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 / Carullo, Gabriele; Governa, Paolo; Leo, Antonio; Gallelli, Luca; Citraro, Rita; Cione, Erika; Caroleo, Maria Cristina; Biagi, Marco; Aiello, Francesca; Manetti, Fabrizio. - In: CHEMISTRYSELECT. - ISSN 2365-6549. - 4:29(2019), pp. 8429-8433. [10.1002/slct.201902572]

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

Biagi, Marco;
2019-01-01

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.
2019
Quercetin‐3‐Oleate Contributes to Skin Wound Healing Targeting FFA1/GPR40 / Carullo, Gabriele; Governa, Paolo; Leo, Antonio; Gallelli, Luca; Citraro, Rita; Cione, Erika; Caroleo, Maria Cristina; Biagi, Marco; Aiello, Francesca; Manetti, Fabrizio. - In: CHEMISTRYSELECT. - ISSN 2365-6549. - 4:29(2019), pp. 8429-8433. [10.1002/slct.201902572]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11381/2960893
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