Journal
JOURNAL OF PEPTIDE SCIENCE
Volume 15, Issue 2, Pages 58-66Publisher
WILEY
DOI: 10.1002/psc.1107
Keywords
proteasome; inhibitors; synthetic and natural products; crystallographic analysis; polyvalency
Funding
- Sonderforschungsbereich 594 (Deutsche Forschungsgemeinschaft) [TP-A11]
Ask authors/readers for more resources
Since the discovery of the proteasome and its structure elucidation intensive research programs in academic institutions and pharmaceutical industries led to identification of a wide spectrum of synthetic and natural small proteasomal inhibitors. Activity studies with these small molecules helped to deeply understand the complex biochemical organization and functioning of the proteasome. The new structural and biochemical insights placed the proteasome as an important anti-cancer drug target, as revealed by the dipeptide boronate proteasome inhibitor, bortezomib, which is currently used for treatment of multiple myeloma. Serious side effects and partial cell resistance against bortezomib demand creation and discovery of new improved generations of more specific and potent proteasomal inhibitors. Copyright (c) 2008 European Peptide Society and John Wiley & Sons, Ltd.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available