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Issue 10, 2015
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Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase

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Abstract

N-Myristoyltransferase (NMT) is a potential drug target in Leishmania parasites. Scaffold-hopping from published inhibitors yielded the serendipitous discovery of a chemotype selective for Leishmania donovani NMT; development led to high affinity inhibitors with excellent ligand efficiency. The binding mode was characterised by crystallography and provides a structural rationale for selectivity.

Graphical abstract: Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase

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Supplementary files

Article information


Submitted
06 Jun 2015
Accepted
04 Aug 2015
First published
17 Aug 2015

This article is Open Access

Med. Chem. Commun., 2015,6, 1761-1766
Article type
Concise Article
Author version available

Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase

M. D. Rackham, Z. Yu, J. A. Brannigan, W. P. Heal, D. Paape, K. V. Barker, A. J. Wilkinson, D. F. Smith, R. J. Leatherbarrow and E. W. Tate, Med. Chem. Commun., 2015, 6, 1761
DOI: 10.1039/C5MD00241A

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