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Application of a proteolysis/mass spectrometry method for investigating the effects of inhibitors on hydroxylase structure.

Abstract:
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.
Publication status:
Published

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Publisher copy:
10.1021/jm900285r

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Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry, Organic Chemistry
Role:
Author
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Journal:
Journal of medicinal chemistry
Volume:
52
Issue:
9
Pages:
2799-2805
Publication date:
2009-05-05
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:ebcdba2f-b4e1-42b8-a2ed-baa8b1395237
Source identifiers:
34680
Local pid:
pubs:34680

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