Activity-based chemoproteomic profiling reveals the active kinome of <i>Leishmania</i>.

ABSTRACT:

Background

Leishmania parasites cause neglected tropical diseases such as cutaneous and visceral leishmaniasis, which have limited treatment options and rising drug resistance. Protein kinases are pivotal in Leishmania biology and attractive drug targets, but their functional status in the parasite remains largely unexplored.

Methods

We applied activity-based protein profiling (ABPP) with custom in-house cell-permeable ATP-site directed probes to map the ligandable, "active kinome" of Leishmania mexicana. Three related covalent probes featuring an ATP-mimetic scaffold, electrophilic warhead (targeting catalytic lysines or cysteines), and alkyne tag were synthesised to broadly capture active kinases. Live parasites were labelled with probes, followed by c

SUBMITTER: Porta EOJ 

PROVIDER: S-EPMC12816314 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature