Imperial College London
Professor Robin Leatherbarrow

ProfessorRobinLeatherbarrow

Faculty of Natural Sciences, Department of Chemistry

Academic Visitor
 
 
 
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Contact

 

r.leatherbarrow Website

 
 
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Location

 

ChemistrySouth Kensington Campus

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Summary

 

Publications

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}
}
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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  -
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