Validating targets antiparasitic chemotherapy
The Action aims at uniting scientists with different backgrounds to create synergistic interactions paving the way for antiparasitic drug discovery for diseases caused by protozoa and helminths.The scientific aim is to bundle together the identification and validation of parasite drug targets based on the established genomes, medicinal chemistry including structure-based drug design, crystallography, bioinformatics, and drug targeting using chemical and nanotechnological approaches to improve drug performance.
The differences between protein kinases of a parasite and their homologues in its host cell suggest that specific inhibition of the former can be achieved.Parasitic protozoa infecting humans have a staggering impact on public health, especially in the developing world.Furthermore, several protozoan species are major pathogens of domestic animals and have a considerable impact on food production.Research into parasite PKs has benefited greatly from genome and EST sequencing projects, with the genomes from a few species fully sequenced (notably that from the malaria parasite Plasmodium falciparum) and several more under way, the structural features that are important to design specific inhibitors against these PKs will be reviewed in the present work.Keywords: Apicomplexa; Kinases; crystallography; drug design; parasites Document Type: Research Article DOI: https://doi.org/10.2174/138945007780058979 Affiliations: Universidade Federal de Mato Grosso do Sul - UFMS.Owing to the absence of antiparasitic vaccines and the constant threat of drug resistance, the development of novel antiparasitic chemotherapies remains of major importance for disease control.
A better understanding of drug transport (uptake and efflux), drug metabolism and the identification of drug targets, and mechanisms of drug resistance would facilitate the development of more effective therapies.
Parasitic protozoa infecting humans have a great impact on public health, especially in the developing countries.
In line with the current interest in Protein Kinase (PK) inhibitors as potential drugs against a variety of diseases, the possibility that PKs may represent targets for novel anti-parasitic agents is being explored.
We describe the approaches and technologies that have been influential for each parasite and develop new ideas for future research directions, including mode-of-action studies for drug target deconvolution.
Expected final online publication date for the Annual Review of Pharmacology and Toxicology Volume 54 is January 06, 2014. Division of Biological Chemistry and Drug Discovery, College of Life Scinces, University of Dundee, Dundee, DD1 5EH, United Kingdom; email: [email protected]
Centro de Ciencias Biologicas e da Saude -CCBS-Departamento de Morfofisiologia-Laboratório de Bioquímica, Caixa Postal 549- CEP 79070-900 Campo Grande-MS, Brazil.