Selective Helix-Mimetics as Tools in Malaria Research

Malaria is a debilitating disease caused by parasites transmitted by mosquitoes. It is among the most serious challenges facing the developing world, with an estimated 500 million cases and up to a million deaths, predominantly children, in 2002. Although drug therapies exist, parasite resistance has been recorded for all frontline drugs. The identification of new drug targets and the design of novel drugs to treat malaria are therefore urgently needed and are of significant therapeutic importance. The binding of one protein to another, a protein-protein interaction (PPI), is often a key event in disease development. Such interactions are critically important for both the movement and the ability of malaria parasites to invade host cells. Thus, disruption of the PPIs involved in parasite invasion has the potential to revolutionise the treatment of this disease. Many of these PPIs are mediated by alpha-helices, a structural element of proteins, and thus effective imitation of this structure is a promising strategy for suppressing these binding events. By investigating how these inhibitors affect the parasite’s biology it will be possible to understand better the role of each PPI, facilitating the development of more effective and selective anti-malarial drugs. This concept represents a novel approach to the challenge of treating malaria, and could form a new foundation for future efforts in the field.

Project details

Basic Science
Drug-based Strategies

Oct 2016

$98,231

United Kingdom