García-Echeverría Carlos
Oncology Research, Novartis Pharma Inc., Basel, CH-4002, Switzerland.
Mini Rev Med Chem. 2002 Jun;2(3):247-59. doi: 10.2174/1389557023406142.
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 non-specific 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.
