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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Recent Advances in the Identification and Development of 20S Proteasome Inhibitors

Author(s): Carlos Garcia-Echeverria

Volume 2, Issue 3, 2002

Page: [247 - 259] Pages: 13

DOI: 10.2174/1389557023406142

Price: $65

Abstract

The involvement of the 20S proteasome in the degradation of critical intracellular regulatory proteins has suggested the potential use of proteasome inhibitors as novel anti-inflammatory agents and for the treatment of cancer and auto-immune diseases. Early inhibitors of the 20S proteasome were relatively nonspecific compounds and used for in vitro studies of the ubiquitin / proteasome-dependent degradation pathway. The inherent drawbacks of these inhibitors (e.g., non-target specific, too reactive or unstable) has prompted medicinal chemists to search for alternative subunit-specific proteasome inhibitors. This manuscript summarises recent salient medicinal chemistry achievements in this area of research.

Keywords: 20s proteasome inhibitor, anti-inflammatory agent


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