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Medchemcomm ; 6(10): 1761-1766, 2015 Oct 08.
Article in English | MEDLINE | ID: mdl-26962429

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.

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