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- W2890144621 abstract "Crystallography has guided the hybridization of two series of Trypanosoma brucei N-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 led to compounds that have greater than 1000-fold selectivity for TbNMT vs HsNMT. Further optimization of the hybrid series has identified compounds with significant trypanocidal activity capable of crossing the blood-brain barrier. By using CF-1 mdr1a deficient mice, we were able to demonstrate full cures in vivo in a mouse model of stage 2 African sleeping sickness. This and previous work provides very strong validation for NMT as a drug target for human African trypanosomiasis in both the peripheral and central nervous system stages of disease." @default.
- W2890144621 created "2018-09-27" @default.
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- W2890144621 date "2018-09-12" @default.
- W2890144621 modified "2023-10-14" @default.
- W2890144621 title "A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant <i>N</i>-Myristoyltransferase Inhibitors" @default.
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- W2890144621 doi "https://doi.org/10.1021/acs.jmedchem.8b00884" @default.
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