WIPO Fellowship - Probing the ubiquitination system as a target for developing new anti-malarials

Status
Completed
Start date
End date
Start stage
Discovery

During her fellowship at the University of Melbourne with the host scientists Leanne Tilley and Matthew Dixon, Tahmina Ahmed from the International Center for Diarrheal Disease Research in Bangladesh (iccdr,b) investigated the antimalarial activity of two novel antimalarial compounds inhibitors. The compounds have been shown to have activity against enzymes that activate ubiquitin and ubiquitin-like proteins. Ms. Ahmed measured the anti-malarial activities of these drugs. This project investigated two drug candidates. Compound 1 proved more potent than chloroquine (IC50 59 nM) and artemisinin (IC50 4 nM). Antimalarial drugs that inhibit apicoplast biogenesis exhibit a delayed death mechanism of killing, however, both compounds 1 and 2 kill parasites rapidly.