Solid-Phase Synthesis and Application of a Clickable Version of Epoxomicin for Proteasome Activity Analysis.

ABSTRACT: Degradation of proteins by the proteasome is an essential cellular process and one that many wish to study in a variety of disease types. There are commercially available probes that can monitor proteasome activity in cells, but they typically contain common fluorophores that limit their simultaneous use with other activity-based probes. In order to exchange the fluorophore or incorporate an enrichment tag, the proteasome probe likely has to be synthesized which can be cumbersome. Here, we describe a simple synthetic procedure that only requires one purification step to generate epoxomicin, a selective proteasome inhibitor, with a terminal alkyne. Through a copper-catalyzed cycloaddition, any moiety containing an azide can be incorporated into the probe. Many fluorophores are commercially

SUBMITTER: Salazar-Chaparro AF 

PROVIDER: S-EPMC9122039 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature