Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/6410
Title: Discovery of the first potent and selective Mycobacterium tuberculosis Zmp1 inhibitor.
Authors: Mori, Mattia 
Moraca, Francesca
Deodato, Davide
Ferraris, Dm
Selchow, P
Sander, P
Rizzi, M
Botta, Maurizio 
Issue Date: 2014
Project: None 
Journal: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Abstract: 
The Mycobacterium tuberculosis extracellular zinc metalloprotease 1 (Zmp1) has been proposed to play a key role in phagosome maturation and to enhance the survival of Mycobacterium tuberculosis in the host. Consequently, small molecule inhibitors of Zmp1 are of pivotal importance as a tool to better understand the pathogenicity of Zmp1 and as lead candidates for pharmacological intervention. Here we combined in silico structure-based inhibitor design with biochemical studies to discover and characterize the first potent competitive Zmp1 inhibitor showing a Ki of 94nM and a high selectivity for Zmp1 with respect to human Neprilysin.
Description: 
60086
URI: http://hdl.handle.net/20.500.12779/6410
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2014.04.004
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