Back to Search
Start Over
Mixing of peptides and electrophilic traps gives rise to potent, broad-spectrum proteasome inhibitors.
- Source :
-
Organic & biomolecular chemistry [Org Biomol Chem] 2007 May 07; Vol. 5 (9), pp. 1416-26. Date of Electronic Publication: 2007 Mar 23. - Publication Year :
- 2007
-
Abstract
- The synthesis and evaluation of hybrid proteasome inhibitors that contain structural elements of the known inhibitors bortezomib, epoxomicin and peptide vinyl sulfones is described. From the panel of 15 inhibitors some structure activity relationships can be deduced with regard to inhibitory activity in relation to peptide recognition element, inhibitor size and nature of the electrophilic trap. Further, the panel contains one of the most potent peptide-based pan-proteasome inhibitors reported to date.
- Subjects :
- Cell Line
Drug Evaluation, Preclinical
Enzyme Inhibitors chemistry
Humans
Proteasome Endopeptidase Complex metabolism
Static Electricity
Structure-Activity Relationship
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacology
Peptides chemistry
Peptides pharmacology
Proteasome Inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1477-0520
- Volume :
- 5
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Organic & biomolecular chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 17464411
- Full Text :
- https://doi.org/10.1039/b702268a