title: Fluorescent small molecule probe to modulate and explore α2β1 integrin function.
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 α2β1 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 α2β1 integrin and collagen, and due to its fluorescent properties, it can be employed in wide variety of biological applications.
authors.affiliation: Computational Bioscience Laboratory, Department of Biological and Environmental Science, University of Jyväskylä, Finland.
authors.forename: Jarkko T
authors.initials: JT
authors.lastname: Koivunen
authors.forename: Liisa
authors.initials: L
authors.lastname: Nissinen
authors.forename: Jarmo
authors.initials: J
authors.lastname: Käpylä
authors.forename: Johanna
authors.initials: J
authors.lastname: Jokinen
authors.forename: Marjo
authors.initials: M
authors.lastname: Pihlavisto
authors.forename: Anne
authors.initials: A
authors.lastname: Marjamäki
authors.forename: Jyrki
authors.initials: J
authors.lastname: Heino
authors.forename: Juhani
authors.initials: J
authors.lastname: Huuskonen
authors.forename: Olli T
authors.initials: OT
authors.lastname: Pentikäinen
mesh_terms: D001665:Binding Sites; D003094:Collagen / Q000378:metabolism; D005456:Fluorescent Dyes / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D038982:Integrin alpha2beta1 / Q000737:chemistry / Q000378:metabolism*; D008958:Models, Molecular; D011485:Protein Binding; D013050:Spectrometry, Fluorescence
chemical_list: D005456:Fluorescent Dyes; D038982:Integrin alpha2beta1; D003094:Collagen