A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission
oleh: 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
| Format: | Article |
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| Diterbitkan: | Nature Portfolio 2017-09-01 |
Deskripsi
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.