Identification of PfPKG (protein kinase G) inhibitors as antimalarial potential

Malaria remains a serious public health problem in several countries around the world, including Brazil. Although the number of cases has been falling consistently in recent years due to strategies to combat malaria, major challenges still remain for the eradication of the disease. Among the main obstacles, the recurrent evolution of Plasmodium resistance to antimalarial drugs deserves mention. This is because in the absence of an effective vaccine, immediate treatment contributes to interrupting the transmission of the parasite. Within this context, identifying compounds that are active against malaria parasites is of great importance. A virtual screening strategy will be used to select compounds with inhibitory potential against the protein kinase G (PKG) of the parasite. This kinase is essential during the different stages of the parasite’s life cycle, including the asexual blood stages, responsible for the symptoms of the disease. The selected compounds will then be validated experimentally in in vitro tests against P. falciparum, and the cytotoxicity of the compounds will be measured using human cells. These efforts aim to support the identification of compounds that may be candidates for the development of new antimalarials.

Project details

Drug Resistance
Drug-based Strategies

Jul 2017 — Dec 2017

Brazil