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Updated: Jan 4, 2026

The Use of a β-lactamase-based Conductimetric Biosensor Assay to Detect Biomolecular Interactions
Published on: February 1, 2018
Could Dissecting the Molecular Framework of β-Lactam Integrin Ligands Enhance Selectivity?
Giulia Martelli1, Monica Baiula2, Alberto Caligiana2
1Department of Chemistry "G. Ciamician" , University of Bologna , Via Selmi 2 , 40126 Bologna , Italy.
Abstract:
By dissecting the structure of β-lactam-based ligands, a new series of compounds was designed, synthesized, and evaluated toward integrins αvβ3, α5β1, and α4β1. New selective ligands with antagonist or agonist activities of cell adhesion in the nanomolar range were obtained. The best agonist molecules induced significant adhesion of SK-MEL-24 cells and Saos-2 cells as a valuable model for osteoblast adhesion. These data could lead to the development of new agents to improve cellular osseointegration and bone regeneration. Molecular modeling studies on prototypic compounds and αvβ3 or α5β1 integrin supported the notion that ligand carboxylate fixing to the metal ion-dependent adhesion site in the β-subunit can be sufficient for binding the receptors, while the aryl side chains play a role in determining the selectivity as well as agonism versus antagonism.
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