期刊
MEDCHEMCOMM
卷 6, 期 10, 页码 1761-1766出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c5md00241a
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资金
- Wellcome Trust [087792]
- Medical Research Council [0900278, U117532067]
- EU [HEALTH-F3-2009-223044]
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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