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A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission

Authors :
David A. Baker
Lindsay B. Stewart
Jonathan M. Large
Paul W. Bowyer
Keith H. Ansell
María B. Jiménez-Díaz
Majida El Bakkouri
Kristian Birchall
Koen J. Dechering
Nathalie S. Bouloc
Peter J. Coombs
David Whalley
Denise J. Harding
Ela Smiljanic-Hurley
Mary C. Wheldon
Eloise M. Walker
Johannes T. Dessens
María José Lafuente
Laura M. Sanz
Francisco-Javier Gamo
Santiago B. Ferrer
Raymond Hui
Teun Bousema
Iñigo Angulo-Barturén
Andy T. Merritt
Simon L. Croft
Winston E. Gutteridge
Catherine A. Kettleborough
Simon A. Osborne
Source :
Nature Communications, Vol 8, Iss 1, Pp 1-9 (2017)
Publication Year :
2017
Publisher :
Nature Portfolio, 2017.

Abstract

Protein kinases are promising drug targets for treatment of malaria. Here, starting with a medicinal chemistry approach, Baker et al. generate an imidazopyridine that selectively targets Plasmodium falciparum PKG, inhibits blood stage parasite growth in vitro and in mice and blocks transmission to mosquitoes.

Subjects

Subjects :
Science

Details

Language :
English
ISSN :
20411723 and 48607312
Volume :
8
Issue :
1
Database :
Directory of Open Access Journals
Journal :
Nature Communications
Publication Type :
Academic Journal
Accession number :
edsdoj.0c48607312374096801bf91f077ff9c0
Document Type :
article
Full Text :
https://doi.org/10.1038/s41467-017-00572-x