Nature Communications (Sep 2017)
A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission
- 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
Affiliations
- David A. Baker
- Faculty of Infectious and Tropical Diseases, London School of Hygiene & Tropical Medicine
- Lindsay B. Stewart
- Faculty of Infectious and Tropical Diseases, London School of Hygiene & Tropical Medicine
- Jonathan M. Large
- LifeArc, Accelerator Building
- Paul W. Bowyer
- Faculty of Infectious and Tropical Diseases, London School of Hygiene & Tropical Medicine
- Keith H. Ansell
- LifeArc, Accelerator Building
- María B. Jiménez-Díaz
- Tres Cantos Medicines Development Campus-Diseases of the Developing World
- Majida El Bakkouri
- Structural Genomics Consortium, University of Toronto
- Kristian Birchall
- LifeArc, Accelerator Building
- Koen J. Dechering
- TropIQ Health Sciences
- Nathalie S. Bouloc
- LifeArc, Accelerator Building
- Peter J. Coombs
- LifeArc, Accelerator Building
- David Whalley
- LifeArc, Accelerator Building
- Denise J. Harding
- LifeArc, Accelerator Building
- Ela Smiljanic-Hurley
- LifeArc, Accelerator Building
- Mary C. Wheldon
- LifeArc, Accelerator Building
- Eloise M. Walker
- Faculty of Infectious and Tropical Diseases, London School of Hygiene & Tropical Medicine
- Johannes T. Dessens
- Faculty of Infectious and Tropical Diseases, London School of Hygiene & Tropical Medicine
- María José Lafuente
- Tres Cantos Medicines Development Campus-Diseases of the Developing World
- Laura M. Sanz
- Tres Cantos Medicines Development Campus-Diseases of the Developing World
- Francisco-Javier Gamo
- Tres Cantos Medicines Development Campus-Diseases of the Developing World
- Santiago B. Ferrer
- Tres Cantos Medicines Development Campus-Diseases of the Developing World
- Raymond Hui
- Structural Genomics Consortium, University of Toronto
- Teun Bousema
- Department of Medical Microbiology, Radboud University Medical Center
- Iñigo Angulo-Barturén
- Tres Cantos Medicines Development Campus-Diseases of the Developing World
- Andy T. Merritt
- LifeArc, Accelerator Building
- Simon L. Croft
- Faculty of Infectious and Tropical Diseases, London School of Hygiene & Tropical Medicine
- Winston E. Gutteridge
- Faculty of Infectious and Tropical Diseases, London School of Hygiene & Tropical Medicine
- Catherine A. Kettleborough
- LifeArc, Accelerator Building
- Simon A. Osborne
- LifeArc, Accelerator Building
- DOI
- https://doi.org/10.1038/s41467-017-00572-x
- Journal volume & issue
-
Vol. 8,
no. 1
pp. 1 – 9
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.
