Application of a Proteolysis/Mass Spectrometry Method for Investigating the Effects of Inhibitors on Hydroxylase Structure
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- 作者：Christopher J. Stubbs ; Christoph Loenarz ; Jasmin Mecinovi ; Kar Kheng Yeoh ; Nicola Hindley ; Benot M. Linard ; Frank Sobott ; Christopher J. Schofield ; Emily Flashman
- 刊名：Journal of Medicinal Chemistry
- 出版年：2009
- 出版时间：May 14, 2009
- 年：2009
- 卷：52
- 期：9
- 页码：2799-2805
- 全文大小：310K
- 年卷期：v.52,no.9(May 14, 2009)
- ISSN：1520-4804
文摘
Limited proteolysis coupled to matrix-assisted laser desorption/ionization (MALDI) mass spectrometric analyses can be used to screen for compounds that alter protein structure by monitoring stabilizing/destabilizing effects with respect to the rate and nature of proteolysis. When applied to prolyl hydroxylase 2, a key enzyme involved in human oxygen sensing, the method efficiently revealed differential effects on proteolytic stability for structurally similar compounds and for different substrates.