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
Mini-Reviews in Medicinal Chemistry
Title: Recent Advances in the Identification and Development of 20S Proteasome Inhibitors
Volume: 2 Issue: 3
Author(s): Carlos Garcia-Echeverria
Affiliation:
Keywords: 20s proteasome inhibitor, anti-inflammatory agent
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.
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Cite this article as:
Garcia-Echeverria Carlos, Recent Advances in the Identification and Development of 20S Proteasome Inhibitors, Mini-Reviews in Medicinal Chemistry 2002; 2 (3) . https://dx.doi.org/10.2174/1389557023406142
DOI https://dx.doi.org/10.2174/1389557023406142 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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