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EnglishHere we report the synthesis and biological properties of peptide-based molecules bearing constrained analogues of phenylalanine at the C-terminal. Compounds were tested as proteasome subunits' inhibitors. Dehydro-peptides showed good inhibition, in particular against trypsin-like (T-L) proteasome activity while some C-terminal Tic-derivatives inhibit only caspase-like activity in enzymatic beta1 subunits with a certain degree of efficacy. The best analogues of the series demonstrated good resistance to proteolysis and a capacity to permeate the cell membrane.
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| Data di pubblicazione: | 2008 | |
| Titolo: | C-terminal constrained phenylalanine as a pharmacophoric unit in peptide-based proteasome inhibitors | |
| Autori: | BALDISSEROTTO A.; MARASTONI M.; LAZZARI I.; TRAPELLA C.; GAVIOLI R.; TOMATIS R. | |
| Rivista: | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | |
| Parole Chiave: | Constrained phenylalanine analogues; Synthesis; Pseudopeptides; Proteasome inhibition | |
| Abstract: | Here we report the synthesis and biological properties of peptide-based molecules bearing constrained analogues of phenylalanine at the C-terminal. Compounds were tested as proteasome subunits' inhibitors. Dehydro-peptides showed good inhibition, in particular against trypsin-like (T-L) proteasome activity while some C-terminal Tic-derivatives inhibit only caspase-like activity in enzymatic beta1 subunits with a certain degree of efficacy. The best analogues of the series demonstrated good resistance to proteolysis and a capacity to permeate the cell membrane. | |
| Digital Object Identifier (DOI): | 10.1016/j.ejmech.2007.10.002 | |
| Handle: | http://hdl.handle.net/11392/499064 | |
| Appare nelle tipologie: | 03.1 Articolo su rivista |
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