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

Author

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, and Simon A. Osborne

Subjects
Science
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.

Published
2017
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