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通过赖氨酸反应性分析预测配体对膜受体的调节模式。

Prediction of ligand modulation patterns on membrane receptors via lysine reactivity profiling.

机构信息

CAS Key Laboratory of Separation Sciences for Analytical Chemistry, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian, 116023, China.

出版信息

Chem Commun (Camb). 2019 Apr 9;55(30):4311-4314. doi: 10.1039/c9cc00520j.

DOI:10.1039/c9cc00520j
PMID:30829347
Abstract

Herein we provide a mass spectrometry-based lysine reactivity profiling strategy to monitor the ligand modulation of protein receptors, which is achieved by active dimethyl labeling of lysine residues and comparison of the alterations of labeling reactivity during ligand binding. The small-molecule ligand modulation patterns on the catechol-O-methyltransferase and the N-methyl-d-aspartate receptors have been predicted, including both binding regions and related conformational changes.

摘要

在此,我们提供了一种基于质谱的赖氨酸反应性谱分析策略,用于监测配体对蛋白受体的调节作用,该策略通过赖氨酸残基的活性二甲基化标记以及配体结合过程中标记反应性的变化来实现。我们预测了小分子配体对儿茶酚-O-甲基转移酶和 N-甲基-D-天冬氨酸受体的调节模式,包括结合区域和相关构象变化。

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