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.

中文翻译：

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一种监测酪氨酸激酶抑制剂机制的快速方法


Src 激酶结构域内的蛋氨酸残基作为独特的 NMR 探针，能够区分全长 Src 的不同构象状态，包括替代药物抑制形式。这种方法提供了一种快速方法来区分药物开发任何阶段的各种抑制机制，无需解析 Src-药物复合物的结构。使用选择性的 ¹³甲基富集蛋氨酸，可在一小时内获得光谱，而具有可比信息的自然丰度光谱可在几个小时内获得。