4.1 Article

Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase

期刊

MEDCHEMCOMM
卷 6, 期 10, 页码 1761-1766

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c5md00241a

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资金

  1. Wellcome Trust [087792]
  2. Medical Research Council [0900278, U117532067]
  3. EU [HEALTH-F3-2009-223044]

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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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