Inhibitors of the 20S proteasome β5 subunit as potent and selective agents against <i>Trichomonas vaginalis</i>.

ABSTRACT: Trichomonas vaginalis is the causative agent of the most prevalent, non-viral sexually transmitted infectious disease, yet treatment options are limited to three nitroheterocyclic antimicrobials of the same drug class, and resistance to these agents is a manifest clinical problem. The 20S proteasome is a validated new drug target against T. vaginalis, but inhibitors of the proteasome complex have so far only shown modest selectivity over human cells. We screened a library of 373 diverse peptide inhibitors with different reactive warheads against diverse T. vaginalis strains in a growth and survival assay and identified several compounds with potencies in the 10-20 nM range. Notably, these compounds were up to 200-fold selective for T. vaginalis over mammalian ce

SUBMITTER: Miyamoto Y 

PROVIDER: S-EPMC12691669 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature