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Proteasome inhibitors for cancer therapy.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2012 Apr 01; Vol. 20 (7), pp. 2362-8. Date of Electronic Publication: 2012 Feb 11. - Publication Year :
- 2012
-
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).<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Boronic Acids pharmacology
Boronic Acids therapeutic use
Cell Line, Tumor
Cell Proliferation drug effects
Drug Screening Assays, Antitumor
Humans
Liver enzymology
Mice
Neoplasms drug therapy
Nitro Compounds pharmacology
Nitro Compounds therapeutic use
Protease Inhibitors pharmacology
Protease Inhibitors therapeutic use
Proteasome Endopeptidase Complex metabolism
Boronic Acids chemistry
Nitro Compounds chemistry
Protease Inhibitors chemistry
Proteasome Inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 20
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 22377673
- Full Text :
- https://doi.org/10.1016/j.bmc.2012.02.007