A Comprehensive Evaluation of the Activity and Selectivity Profile of Ligands for RGD-binding Integrins.

Abstract:

:Integrins, a diverse class of heterodimeric cell surface receptors, are key regulators of cell structure and behaviour, affecting cell morphology, proliferation, survival and differentiation. Consequently, mutations in specific integrins, or their deregulated expression, are associated with a variety of diseases. In the last decades, many integrin-specific ligands have been developed and used for modulation of integrin function in medical as well as biophysical studies. The IC50-values reported for these ligands strongly vary and are measured using different cell-based and cell-free systems. A systematic comparison of these values is of high importance for selecting the optimal ligands for given applications. In this study, we evaluate a wide range of ligands for their binding affinity towards the RGD-binding integrins αvβ3, αvβ5, αvβ6, αvβ8, α5β1, αIIbβ3, using homogenous ELISA-like solid phase binding assay.

journal_name

Sci Rep

journal_title

Scientific reports

authors

Kapp TG,Rechenmacher F,Neubauer S,Maltsev OV,Cavalcanti-Adam EA,Zarka R,Reuning U,Notni J,Wester HJ,Mas-Moruno C,Spatz J,Geiger B,Kessler H

doi

10.1038/srep39805

subject

Has Abstract

pub_date

2017-01-11 00:00:00

pages

39805

issn

2045-2322

pii

srep39805

journal_volume

7

pub_type

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