Small-Molecule Inhibitors of Haemophilus influenzae IgA1 Protease.

ABSTRACT: Newly identified, nontypable Haemophilus influenzae (H. influenza) strains represent a serious threat to global health. Due to the increasing prevalence of antibiotic resistance, virulence factors have emerged as potential therapeutic targets that would be less likely to promote resistance. IgA1 proteases are secreted virulence factors of many Gram-negative human pathogens. These enzymes play important roles in tissue invasion as well as evasion of the immune response, yet there has been limited work on pharmacological inhibitors. Here, we report the discovery of the first small molecule, nonpeptidic inhibitors of H. influenzae IgA1 proteases. We screened over 47 000 compounds in a biochemical assay using recombinant protease and identified a hit compound with micromol

SUBMITTER: Shehaj L 

PROVIDER: S-EPMC6625846 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature