Last Updated: 10/12/2025
Discovery and development of antimalarial drugs: Structural biology, medicinal chemistry and parasitology
Objectives
*Original title in Portuguese: Descoberta e Desenvolvimento de Fármacos Antimaláricos: Biologia Estrutural, Química Medicinal e Parasitologia
The research project aims at:
- the elucidation of the three-dimensional structure of phosphatidylinositol-4-OH kinase (PI4K), an important enzyme in the metabolism of Plasmodium falciparum;
- the standardization and development of in vitro and in vivo tests of bioactive molecules as candidates for antimalarials and
- the discovery and development of new bioactive compounds as drug candidates for malaria.
Malaria, caused by protozoa of the genus Plasmodium, is one of the main public health problems in the world. The disease occurs in 109 countries, being endemic in tropical and subtropical regions of Africa, Southeast Asia and Latin America. Half of the world’s population (3.3 billion people) is exposed to malaria transmission in risk areas. In 2013, 198 million cases and 584 thousand deaths were recorded, most of them in Africa (WHO, 2014). The emergence of drug resistance cases makes the search for new molecular targets and the development of chemotherapeutic agents against the disease extremely important. To achieve the objectives, integrated studies in structural molecular biology, enzymatic kinetics, cell biology, parasitology and pharmacology will be employed. Phosphatidylinositol-4-OH kinase (PI4K), a ubiquitous enzyme in eukaryotes, is responsible for lipid phosphorylation and participates in the regulation of intracellular vesicle signaling and transport. This enzyme was recently described as essential in all phases of the parasite’s cell cycle. In addition, PI4K presents significant differences from the human homologous protein, making it an attractive molecular target for the development of new antimalarials. The project will be developed at the Medicinal and Computational Chemistry Laboratories – LQMC, located at the Center for Innovation in Biodiversity and Pharmaceuticals – CIBFar-CEPID of the Physics Institute of São Carlos-USP. The LQMC-CIBFar laboratories have complete infrastructure to carry out all the steps proposed in this research project.
Jan 2016 — Dec 2018
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