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

Expanding the scope of PNA-encoded libraries: divergent synthesis of libraries targeting cysteine, serine and metalloproteases as well as tyrosine phosphatases
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DOI:
10.1016/j.tet.2007.03.033
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发表时间:
2007-07-09
期刊:
影响因子:
2.1
通讯作者:
Winssinger, Nicolas
Winssinger, Nicolas
中科院分区:
化学3区
文献类型:
--
作者:
Debaene, Francois;Da Silva, Julien A.;Winssinger, Nicolas

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制备了7个针对蛋白水解酶和磷酸酶的PNA编码的组合文库,分别以共价可逆和不可逆机理为基础的抑制剂。这些文库是用修饰的PNA单体合成的,大大增加了文库在生物相关缓冲液中的水溶性。这些文库被证明能够选择性地抑制靶向酶。(C)2007爱思唯尔有限公司。保留所有权利。
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.