1449280-96-9Relevant academic research and scientific papers
Modulation of αvβ3- and α5β1-integrin-mediated adhesion by dehydro-β-amino acids containing peptidomimetics
Tolomelli, Alessandra,Baiula, Monica,Belvisi, Laura,Viola, Angelo,Gentilucci, Luca,Troisi, Stefano,Dattoli, Samantha Deianira,Spampinato, Santi,Civera, Monica,Juaristi, Eusebio,Escudero, Margarita
, p. 258 - 268 (2013/10/01)
A novel class of low molecular weight ligands of αvβ 3 and α5β1 integrins, that possess a dehydro-β-amino acid as conformationally constrained core, linked to the pharmacophoric moieties mimicking the RGD recognition sequence, have been synthesized through a very simple protocol. Cell adhesion assays and integrin-mediated signaling activation experiments suggested a good affinity of these compounds toward both integrin receptors. Moreover, further elongation with two glycine units allowed to obtain an excellent dual inhibitor. Structural models for αvβ3 integrin-ligand binding con firmed that the dehydro-β-amino derivatives are able to act as an electrostatic clamp by establishing several stabilizing interactions with the receptor.
