Rhomboid intramembrane proteases regulate pathophysiological processes, yet their targeting in a disease context has never been achieved.
Scientists from the groups of Kvido Stříšovský and Pavel Majer at IOCB Prague in collaboration with scientists from Johns Hopkins University have shown that inhibition of a rhomboid protease of the malaria parasite Plasmodium by peptidyl ketoamides potently inhibits parasite invasion and clears blood-stage malaria.
These findings establish a strategy for designing parasite-selective rhomboid inhibitors and expose a druggable dependence on rhomboid proteolysis in non-motile parasites.
Read the paper:
- Gandhi, S., Baker, R.P., Cho, S., Stanchev, S., Strisovsky, K., Urban, S., Designed Parasite-Selective Rhomboid Inhibitors Block Invasion and Clear Blood-Stage Malaria, Cell Chemical Biology 2020. https://doi.org/10.1016/j.chembiol.2020.08.011
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