Novel Nucleus-Oriented Quenched Activity-Based Probes Link Cathepsin Nuclear Localization with Mitosis.

ABSTRACT: Cysteine cathepsins are important proteases that are highly upregulated in cancers and other diseases. While their reported location is mostly endolysosomal, some evidence shows their nuclear localization and involvement in the cell cycle. We aim to generate tools to investigate the involvement of cathepsins in the cell cycle progression. To investigate nuclear cathepsin activity, we designed nucleus-directed quenched activity-based probes (qABPs) by attaching cell-penetrating peptides (CPPs). qABPs are active-site-directed compounds that enable direct real-time monitoring of enzyme activity by the covalent linkage between the probe and the enzyme's active site. Biochemical evaluation of the CPP-qABPs showed potent and selective probes; cell fractionation, multimodal flow cytometry-imaging

SUBMITTER: Shannon KR 

PROVIDER: S-EPMC11877631 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature