Dynamic Combinatorial Chemistry Employing Boronic Acids/Boronate Esters Leads to Potent Oxygenase Inhibitors

被引:69
作者
Demetriades, Marina [2 ]
Leung, Ivanhoe K. H. [2 ]
Chowdhury, Rasheduzzaman [2 ]
Chan, Mun Chiang [2 ]
McDonough, Michael A. [2 ]
Yeoh, Kar Kheng [2 ]
Tian, Ya-Min [3 ]
Claridge, Timothy D. W. [2 ]
Ratcliffe, Peter J. [3 ]
Woon, Esther C. Y. [1 ]
Schofield, Christopher J. [2 ]
机构
[1] Natl Univ Singapore, Dept Pharm, Singapore 117543, Singapore
[2] Univ Oxford, Chem Res Lab, Oxford OX1 3TA, England
[3] Univ Oxford, Nuffield Dept Clin Med, Oxford OX3 7BN, England
关键词
boron; combinatorial chemistry; mass spectrometry; oxygenase; prolyl hydroxylase; MASS-SPECTROMETRY LEADS; BINDING INTERACTIONS; ACID;
D O I
10.1002/anie.201202000
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Dynamic duo: The reversible reaction of boronic acids with alcohols to form boronate esters, coupled to protein mass spectrometry analyses, was used to discover potent oxygenase inhibitors. This dynamic combinatorial mass spectrometry technique could potentially be applied to the identification of other protein inhibitors. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
引用
收藏
页码:6672 / 6675
页数:4
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