Discovery of the first potent and selective Mycobacterium tuberculosis Zmp1 inhibitor

Mattia Mori, Francesca Moraca, Davide Deodato, Davide M. Ferraris, Petra Selchow, Peter Sander, Menico Rizzi, Maurizio Botta

Risultato della ricerca: Contributo su rivistaArticolo in rivistapeer review

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 94 nM and a high selectivity for Zmp1 with respect to human Neprilysin.

Lingua originaleInglese
pagine (da-a)2508-2511
Numero di pagine4
RivistaBioorganic and Medicinal Chemistry Letters
Volume24
Numero di pubblicazione11
DOI
Stato di pubblicazionePubblicato - 1 giu 2014

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