title: 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.
authors.affiliation: Institute for Advanced Study and Center for Integrated Protein Science, Department of Chemistry, Technische Universität München, Lichtenbergstr. 4, 85747 Garching, Germany.
authors.forename: Tobias G
authors.initials: TG
authors.lastname: Kapp
authors.affiliation: Institute for Advanced Study and Center for Integrated Protein Science, Department of Chemistry, Technische Universität München, Lichtenbergstr. 4, 85747 Garching, Germany.
authors.forename: Florian
authors.initials: F
authors.lastname: Rechenmacher
authors.affiliation: Institute for Advanced Study and Center for Integrated Protein Science, Department of Chemistry, Technische Universität München, Lichtenbergstr. 4, 85747 Garching, Germany.
authors.forename: Stefanie
authors.initials: S
authors.lastname: Neubauer
authors.affiliation: Institute for Advanced Study and Center for Integrated Protein Science, Department of Chemistry, Technische Universität München, Lichtenbergstr. 4, 85747 Garching, Germany.
authors.forename: Oleg V
authors.initials: OV
authors.lastname: Maltsev
authors.affiliation: Max-Planck-Institute for Medical Research, Department of Biointerface Science and Technology, Heidelberg, Postal address: Heisenbergstr. 3, 70 569 Stuttgart, Germany.
authors.forename: Elisabetta A
authors.initials: EA
authors.lastname: Cavalcanti-Adam
authors.affiliation: Department of Molecular Cell Biology, Weizmann Institute of Science, Rehovot, 7610001, Israel.
authors.forename: Revital
authors.initials: R
authors.lastname: Zarka
authors.affiliation: Clinical Research Unit, Department of Obstetrics &Gynecology, Technische Universität München, Ismaninger Strasse 22, 81675 Munich, Germany.
authors.forename: Ute
authors.initials: U
authors.lastname: Reuning
authors.affiliation: Pharmaceutical Radiochemistry, Technische Universität München, Munich, Germany.
authors.forename: Johannes
authors.initials: J
authors.lastname: Notni
authors.affiliation: Pharmaceutical Radiochemistry, Technische Universität München, Munich, Germany.
authors.forename: Hans-Jürgen
authors.initials: HJ
authors.lastname: Wester
authors.affiliation: Biomaterials, Biomechanics and Tissue Engineering Group, Department of Materials Science and Metallurgical Engineering, and Centre for Research in NanoEngineering (CRNE), Technical University of Catalonia, 08028-Barcelona, Spain.
authors.forename: Carlos
authors.initials: C
authors.lastname: Mas-Moruno
authors.affiliation: Max-Planck-Institute for Medical Research, Department of Biointerface Science and Technology, Heidelberg, Postal address: Heisenbergstr. 3, 70 569 Stuttgart, Germany.
authors.forename: Joachim
authors.initials: J
authors.lastname: Spatz
authors.affiliation: Department of Molecular Cell Biology, Weizmann Institute of Science, Rehovot, 7610001, Israel.
authors.forename: Benjamin
authors.initials: B
authors.lastname: Geiger
authors.affiliation: Institute for Advanced Study and Center for Integrated Protein Science, Department of Chemistry, Technische Universität München, Lichtenbergstr. 4, 85747 Garching, Germany.
authors.forename: Horst
authors.initials: H
authors.lastname: Kessler
mesh_terms: D001691:Biological Therapy; D004797:Enzyme-Linked Immunosorbent Assay; D005786:Gene Expression Regulation; D006801:Humans; D056747:Immunomodulation; D020128:Inhibitory Concentration 50; D016023:Integrins / Q000819:agonists / Q000378:metabolism*; D008024:Ligands; D011485:Protein Binding; D011971:Receptors, Immunologic / Q000378:metabolism*; D018000:Receptors, Peptide / Q000378:metabolism*
chemical_list: D016023:Integrins; D008024:Ligands; D011971:Receptors, Immunologic; D018000:Receptors, Peptide; C051382:arginyl-glycyl-aspartic acid directed cell adhesion receptor