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.
Original language | English |
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Pages (from-to) | 1761-1766 |
Number of pages | 6 |
Journal | MedChemComm |
Volume | 6 |
Issue number | 10 |
DOIs | |
Publication status | Published - 17 Aug 2015 |