Discovery of <i>Leishmania</i> Druggable Serine Proteases by Activity-Based Protein Profiling.

ABSTRACT: Leishmaniasis are a group of diseases caused by parasitic protozoa of the genus Leishmania. Current treatments are limited by difficult administration, high cost, poor efficacy, toxicity, and growing resistance. New agents, with new mechanisms of action, are urgently needed to treat the disease. Although extensively studied in other organisms, serine proteases (SPs) have not been widely explored as antileishmanial drug targets. Herein, we report for the first time an activity-based protein profiling (ABPP) strategy to investigate new therapeutic targets within the SPs of the Leishmania parasites. Active-site directed fluorophosphonate probes (rhodamine and biotin-conjugated) were used for the detection and identification of active Leishmania serine hydrolases (SHs). Si

SUBMITTER: Porta EOJ 

PROVIDER: S-EPMC9335491 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature