Journal
CURRENT PROTEIN & PEPTIDE SCIENCE
Volume 19, Issue 4, Pages 358-367Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1389203718666170111121856
Keywords
Natural compound; ubiquitin proteasome system; proteasome inhibitor; drug discovery; cancer; clinical trial
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Funding
- Natural Science Foundation of Heilongjiang Province, China [C201432]
- Scientific Research Foundation for the Returned Overseas Chinese Scholars, State Education Ministry
- National Natural Science Foundation of China [81772492/H1615]
- National Cancer Institute [R21CA184788]
- National Institutes of Health [P30 CA022453]
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Natural products serve as a main resource for drug discovery. The ubiquitin-proteasome system (UPS) is one of the primary intracellular protein degradation systems, which is responsible for the degradation of most short-lived, mis-folded and aged proteins. The proteasome is a validated target for cancer treatment, since cancer cells are more reliant on high levels of proteasome activity to maintain the dynamic protein homeostasis required for enhanced metabolism and unrestricted proliferation. Encouraged by success of bortezomib in the treatment of multiple myeloma, several second-generation proteasome inhibitors have been developed based on natural resources, and are being tested in various clinical settings. In this paper, we reviewed the most widely investigated proteasome inhibitors, including their natural product origins, compound-discovery and optimization, as well as their current status in both preclinical and clinical studies.
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