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Morstein, Johannes; Trads, Julie B.; Hinnah, Konstantin; Willems, Sabine; Barber, David M.; Trauner, Michael; Merk, Daniel and Trauner, Dirk (2020): Optical control of the nuclear bile acid receptor FXR with a photohormone. In: Chemical Science, Vol. 11, No. 2: pp. 429-434

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Abstract

Herein, we report a photoswitchable modulator for a nuclear hormone receptor that exerts its hormonal effects in a light-dependent fashion. The azobenzene AzoGW enables optical control of the farnesoid X receptor (FXR), a key regulator of hepatic bile acid, lipid and glucose metabolism. AzoGW was derived from the synthetic agonist GW4064 through an azologization strategy and is a metabolically stable, highly selective photoswitchable FXR agonist in its dark-adapted form. Upon irradiation, the thermally bistable 'photohormone' becomes significantly less active. Optical control of FXR was demonstrated in a luminescence reporter gene assay and through light-dependent reversible transcription modulation of FXR target genes (CYP7A1, Ost alpha, Ost beta) in liver cells.

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