Last Updated: 06/11/2023
Kinase prioritization and discovery of compounds with anti-malarial activity against different stages of Plasmodium vivax using chemogenomics, bioinformatics, cheminformatics, and experimental evaluation tools
Objectives
*Original title in Portuguese: Priorização de quinases e descoberta de compostos com atividade antimalárica contra diferentes estágios de Plasmodium vivax utilizando ferramentas de quimiogenômica, bioinformática, quimioinformática e ensaios experimentais
The goal of this work plan is the identification of compounds that target kinases with antiplasmodial activity in P. vivax isolates through chemogenomics, bioinformatics, cheminformatics, and experimental assays strategies.
Malaria is one of the main diseases in tropical and subtropical countries in the world, caused by protozoa from the genus Plasmodium. Nowadays, the main strategy in the control of Malaria is based on the treatment. The always-recurrent resistance to the antimalarial drugs is a big barrier to the battle against Malaria, leading to new outbreaks of the disease. Among the potential new therapeutic targets against Malaria, the protein kinases stand out for their capabilities to interfere in other protein’s activities through phosphorylation and for their involvement in almost all cellular processes. The kinome study is very important for the understanding of parasite physiology and gives information about how to interrupt adaptive mechanisms of these organisms. Computer-Aided Drug Design (CADD) is considered a great strategy to increase the success rate in the discovery of active compounds with a smaller cost. To achieve the goal, this research will characterize and update the kinome of different Plasmodium species, prioritize kinases as therapeutic targets and repurpose drugs that might target these kinases. It will also develop an integrative in silico platform to the discovery of new multistage antimalarial drugs.
Feb 2020 — May 2022
