title: Proteasome inhibitors for cancer therapy.
abstract: Proteasome, a large multicatalytic proteinase complex that plays an important role in processing of proteins, has been shown to possess multiple catalytic activities. Among its various activities, the 'chymotrypsin-like' activity of proteasome has emerged as the focus of drug discovery efforts in cancer therapy. Herein we report chiral boronate derived novel, potent, selective and cell-permeable peptidomimetic inhibitors 6 and 7 that displayed activity against various rodent and human tumor cell lines (in vitro).
authors.affiliation: Cephalon Inc., 145 Brandywine Parkway, West Chester, PA 19380, United States.
authors.forename: Mohamed
authors.initials: M
authors.lastname: Iqbal
authors.forename: Patricia A
authors.initials: PA
authors.lastname: Messina McLaughlin
authors.forename: Derek
authors.initials: D
authors.lastname: Dunn
authors.forename: Satish
authors.initials: S
authors.lastname: Mallya
authors.forename: Jean
authors.initials: J
authors.lastname: Husten
authors.forename: Mark A
authors.initials: MA
authors.lastname: Ator
authors.forename: Sankar
authors.initials: S
authors.lastname: Chatterjee
mesh_terms: D000818:Animals; D001897:Boronic Acids / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008099:Liver / Q000201:enzymology; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy; D009574:Nitro Compounds / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D011480:Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism; D061988:Proteasome Inhibitors
chemical_list: D001897:Boronic Acids; D009574:Nitro Compounds; D011480:Protease Inhibitors; D061988:Proteasome Inhibitors; D046988:Proteasome Endopeptidase Complex