Optical control of the nuclear bile acid receptor FXR with a photohormone†,Chemical Science

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Optical control of the nuclear bile acid receptor FXR with a photohormone†
Chemical Science ( IF 9.969 ) Pub Date : 2023-02-15 , DOI: 10.1039/c9sc02911g
Johannes Morstein, Julie B. Trads, Konstantin Hinnah, Sabine Willems, David M. Barber, Michael Trauner, Daniel Merk, Dirk Trauner

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, Ostα, Ostβ) in liver cells.

更新日期：2020-01-02

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