Deconvolution of the On-Target Activity of Plasmepsin V Peptidomimetics in <i>Plasmodium falciparum</i> Parasites.

ABSTRACT: Plasmepsin V (PMV), an essential aspartyl protease, plays a critical role during the asexual blood stage of infection of Plasmodium by enabling the export of parasite proteins into the host red blood cell. This export is vital for parasite survival and pathogenesis, making PMV an attractive target for antimalarial drug development. Peptidomimetic inhibitors designed to mimic the natural substrate of PMV have demonstrated potent parasite-killing activity by blocking protein export. While these compounds have been instrumental in validating PMV as a bona fide antimalarial target, inconsistencies between their biochemical potency and cellular activity have raised questions regarding their precise mechanism of action. In this study, we employed chemoproteomic approaches, includin

SUBMITTER: Su W 

PROVIDER: S-EPMC12706786 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature