Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 58, Issue 43, Pages 15421-15428Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201905790
Keywords
diazocines; GIRK channels; photopharmacology; photoswitchable molecules; potassium channels
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Funding
- Danish National Research Foundation Center for DNA Nanotechnology [DNRF81]
- Aarhus University, Faculty of Science and Technology
- Studienstiftung des deutschen Volkes
- Alexander von Humboldt Foundation
- Deutsche Forschungsgemeinschaft [SFB1116, TPA01]
- European Commission [PIEF-GA-2013-627990]
- European Research Council [268795]
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Photopharmacology relies on ligands that change their pharmacodynamics upon photoisomerization. Many of these ligands are azobenzenes that are thermodynamically more stable in their elongated trans-configuration. Often, they are biologically active in this form and lose activity upon irradiation and photoisomerization to their cis-isomer. Recently, cyclic azobenzenes, so-called diazocines, have emerged, which are thermodynamically more stable in their bent cis-form. Incorporation of these switches into a variety of photopharmaceuticals could convert dark-active ligands into dark-inactive ligands, which is preferred in most biological applications. This pharmacological sign-inversion is demonstrated for a photochromic blocker of voltage-gated potassium channels, termed CAL, and a photochromic opener of G protein-coupled inwardly rectifying potassium (GIRK) channels, termed CLOGO.
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