Journal of the American Chemical Society, Vol.133, No.37, 14558-14561, 2011
Fluorescent Small Molecule Probe to Modulate and Explore alpha 2 beta 1 Integrin Function
Collagen binding integrins are an important family of cell surface receptors that mediate bidirectionally signals between the interior of the cell and the extracellular matrix. The protein-protein interactions between cells and collagen are necessary for many physiological functions, but also promote diseases. For example, the interaction of alpha 2 beta 1 integrin and collagen has been shown to have an important role in thrombus formation and cancer spread. The fact that the discovery of small molecules that can block such protein-protein interactions is highly challenging has significantly hindered the discovery of pharmaceutical agents to treat these diseases. Here, we present a rationally designed novel fluorescent molecule that can be synthesized in just a few minutes from commercially available starting materials. This molecule blocks the protein-protein interaction between alpha 2 beta 1 integrin and collagen, and due to its fluorescent properties, it can be employed in wide variety of biological applications.