The hybrid molecule Quercetin-3-oleate (AV2), accommodates within the binding pocket for allosteric full GPR40 agonists. AV2 endorses skin wound healing acting as a promoter of keratinocytes proliferation and overcomes immunosuppressive conditions in vitro. AV2 stimulated HaCaT wound healing by 51% compared to the untreated control, at the concentration of 1 μM with slight TGF-β production and MMP-9 release. Pretreatment with the known GPR40 antagonist DC260126 abolished its wound healing power. Docking simulations suggested that both molecules share the same binding site.

Quercetin-3-Oleate Contributes to Skin Wound Healing Targeting FFA1/GPR40

Gabriele Carullo;Antonio Leo;Erika Cione;Maria Cristina Caroleo;Francesca Aiello;
2019

Abstract

The hybrid molecule Quercetin-3-oleate (AV2), accommodates within the binding pocket for allosteric full GPR40 agonists. AV2 endorses skin wound healing acting as a promoter of keratinocytes proliferation and overcomes immunosuppressive conditions in vitro. AV2 stimulated HaCaT wound healing by 51% compared to the untreated control, at the concentration of 1 μM with slight TGF-β production and MMP-9 release. Pretreatment with the known GPR40 antagonist DC260126 abolished its wound healing power. Docking simulations suggested that both molecules share the same binding site.
wound healing; GPR40 ligands
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/20.500.11770/295035
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