A1 Refereed original research article in a scientific journal
Blockage of collagen binding to integrin alpha 2 beta 1: structure-activity relationship of protein-protein interaction inhibitors
Authors: Koivunen JT, Nissinen L, Juhakoski A, Pihlavisto M, Marjamaki A, Huuskonen J, Pentikainen OT
Publisher: ROYAL SOC CHEMISTRY
Publication year: 2011
Journal: MedChemComm
Journal name in source: MEDCHEMCOMM
Journal acronym: MEDCHEMCOMM
Volume: 2
Issue: 8
First page : 764
Last page: 770
Number of pages: 7
ISSN: 2040-2503
DOI: https://doi.org/10.1039/c1md00089f
Abstract
The interaction between the alpha 2 beta 1 integrin and collagen plays a crucial role in the development of pathological conditions, such as thrombus formation and cancer cell metastasis. Accordingly, the alpha 2 beta 1 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 alpha 2 beta 1 integrin and collagen. The obtained structure-activity relationship reveals the key features that are required for successful inhibition of this integrin-collagen interaction.
The interaction between the alpha 2 beta 1 integrin and collagen plays a crucial role in the development of pathological conditions, such as thrombus formation and cancer cell metastasis. Accordingly, the alpha 2 beta 1 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 alpha 2 beta 1 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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