Blockage of collagen binding to integrin alpha 2 beta 1: structure-activity relationship of protein-protein interaction inhibitors

: Koivunen JT, Nissinen L, Juhakoski A, Pihlavisto M, Marjamaki A, Huuskonen J, Pentikainen OT

Publisher: ROYAL SOC CHEMISTRY

: 2011

: MedChemComm

: MEDCHEMCOMM

: 2

: 8

: 764

: 770

: 7

: 2040-2503

DOI: https://doi.org/10.1039/c1md00089f

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.