C-terminal constrained phenylalanine as a pharmacophoric unit in peptide-based proteasome inhibitors

Baldisserotto, A.; Marastoni, M.; Lazzari, I.; Trapella, C.; Gavioli, R.; Tomatis, R.

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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.

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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11392/499064

Titolo:	C-terminal constrained phenylalanine as a pharmacophoric unit in peptide-based proteasome inhibitors
Autori interni:	BALDISSEROTTO, Anna MARASTONI, Mauro LAZZARI, Ilaria TRAPELLA, Claudio GAVIOLI, Riccardo TOMATIS, Roberto
Data di pubblicazione:	2008
Rivista:	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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.
Handle:	http://hdl.handle.net/11392/499064
Appare nelle tipologie:	03.1 Articolo su rivista

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