Dataset Information

Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase.

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.

SUBMITTER: Rackham MD

PROVIDER: S-EPMC4757855 | biostudies-literature | 2015 Oct

REPOSITORIES: biostudies-literature

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Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase.

Rackham Mark D MD Yu Zhiyong Z Brannigan James A JA Heal William P WP Paape Daniel D Barker K Victoria KV Wilkinson Anthony J AJ Smith Deborah F DF Leatherbarrow Robin J RJ Tate Edward W EW

MedChemComm 20150819 10

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. ...[more]

PMID: 26962429

Dataset Information

Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase.

Publications

Discovery of high affinity inhibitors of <i>Leishmania donovani N</i>-myristoyltransferase.

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