BIOTEC-NSTDA and FIMECS, Inc. of Japan were recently awarded a THB 27-million grant from The Global Health Innovative Technology (GHIT) Fund to employ a new drug design approach to develop antimalarial drugs to overcome antimalarial drug resistance.
Instead of developing drugs that act as inhibitors of target functions, the new approach is to design drugs based on protein degraders, also known as PROteolysis-TArgeting Chimeras or PROTACs, to destroy target proteins. Protein degraders are designed with one “warhead” that binds the target and another that binds ubiquitin E3 ligase, a protein that marks other proteins for degradation. This approach has the advantage that the protein degraders can bind anywhere on the target, and therefore can be designed against proteins previously not considered as drug targets. PROTAC antimalarials acting on new targets throughout the parasite life cycle could be a game changer in eradicating malaria.
In this project, researchers – led by Dr. Nitipol Srimongkolpithak of BIOTEC Frontier Biodesign and Biomolecular Engineering Research Team - will identify a chemical warhead(s) that can recruit a parasite ubiquitin E3 ligase(s) to degrade a target parasite protein, which will constitute a platform for the design of protein degrader antimalarials.
