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

Autor: 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
Jazyk: angličtina
Rok vydání: 2017
Předmět:
Zdroj: Nature Communications, Vol 8, Iss 1, Pp 1-9 (2017)
Druh dokumentu: article
ISSN: 2041-1723
48607312
DOI: 10.1038/s41467-017-00572-x
Popis: 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.
Databáze: Directory of Open Access Journals