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Issue 8, 2011
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Blockage of collagen binding to integrin α2β1: structure–activity relationship of proteinprotein interaction inhibitors

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Abstract

The interaction between the α2β1 integrin and collagen plays a crucial role in the development of pathological conditions, such as thrombus formation and cancer cell metastasis. Accordingly, the α2β1 integrin is a promising target for the development of new drug molecules to treat these diseases. Here, we have designed, synthesized, and measured in vitro a set of novel drug-like compounds that block the proteinprotein interactions between α2β1 integrin and collagen. The obtained structure–activity relationship reveals the key features that are required for successful inhibition of this integrin–collagen interaction.

Graphical abstract: Blockage of collagen binding to integrin α2β1: structure–activity relationship of protein–protein interaction inhibitors

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Publication details

The article was received on 29 Mar 2011, accepted on 20 May 2011 and first published on 22 Jun 2011


Article type: Concise Article
DOI: 10.1039/C1MD00089F
Citation: Med. Chem. Commun., 2011,2, 764-770
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    Blockage of collagen binding to integrin α2β1: structure–activity relationship of proteinprotein interaction inhibitors

    J. T. Koivunen, L. Nissinen, A. Juhakoski, M. Pihlavisto, A. Marjamäki, J. Huuskonen and O. T. Pentikäinen, Med. Chem. Commun., 2011, 2, 764
    DOI: 10.1039/C1MD00089F

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