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. Arosio, M. Paolillo, A. Gloger, J. Scheuermann, L.L. Pignataro, L. Belvisi, A. DAL CORSO, C.M.A. Gennari. - 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.L. Pignataro;L. Belvisi;A. DAL CORSO
Penultimo
;C.M.A. 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.
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