Discovery of high affinity inhibitors of Leishmania donovani N -myristoyltransferase.
MedChemComm(2015)
摘要
-Myristoyltransferase (NMT) is a potential drug target in parasites. Scaffold-hopping from published inhibitors yielded the serendipitous discovery of a chemotype selective for 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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