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Citation

BibTex format

@article{Goncalves:2012:10.1021/jm300040p,
author = {Goncalves, V and Brannigan, JA and Whalley, D and Ansell, KH and Saxty, B and Holder, AA and Wilkinson, AJ and Tate, EW and Leatherbarrow, RJ},
doi = {10.1021/jm300040p},
journal = {Journal of Medicinal Chemistry},
pages = {3578--3582},
title = {Discovery of Plasmodium vivax N-Myristoyltransferase Inhibitors: Screening, Synthesis, and Structural Characterization of their Binding Mode},
url = {http://dx.doi.org/10.1021/jm300040p},
volume = {55},
year = {2012}
}

RIS format (EndNote, RefMan)

TY  - JOUR
AB - N-Myristoyltransferase (NMT) is a prospective drug target against parasitic protozoa. Herein we report the successful discovery of a series of Plasmodium vivax NMT inhibitors by high-throughput screening. A high-resolution crystal structure of the hit compound in complex with NMT was obtained, allowing understanding of its novel binding mode. A set of analogues was designed and tested to define the chemical groups relevant for activity and selectivity.
AU - Goncalves,V
AU - Brannigan,JA
AU - Whalley,D
AU - Ansell,KH
AU - Saxty,B
AU - Holder,AA
AU - Wilkinson,AJ
AU - Tate,EW
AU - Leatherbarrow,RJ
DO - 10.1021/jm300040p
EP - 3582
PY - 2012///
SN - 0022-2623
SP - 3578
TI - Discovery of Plasmodium vivax N-Myristoyltransferase Inhibitors: Screening, Synthesis, and Structural Characterization of their Binding Mode
T2 - Journal of Medicinal Chemistry
UR - http://dx.doi.org/10.1021/jm300040p
UR - http://hdl.handle.net/10044/1/26848
VL - 55
ER -

Contact

Prof. Ed Tate
GSK Chair in Chemical Biology
Department of Chemistry
Molecular Sciences Research Hub, White City Campus,
82 Wood Lane, London, W12 0BZ

e.tate@imperial.ac.uk
Tel: +44 (0)20 759 + ext 43752 or 45821