Bortezomib Warhead-Switch Confers Dual Activity against Mycobacterial Caseinolytic Protease and Proteasome and Selectivity against Human Proteasome

Mycobacteria harbor two main degradative proteolytic machineries, the caseinolytic protease ClpP1P2 and a proteasome. We recently showed that Bortezomib inhibits ClpP1P2 and exhibits whole cell activity against Mycobacterium tuberculosis. Bortezomib, a dipeptide with a boronic acid warhead, is a hum...

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Bibliographic Details
Main Authors: Thomas Dick, Wilfried Moreira, Sridhar Santhanakrishnan, Brian W. Dymock
Format: Article
Language:English
Published: Frontiers Media S.A. 2017-04-01
Series:Frontiers in Microbiology
Subjects:
TB
Online Access:http://journal.frontiersin.org/article/10.3389/fmicb.2017.00746/full