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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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Carullo et al. (2019) studied this question.
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