@article{9e5d4fd16cf64ddda22d507f94d559f5,
title = "Optical control of the nuclear bile acid receptor FXR with a photohormone",
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, Ostα, Ostβ) in liver cells.",
author = "Johannes Morstein and Trads, {Julie B.} and Konstantin Hinnah and Sabine Willems and Barber, {David M.} and Michael Trauner and Daniel Merk and Dirk Trauner",
note = "Funding Information: J. M. and K. H. thank the German Academic Scholarship Foundation for a fellowship and J. M. thanks the New York University for a MacCracken fellowship and a Margaret and Herman Sokol fellowship. J. B. T. thanks the Danish National Research Foundation Center for DNA Nanotechnology (DNRF81) and Aarhus University for nancial support. D. M. B. thanks the European Commission for a Marie Sk{\l}odowska-Curie Intra-European Fellowship (PIEF-GA-2013-627990). We thank Dr Julia Ast, Dr David Hodson, and Dr Thierry Claudel for experimental support in the initial stages of the project and helpful discussion. We thank Dr Christian Fischer, Christopher J. Arp, Grace Pan and Alan Liu for insightful discussion and proofreading of the manuscript. Publisher Copyright: {\textcopyright} 2020 The Royal Society of Chemistry.",
year = "2020",
doi = "10.1039/c9sc02911g",
language = "English (US)",
volume = "11",
pages = "429--434",
journal = "Chemical Science",
issn = "2041-6520",
publisher = "Royal Society of Chemistry",
number = "2",
}