目前还没有一种全面的策略能同时提供特异性筛选和结合动力学方面的信息。本综述旨在总结不仅用于监测蛋白激酶抑制作用,而且用于在筛选应用的基础上提供动力学和热力学数据的分析方法。重点放在最有前途的光学生物传感技术上。我们讨论了各种方法的智能组合可以提供蛋白激酶与抑制剂相互作用的全面信息。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Analytical methods for protein kinase and inhibitor screening including kinetic evaluation
Protein kinases promote cell processes such as cell growth and proliferation similarly in tumor cells and healthy cells. Pharmaceutical research aims at developing small molecules that inhibit tumor growth binding in the ATP-binding pocket of specific protein kinases. To understand the specificity of the inhibitor, thermodynamic and kinetic data of the kinase-inhibitor binding process are important. A broad range of analytical methods may investigate the interactions between protein kinases and inhibitors. Today, however, there is no comprehensive strategy to provide information on both specificity screening and binding kinetics. The purpose of this review is to summarize analytical methods used not only to monitor the protein kinase inhibition, but also to provide kinetic and thermodynamic data on the basis of screening applications. A focus is set on optical biosensing as the most promising techniques. We discuss, that intelligent combinations of methods can provide comprehensive information on protein kinases interacting with inhibitors.
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来源期刊
Trends in Analytical Chemistry
Trends in Analytical Chemistry 化学-分析化学
CiteScore
20.00
自引率
4.60%
发文量
257
审稿时长
3.4 months
期刊介绍: TrAC publishes succinct and critical overviews of recent advancements in analytical chemistry, designed to assist analytical chemists and other users of analytical techniques. These reviews offer excellent, up-to-date, and timely coverage of various topics within analytical chemistry. Encompassing areas such as analytical instrumentation, biomedical analysis, biomolecular analysis, biosensors, chemical analysis, chemometrics, clinical chemistry, drug discovery, environmental analysis and monitoring, food analysis, forensic science, laboratory automation, materials science, metabolomics, pesticide-residue analysis, pharmaceutical analysis, proteomics, surface science, and water analysis and monitoring, these critical reviews provide comprehensive insights for practitioners in the field.
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