Imperial College London
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DrAnnaBarnard

Faculty of Natural Sciences, Department of Chemistry

Wellcome Trust Sir Henry Dale Fellow
 
 
 
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Contact

 

+44 (0)20 7594 8551a.barnard Website

 
 
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Location

 

Office 301MMolecular Sciences Research HubWhite City Campus

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Summary

 

Publications

Citation

BibTex format

@article{Delves:2018:10.1038/s41467-018-05777-2,
author = {Delves, M and Miguel-Blanco, C and Matthews, H and Molina, I and Ruecker, A and Yahiya, S and Straschil, U and Abraham, M and Leon-Diaz, ML and Fischer, O and Zubiaurre, A and Brandt, J and Cortes, A and Barnard, A and Fuchter, M and Calderon, F and Winzeler, E and Sinden, R and Herreros, E and Gamo, FJ and Baum, J},
doi = {10.1038/s41467-018-05777-2},
journal = {Nature Communications},
title = {A high throughput screen for next-generation leads targeting malaria parasite transmission},
url = {http://dx.doi.org/10.1038/s41467-018-05777-2},
volume = {9},
year = {2018}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - Spread of parasite resistance to artemisinin threatens current frontline antimalarial therapies, highlighting the need for new drugs with alternative modes of action. Since only 0.2–1% of asexual parasites differentiate into sexual, transmission-competent forms, targeting this natural bottleneck provides a tangible route to interrupt disease transmission and mitigate resistance selection. Here we present a high-throughput screen of gametogenesis against a ~70,000 compound diversity library, identifying seventeen drug-like molecules that target transmission. Hit molecules possess varied activity profiles including male-specific, dual acting male–female and dual-asexual-sexual, with one promising N-((4-hydroxychroman-4-yl)methyl)-sulphonamide scaffold found to have sub-micromolar activity in vitro and in vivo efficacy. Development of leads with modes of action focussed on the sexual stages of malaria parasite development provide a previously unexplored base from which future therapeutics can be developed, capable of preventing parasite transmission through the population.
AU  - Delves,M
AU  - Miguel-Blanco,C
AU  - Matthews,H
AU  - Molina,I
AU  - Ruecker,A
AU  - Yahiya,S
AU  - Straschil,U
AU  - Abraham,M
AU  - Leon-Diaz,ML
AU  - Fischer,O
AU  - Zubiaurre,A
AU  - Brandt,J
AU  - Cortes,A
AU  - Barnard,A
AU  - Fuchter,M
AU  - Calderon,F
AU  - Winzeler,E
AU  - Sinden,R
AU  - Herreros,E
AU  - Gamo,FJ
AU  - Baum,J
DO  - 10.1038/s41467-018-05777-2
PY  - 2018///
SN  - 2041-1723
TI  - A high throughput screen for next-generation leads targeting malaria parasite transmission
T2  - Nature Communications
UR  - http://dx.doi.org/10.1038/s41467-018-05777-2
UR  - http://hdl.handle.net/10044/1/62850
VL  - 9
ER  -
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