N-Terminal peptidic boronic acids selectively inhibit human ClpXP

…, J Fishovitz, SB Thorpe, I Lee, WL Santos

文献索引：Knott, Kenneth; Fishovitz, Jennifer; Thorpe, Steven B.; Lee, Irene; Santos, Webster L. Organic and Biomolecular Chemistry, 2010 , vol. 8, # 15 p. 3451 - 3456

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被引用次数: 15

摘要

The synthesis and development of N-terminal peptidic boronic acids as protease inhibitors is reported. N-Terminal peptidic boronic acids interrogate the S′ sites of the target protein for selectivity and provide a new strategy that complements the currently known peptidic α- amino boronic acids (C-terminal boronic acids). After screening a series of N-terminal peptidic boronic acids, the first selective inhibitor of human ClpXP, an ATP-dependent ...