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J Am Chem Soc ; 133(37): 14558-61, 2011 Sep 21.
Artigo em Inglês | MEDLINE | ID: mdl-21863823

RESUMO

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 α2ß1 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 α2ß1 integrin and collagen, and due to its fluorescent properties, it can be employed in wide variety of biological applications.


Assuntos
Corantes Fluorescentes/metabolismo , Integrina alfa2beta1/metabolismo , Sítios de Ligação , Colágeno/metabolismo , Corantes Fluorescentes/química , Humanos , Integrina alfa2beta1/química , Modelos Moleculares , Ligação Proteica , Espectrometria de Fluorescência
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