A1 Refereed original research article in a scientific journal
Blockage of Collagen Binding to Integrin alpha2beta1: Structure-activity Relationships of Protein-protein Interaction Inhibitors
Authors: Koivunen JT, Nissinen L, Juhakoski A, Pihlavisto M, Marjamäki A, Huuskonen J, Pentikäinen OT
Publication year: 2011
Journal: MedChemComm
Volume: 2
First page : 764
Last page: 770
The interaction between the alpha2beta1
integrin and collagen plays a crucial role in the development of pathological
conditions, such as thrombus formation and cancer cell metastasis. Accordingly,
the alpha2beta1 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 protein–protein
interactions between alpha2beta1 integrin and collagen. The obtained
structure–activity relationship reveals the key features that are required for
successful inhibition of this integrin–collagen interaction.
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