Expanding the scope of PNA-encoded libraries: divergent synthesis of libraries targeting cysteine, serine and metalloproteases as well as tyrosine phosphatases

被引:69
作者
Debaene, Francois [1 ]
Da Silva, Julien A. [1 ]
Pianowski, Zbigniew [1 ]
Duran, Fernando J. [1 ]
Winssinger, Nicolas [1 ]
机构
[1] CNRS, Univ Strasbourg 1, Inst Sci & Ingn Supramol, F-67000 Strasbourg, France
关键词
D O I
10.1016/j.tet.2007.03.033
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Seven PNA-encoded combinatorial libraries targeting proteases and phosphatases with covalent reversible and irreversible mechanism-based inhibitors were prepared. The libraries were synthesized using modified PNA monomers, which dramatically increase the water solubility of the libraries in biologically relevant buffers. The libraries were shown to selectively inhibit targeted enzymes. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:6577 / 6586
页数:10
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