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

MedChemComm Pub Date: 2011-06-22 DOI: 10.1039/C1MD00089F

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 protein–protein 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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