Design, synthesis and biological assay of novel tripeptidic tetrazoles as inhibitors of 20S proteasome / 药学学报
Acta Pharmaceutica Sinica
; (12): 472-478, 2012.
Article
in Zh
| WPRIM
| ID: wpr-323017
Responsible library:
WPRO
ABSTRACT
Ubiquitin-proteasome pathway (UPP) is one of the ways utilized for selective degradation of many proteins in cells, and the 20S proteasome takes the functional machinery where hydrolysis of targeted proteins takes place. Based on existing peptide inhibitors, a series of novel tripeptidic tetrazoles have been designed, synthesized, and the structures have been confirmed with 1H NMR, MS and elemental analysis. Among them, three compounds (6b, 6d and 6h) showed inhibitory activities of ChT-L of 20S proteasome.
Full text:
1
Index:
WPRIM
Main subject:
Oligopeptides
/
Pharmacology
/
Tetrazoles
/
Biological Assay
/
Drug Design
/
Molecular Structure
/
Chemistry
/
Proteasome Endopeptidase Complex
/
Proteasome Inhibitors
Language:
Zh
Journal:
Acta Pharmaceutica Sinica
Year:
2012
Type:
Article