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Issue 77, 2017
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Identification of inhibitors targeting Mycobacterium tuberculosis cell wall biosynthesis via dynamic combinatorial chemistry

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Abstract

In this study, we report a dynamic combinatorial approach along with highly efficient in situ screening to identify inhibitors of UDP-galactopyranose mutase (UGM), an essential enzyme involved in mycobacterial cell wall biosynthesis. These two technologies converged to the identification of a new UGM inhibitor chemotype. Importantly, the best molecule not only displayed high affinity for the target enzyme but also exhibited in vitro growth inhibition against whole Mycobacterium tuberculosis cells. The strategy described here provides an avenue to explore a novel inhibitor class for UGMs and paves the way for further pharmacological studies on tuberculosis treatment.

Graphical abstract: Identification of inhibitors targeting Mycobacterium tuberculosis cell wall biosynthesis via dynamic combinatorial chemistry

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Publication details

The article was received on 07 Jul 2017, accepted on 09 Aug 2017 and first published on 09 Aug 2017


Article type: Communication
DOI: 10.1039/C7CC05251K
Citation: Chem. Commun., 2017,53, 10632-10635
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    Identification of inhibitors targeting Mycobacterium tuberculosis cell wall biosynthesis via dynamic combinatorial chemistry

    J. Fu, H. Fu, M. Dieu, I. Halloum, L. Kremer, Y. Xia, W. Pan and S. P. Vincent, Chem. Commun., 2017, 53, 10632
    DOI: 10.1039/C7CC05251K

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