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Development of Isoxazoline-Containing Peptidomimetics as Dual αvβ3 and α5β1 Integrin Ligands

✍ Scribed by Dr. Alessandra Tolomelli; Prof. Luca Gentilucci; Dr. Elisa Mosconi; Dr. Angelo Viola; Dr. Samantha Deianira Dattoli; Dr. Monica Baiula; Prof. Santi Spampinato; Dr. Laura Belvisi; Dr. Monica Civera

Publisher
John Wiley and Sons
Year
2011
Tongue
English
Weight
544 KB
Volume
6
Category
Article
ISSN
1860-7179

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✦ Synopsis

Abstract

Isoxazoline‐containing peptidomimetics, designed to be effective α~v~β~3~ and α~5~β~1~ integrin ligands, were synthesized through an original procedure involving N,O‐bis(trimethylsilyl)hydroxyamine conjugate addition to alkylidene acetoacetates, followed by intramolecular hemiketalization. To mimic the RGD recognition sequence, basic and acidic terminal appendages were introduced, and the final products were tested in cell adhesion inhibition assays. All the synthesized compounds proved to be excellent ligands for both integrin receptors, and a strong influence on intracellular signaling and phosphorylation pathways was demonstrated by evaluation of fibronectin‐induced phosphorylation of ERK. The molecular basis of the observed inhibitory activity was suggested on the results of docking experiments.

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