Description
Title: Proteasome Inhibitors with Specific Sites
Abstract: The proteasome is a multi-subunit protein degradation machine that is essential for maintaining protein homeostasis and for controlling a wide range of cellular processes through the degradation of regulatory proteins. Inhibitors of the proteasome are crucial tools for biomedical research. Bortezomib, carfilzomib, and ixazomib are three proteasome inhibitors that have received FDA approval for the treatment of multiple myeloma; marizomib is another inhibitor that is presently undergoing clinical trials. Three pairs of active sites—active sites 5, 2, and 1—make up the proteolytic core of the proteasome. Since they all inhibit multiple active sites, clinical inhibitors and inhibitors that are frequently used in research (like epoxomicin and MG-132) have undergone thorough reviews. Over the past ten years, highly specialized inhibitors of both the unique immunoproteasome active sites specific to lymphoid tissue as well as individual active sites have been created. Here, we present a thorough analysis of these mammalian proteasome site-specific inhibitors and discuss their applications in research on the biology of the active sites as well as their functions as potential drug targets for the treatment of various diseases.
Keywords: ubiquitin-proteasome system; immunoproteasome
Paper Quality: SCOPUS / Web of Science Level Research Paper
Subject: Biomolecules
Writer Experience: 20+ Years
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