Fluorescent Small Molecule Probe to Modulate and Explore alpha 2 beta 1 Integrin Function

: Koivunen JT, Nissinen L, Kapyla J, Jokinen J, Pihlavisto M, Marjamaki A, Heino J, Huuskonen J, Pentikainen OT

Publisher: AMER CHEMICAL SOC

: 2011

: JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

: J AM CHEM SOC

: 37

: 133

: 37

: 14558

: 14561

: 4

: 0002-7863

DOI: https://doi.org/10.1021/ja206086c

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.