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Issue 8, 2011
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Blockage of collagen binding to integrin α2β1: structure–activity relationship of protein–protein 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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Supplementary files

Article information


Submitted
29 Mar 2011
Accepted
20 May 2011
First published
22 Jun 2011

Med. Chem. Commun., 2011,2, 764-770
Article type
Concise Article

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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