title: Advances in and applications of proteasome inhibitors.
abstract: With the recent US Food and Drug Administration approval of bortezomib (Velcade) for the treatment of relapsed multiple myeloma, the proteasome has emerged as a new therapeutic target with diverse pathology. Drug discovery programs in academia and the pharmaceutical industry have developed a range of low nanomolar synthetic and natural inhibitors of the 20S proteasome core particle that have entered human clinical trials as significant anti-cancer and anti-inflammatory leads. Moreover, proteasome inhibitors continue to serve as valuable research tools in cellular biology through the elucidation of important biological processes associated with the ubiquitin-proteasome pathway of protein degradation. This review will highlight recent advances in the development and application of proteasome inhibitors.
authors.affiliation: Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California at San Diego, La Jolla, CA 92093, USA. bsmoore@ucsd.edu
authors.forename: Bradley S
authors.initials: BS
authors.lastname: Moore
authors.forename: Alessandra S
authors.initials: AS
authors.lastname: Eustáquio
authors.forename: Ryan P
authors.initials: RP
authors.lastname: McGlinchey
mesh_terms: D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D006801:Humans; D061988:Proteasome Inhibitors
chemical_list: D004791:Enzyme Inhibitors; D061988:Proteasome Inhibitors