Title: Recent Advances in the Identification and Development of 20S Proteasome Inhibitors
VOLUME: 2 ISSUE: 3
Author(s):Carlos Garcia-Echeverria
Affiliation:Oncology Research,Novartis Pharma Inc., CH-4002 Basel, Switzerland
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.
