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 IC 50 -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…

• DF
  Deutsche Forschungsgemeinschaft
• TU
  Technische Universität München
• IG
  International Graduate School of Science and Engineering