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.
Carullo, G., Governa, P., Leo, A., Gallelli, L., Citraro, R., Cione, E., et al. (2019). Quercetin‐3‐Oleate Contributes to Skin Wound Healing Targeting FFA1/GPR40. CHEMISTRYSELECT, 4(29), 8429-8433 [10.1002/slct.201902572].
Quercetin‐3‐Oleate Contributes to Skin Wound Healing Targeting FFA1/GPR40
Carullo, GabrieleMethodology
;Governa, PaoloInvestigation
;Biagi, MarcoMethodology
;Manetti, FabrizioConceptualization
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.
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https://hdl.handle.net/11365/1078436