Salicylaldehyde (SA) derivatives are emerging as useful fragments to obtain reversible-covalent inhibitors interacting with lysine residues of the target protein. Here we report on the SA installation at the C terminus of an integrin-binding cyclopeptide, leading to enhanced ligand affinity for the receptor as well as stronger biological activity in cultured glioblastoma cells.
RGD cyclopeptide equipped with a lysine-engaging salicylaldehyde shows enhanced integrin affinity and cell detachment potency / G. Sacco, D.A.. - In: CHEMISTRY. - ISSN 1521-3765. - 29:19(2023 Apr 03), pp. e202203768.1-e202203768.8. [10.1002/chem.202203768]
RGD cyclopeptide equipped with a lysine-engaging salicylaldehyde shows enhanced integrin affinity and cell detachment potency
G. SaccoPrimo
;L. Pignataro;L. Belvisi;A. Dal Corso
Penultimo
;C. Gennari
Ultimo
2023
Abstract
Salicylaldehyde (SA) derivatives are emerging as useful fragments to obtain reversible-covalent inhibitors interacting with lysine residues of the target protein. Here we report on the SA installation at the C terminus of an integrin-binding cyclopeptide, leading to enhanced ligand affinity for the receptor as well as stronger biological activity in cultured glioblastoma cells.
| File | Dimensione | Formato | |
|---|---|---|---|
|
chem.202203768.pdf
accesso aperto
Tipologia:
Publisher's version/PDF
Licenza:
Creative commons
Dimensione
6.31 MB
Formato
Adobe PDF
|
6.31 MB | Adobe PDF | Visualizza/Apri |
Pubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
