title: A photochromic agonist for μ-opioid receptors.
abstract: Opioid receptors (ORs) are widely distributed in the brain, the spinal cord, and the digestive tract and play an important role in nociception. All known ORs are G-protein-coupled receptors (GPCRs) of family A. Another well-known member of this family, rhodopsin, is activated by light through the cis/trans isomerization of a covalently bound chromophore, retinal. We now show how an OR can be combined with a synthetic azobenzene photoswitch to gain light sensitivity. Our work extends the reach of photopharmacology and outlines a general strategy for converting Family A GPCRs, which account for the majority of drug targets, into photoreceptors.
authors: Department of Chemistry, Ludwig-Maximilians-University (LMU) Munich and Center of Integrated Protein Science, Butenandtstrasse 5-13, 81377 Munich (Germany).
authors: Matthias
authors: M
authors: Schönberger
authors: Dirk
authors: D
authors: Trauner
mesh_terms: D001391:Azo Compounds / Q000737:chemistry*; D010786:Photoreceptor Cells / Q000378:metabolism*; D011485:Protein Binding; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu / Q000378:metabolism*
chemical_list: D001391:Azo Compounds; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu; C009850:azobenzene
keywords: azobenzenes; fentanyl; opioid receptors; photopharmacology; photoswitches