Journal
TRENDS IN PHARMACOLOGICAL SCIENCES
Volume 36, Issue 7, Pages 452-460Publisher
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2015.04.011
Keywords
serine-threonine protein kinases; gatekeeper; ATP-binding pocket; orthogonal inhibitors; chemotherapy; parasites
Categories
Funding
- NIH [AI094098]
Ask authors/readers for more resources
Apicomplexan parasites cause some of the most severe human diseases, including malaria (caused by Plasmodium), toxoplasmosis, and cryptosporidiosis. Treatments are limited by the lack of effective drugs and development of resistance to available agents. By exploiting novel features of protein kinases in these parasites, it may be possible to develop new treatments. We summarize here recent advances in identifying small molecule inhibitors against a novel family of plant-like, calcium-dependent kinases that are uniquely expanded in apicomplexan parasite. Analysis of the 3D structure, activation mechanism, and sensitivity to small molecules had identified several attractive chemical scaffolds that are potent and selective inhibitors of these parasite kinases. Further optimization of these leads may yield promising new drugs for treatment of these parasitic infections.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available