Research programme

Drug discovery

The drug discovery programme is the main focus of SAMI activities. The objective of the programme is the discovery and pre-clinical development of novel antimalarial drugs. Two parallel approaches are being pursued: a target to lead and lead to target approach.

Target to lead approach: This approach aims to identify, characterize, and validate novel potential drug targets (essential parasite molecules and pathways). The goal is to discover or rationally design and synthesize novel lead compounds that inhibit parasite growth and survival. Researchers involved in this programme include molecular biologists, microbiologists, biochemists, pharmacologists, bioinformaticians, and medicinal chemists.

Lead to target approach: In this approach, chemical compounds of natural or synthetic origin are selected and screened for antimalarial activity, followed by elucidation and validation of their mode of action using functional genomics approaches. The biological activity of selected compounds is being optimized through investigation of structure-activity relationships (SARs). Researchers involved in this programme include bioinformaticians, medicinal chemists, parasitologists, and biochemists.

Current SAMI Research projects:

- Exploiting the utilisation of coenzyme A and pantothenate by the malaria parasite P. falciparum as an antimalarial drug target

- Novel antimalarial agents targeting Plasmodium falciparum spermidine synthase by way of rational-based drug design

- Plasmodium falciparum GTP cyclohydrolase I (PfGCHI): Optimisation of purification and activity, structure determination and inhibition studies

- Quinoline and non-quinoline haemozoin inhibitors that circumvent chloroquine resistance

- Signalling pathways controlling the cell cycle of Plasmodium falciparum as antimalarial drug target

- Structure-based drug discovery against a novel antimalarial drug target, AdoMetDC/ODC