Refereed journal article or data article (A1)
Fluorescent Small Molecule Probe to Modulate and Explore alpha 2 beta 1 Integrin Function
List of Authors: Koivunen JT, Nissinen L, Kapyla J, Jokinen J, Pihlavisto M, Marjamaki A, Heino J, Huuskonen J, Pentikainen OT
Publisher: AMER CHEMICAL SOC
Publication year: 2011
Journal: Journal of the American Chemical Society
Journal name in source: JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Journal acronym: J AM CHEM SOC
Number in series: 37
Volume number: 133
Issue number: 37
Start page: 14558
End page: 14561
Number of pages: 4
ISSN: 0002-7863
DOI: http://dx.doi.org/10.1021/ja206086c
Abstract
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.
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.