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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Veröffentlicht in:Front Microbiol
Hauptverfasser: Moreira, Wilfried, Santhanakrishnan, Sridhar, Dymock, Brian W., Dick, Thomas
Format: Artigo
Sprache:Inglês
Veröffentlicht: Frontiers Media S.A. 2017
Schlagworte:
Microbiology
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5406460/
https://ncbi.nlm.nih.gov/pubmed/28496439
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.3389/fmicb.2017.00746
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