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

Author: Garcia-Echeverria C.

Source: Mini Reviews in Medicinal Chemistry, Volume 2, Number 3, June 2002 , pp. 247-259(13)

Publisher: Bentham Science Publishers

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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

Language: English

Document Type: Review article

DOI: 10.2174/1389557023406142

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