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一种通过质谱研究靶蛋白-药物相互作用的创新方法。

An innovative method to study target protein-drug interactions by mass spectrometry.

作者信息

Müller Mathias Q, de Koning Leo J, Schmidt Andreas, Ihling Christian, Syha Yvonne, Rau Oliver, Mechtler Karl, Schubert-Zsilavecz Manfred, Sinz Andrea

机构信息

Department of Pharmaceutical Chemistry and Bioanalytics, Institute of Pharmacy, Martin-Luther-Universität Halle-Wittenberg, Wolfgang-Langenbeck-Strasse 4, D-06120 Halle/Saale, Germany.

出版信息

J Med Chem. 2009 May 14;52(9):2875-9. doi: 10.1021/jm9000665.

DOI:10.1021/jm9000665
PMID:19379014
Abstract

We report the combination of chemical cross-linking and high-resolution mass spectrometry for analyzing conformational changes in target proteins that are induced by drug binding. With this approach conformational changes in the peroxisome proliferator-activated receptor alpha (PPARalpha) upon binding of low-molecular weight compounds were readily detected, proving that the strategy provides a basis to efficiently characterize target protein-drug interactions.

摘要

我们报告了化学交联与高分辨率质谱联用的方法，用于分析药物结合诱导的靶蛋白构象变化。通过这种方法，很容易检测到低分子量化合物结合后过氧化物酶体增殖物激活受体α（PPARα）的构象变化，证明该策略为有效表征靶蛋白-药物相互作用提供了基础。

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