Drug-resistant malaria to be treated by proteasome inhibitors

proteasome inhibitors

A new study published in the Journal PLOS Pathogens shares insights into the significant promise of Proteasome inhibitors in the treatment of multidrug-resistant malaria. According to the study, Proteasome inhibitors consist of components with a novel combination which helps in treating the disease.

The growing spread of drug-resistant malaria had involved scientists in drawing efforts towards developing vital options with compounds that are not receptive to the current mechanisms of antimalarial drug resistance. Malaria is caused due to protozoan parasite Plasmodium falciparum and is widely affecting the population of Southeast Asia.

Based on recent findings, the P. falciparum proteasome, a protein complex, is capable of degrading damaged and superfluous proteins. As basis for the study, experts have characterized antimalarial activity of two P. falciparum-selective proteasome inhibitors viz. the covalent peptide vinyl sulfones WLL-vs (WLL) and WLW-vs (WLW).

According to reports, the inhibitors showcased potent antimalarial activity against drug-resistant- P. falciparum among parasites belonging to the early ring stage, which are known to be difficult to treat. Furthermore, it was observed that the parasites were cross-resistant to both the compounds. Additionally, partial resistance to one compound led to hypersensitivity among the other.

According to reports, the data was elucidated on the basis of activity-based profiling of molecular modeling and proteasome complex, in connection with its interactions with the inhibitors.

Results also concluded potent synergy between multiple and chemically varied classes of antimalarial agents and proteasome inhibitors. On basis of the results, it was observed that an underscore of potential targeting of Plasmodium proteasome with small molecule inhibitors is a medium to combat multidrug-resistant malaria.