Last Updated: 05/01/2025
Discovery and planning Plasmodium falciparum enolase inhibitors as new antimalarial agents
Objectives
This project aims to discover and develop bioactive molecules as candidate antimalarial drugs. To this end, a strategy involving methods in enzyme kinetics, structural biology and medicinal chemistry was planned.
Enolase Plasmodium falciparum (Pfen), is an important biomolecule in the glycolytic pathway and essential to the development of the protozoa, since the parasite is highly dependent on glycolysis for energy production. Furthermore, Pfen has been found in many subcellular compartments (cytosol, nucleus, plasma membrane, vacuole and cytoskeleton), suggesting alternative functions (function moonlight) that are not related to the glycolytic pathway. So Pfen is an attractive molecular target for the search for new therapeutic opportunities ahead to malaria.
Natural products are isolated compounds and extracts from Brazilian plants were selected based on ethnobotanical knowledge and chemotaxonomic. The synthetic compounds were provided by non-governmental organization “Medicine for Malaria Venture” (MMV), which have antiplasmodial activity in vitro, however, with still unknown mechanism of inhibition.
The integration of modern strategies of drug design will be critical to determining the mechanism of action of the identified bioactive compounds as well as for the development of molecules with optimized properties to new drug candidates antimalarials.
Apr 2015 — Mar 2017
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