监测酪氨酸激酶抑制剂机制的快速方法

IF 5.3 2区材料科学 Q2 MATERIALS SCIENCE, MULTIDISCIPLINARY

ACS Applied Nano Materials Pub Date : 2024-11-08 DOI:10.1021/acs.jmedchem.4c02042

Alejandro Fernández, Margarida Gairí, María Teresa González, Miquel Pons

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引用次数: 0

摘要

Src 激酶结构域内的蛋氨酸残基是独特的核磁共振探针，能够区分全长 Src 的不同构象状态，包括药物抑制的替代形式。这种方法提供了在药物开发的任何阶段区分各种抑制机制的快速方法，无需解析 Src-药物复合物的结构。利用选择性 13C 甲基富集蛋氨酸，可以在一小时内获得光谱，而在几小时内就能获得具有可比信息的自然丰度光谱。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

A Fast Method to Monitor Tyrosine Kinase Inhibitor Mechanisms

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A Fast Method to Monitor Tyrosine Kinase Inhibitor Mechanisms

Methionine residues within the kinase domain of Src serve as unique NMR probes capable of distinguishing between distinct conformational states of full-length Src, including alternative drug-inhibited forms. This approach offers a rapid method to differentiate between various inhibition mechanisms at any stage of drug development, eliminating the need to resolve the structure of Src-drug complexes. Using selectively ¹³C-methyl-enriched methionine, spectra can be acquired in under an hour, while natural abundance spectra with comparable information are achievable within a few hours.

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来源期刊

ACS Applied Nano Materials Multiple-

CiteScore

8.30

自引率

3.40%

发文量

1601

期刊介绍： ACS Applied Nano Materials is an interdisciplinary journal publishing original research covering all aspects of engineering, chemistry, physics and biology relevant to applications of nanomaterials. The journal is devoted to reports of new and original experimental and theoretical research of an applied nature that integrate knowledge in the areas of materials, engineering, physics, bioscience, and chemistry into important applications of nanomaterials.