A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors

[Image: see text] Crystallography has guided the hybridization of two series of Trypanosoma bruceiN-myristoyltransferase (NMT) inhibitors, leading to a novel highly selective series. The effect of combining the selectivity enhancing elements from two pharmacophores is shown to be additive and has le...

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Udgivet i:J Med Chem
Main Authors: Harrison, Justin R., Brand, Stephen, Smith, Victoria, Robinson, David A., Thompson, Stephen, Smith, Alasdair, Davies, Kenneth, Mok, Ngai, Torrie, Leah S., Collie, Iain, Hallyburton, Irene, Norval, Suzanne, Simeons, Frederick R. C., Stojanovski, Laste, Frearson, Julie A., Brenk, Ruth, Wyatt, Paul G., Gilbert, Ian H., Read, Kevin D.
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2018
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6167002/
https://ncbi.nlm.nih.gov/pubmed/30207721
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b00884
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