Proteasome inhibitors: from research tools to drug candidates.

Chemistry & biology ·Vol. 8 ·No. 8 ·2001-08-00 ·Pages 739-58

Kisselev AF, Goldberg AL

Abstract

The 26S proteasome is a 2.4 MDa multifunctional ATP-dependent proteolytic complex, which degrades the majority of cellular polypeptides by an unusual enzyme mechanism. Several groups of proteasome inhibitors have been developed and are now widely used as research tools to study the role of the ubiquitin-proteasome pathway in various cellular processes, and two inhibitors are now in clinical trials for treatment of multiple cancers and stroke.

Keywords

Non-programmatic

MeSH Terms

Animals Anti-HIV Agents/chemistry,metabolism,therapeutic use Anti-Inflammatory Agents/chemistry,metabolism,therapeutic use Antineoplastic Agents/chemistry,metabolism,therapeutic use Binding Sites Catalysis Humans Models, Molecular Multienzyme Complexes/metabolism Peptide Hydrolases/metabolism Protease Inhibitors/chemistry,classification,metabolism,therapeutic use Proteasome Endopeptidase Complex Protein Structure, Quaternary Protein Subunits Ubiquitin/metabolism

Chemicals

Anti-HIV Agents Anti-Inflammatory Agents Antineoplastic Agents Multienzyme Complexes Protease Inhibitors Protein Subunits Ubiquitin Peptide Hydrolases Proteasome Endopeptidase Complex ATP dependent 26S protease

Authors & Affiliations

2 authors, click to expand affiliations / ORCID

Kisselev A F

Department of Cell Biology, Harvard Medical School, 240 Longwood Ave., Boston, MA 02115, USA. alexei_kisselev@hms.harvard.edu

Goldberg A L

Article Info

Journal

Chemistry & biology

Abbr.

Chem Biol

ISSN

1074-5521

DOI

10.1016/s1074-5521(01)00056-4

alexei_kisselev@hms.harvard.edu

Published

2001-08-00

Pages

739-58

Language

English

Region

United States

NLM ID

9500160

Subset

External Links

PubMed source DOI: 10.1016/s1074-5521(01)00056-4 View journal details

Analysis Services

Proteasome inhibitors: from research tools to drug candidates.

Contact

WeChat Official Account