Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase

Mark D. Rackham, Zhiyong Yu, James A. Brannigan, William P. Heal, Daniel Paape, K. Victoria Barker, Anthony J. Wilkinson, Deborah F. Smith, Robin J. Leatherbarrow, Edward W. Tate*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review


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.

Original languageEnglish
Pages (from-to)1761-1766
Number of pages6
Issue number10
Publication statusPublished - 17 Aug 2015

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