Issue 15, 2010

N-Terminal peptidic boronic acids selectively inhibit human ClpXP

Abstract

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 serine protease present in the mitochondrial matrix, was discovered. This should facilitate the understanding of the physiological function of this protease

Graphical abstract: N-Terminal peptidic boronic acids selectively inhibit human ClpXP

Supplementary files

Article information

Article type
Paper
Submitted
16 Mar 2010
Accepted
13 May 2010
First published
04 Jun 2010

Org. Biomol. Chem., 2010,8, 3451-3456

N-Terminal peptidic boronic acids selectively inhibit human ClpXP

K. Knott, J. Fishovitz, S. B. Thorpe, I. Lee and W. L. Santos, Org. Biomol. Chem., 2010, 8, 3451 DOI: 10.1039/C004247A

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