Structural highlights
Function
[NMT_ASPFU] Adds a myristoyl group to the N-terminal glycine residue of certain cellular proteins.
Publication Abstract from PubMed
N-Myristoyltransferase (NMT) represents a promising drug target within the parasitic protozoa Trpanosoma brucei (T. brucei), the causative agent for human African trypanosomiasis (HAT) or sleeping sickness. We have previously validated T. brucei NMT as a promising druggable target for the treatment of HAT in both stage 1 and 2 of the disease. We report on the use of the previously reported DDD85646 (1) as a start point for the design of a class of potent, brain penetrant inhibitors of T. brucei NMT.
Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors.,Bayliss T, Robinson DA, Smith VC, Brand S, McElroy SP, Torrie LS, Mpamhanga C, Norval S, Stojanovski L, Brenk R, Frearson JA, Read KD, Gilbert IH, Wyatt PG J Med Chem. 2017 Nov 10. doi: 10.1021/acs.jmedchem.7b01255. PMID:29125744[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Bayliss T, Robinson DA, Smith VC, Brand S, McElroy SP, Torrie LS, Mpamhanga C, Norval S, Stojanovski L, Brenk R, Frearson JA, Read KD, Gilbert IH, Wyatt PG. Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors. J Med Chem. 2017 Nov 10. doi: 10.1021/acs.jmedchem.7b01255. PMID:29125744 doi:http://dx.doi.org/10.1021/acs.jmedchem.7b01255
