Synthesis and Application of a Versatile Immunoproteasome Activity Probe.

Autor: Halder S; Purdue University, Chemistry, UNITED STATES OF AMERICA., Loy CA; University of California Irvine, Pharmaceutical Sciences, UNITED STATES OF AMERICA., Trader DJ; University of California Irvine, Department of Pharmaceutical Sciences, 856 Health Sciences Rd, 92617, Irvine, UNITED STATES OF AMERICA.
Jazyk: angličtina
Zdroj: Chembiochem : a European journal of chemical biology [Chembiochem] 2024 Oct 04, pp. e202400571. Date of Electronic Publication: 2024 Oct 04.
DOI: 10.1002/cbic.202400571
Abstrakt: The immunoproteasome (iCP) has gained significant interest in recent years as it has been discovered to be significantly expressed under inflammatory conditions, as well as playing significant roles in several diseases, such as autoimmune disorders, viral infection, and cancer. Selective inhibitors have been generated as a method to overcome the off-target effects of current proteasome inhibitor therapeutics. However, selective probes that allow for monitoring this protein complex remain limited, hindering our understanding of the iCP. Current probes are non-selective, not commercially available, or require difficult synthesis. Here, we describe the modular synthesis and application of an iCP-selective probe. The modular nature of the synthetic strategy can enable the incorporation of different fluorophores and covalent warheads, demonstrating the versatility of this probe.
(© 2024 Wiley‐VCH GmbH.)
Databáze: MEDLINE
Externí odkaz: