Discovery of high affinity inhibitors of -myristoyltransferase.

Medchemcomm

Department of Chemistry , Imperial College London, South Kensington Campus , London , SW7 2AZ , UK . Email: ; Tel: +44 (0) 2075 943752.

Published: October 2015

-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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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4757855PMC
http://dx.doi.org/10.1039/c5md00241aDOI Listing

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