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

Author(s): Carlos Garcia-Echeverria.

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 2 , Issue 3 , 2002

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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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Article Details

VOLUME: 2
ISSUE: 3
Year: 2002
Page: [247 - 259]
Pages: 13
DOI: 10.2174/1389557023406142
Price: $58

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