Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 56, Issue 25, Pages 7282-7287Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201701524
Keywords
acetylcholine receptors; azobenzenes; dualsteric ligands; G-protein-coupled receptors; photopharmacology
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Funding
- International Doctoral Program Receptor Dynamics: Emerging Paradigms for Novel Drugs
- Marie Curie Initial Training Network (ITN) WntsApp [608180]
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The investigation of the mode and time course of the activation of G-protein-coupled receptors (GPCRs), in particular muscarinic acetylcholine (mACh or M) receptors, is still in its infancy despite the tremendous therapeutic relevance of M receptors and GPCRs in general. We herein made use of a dualsteric ligand that can concomitantly interact with the orthosteric, that is, the neurotransmitter, binding site and an allosteric one. We synthetically incorporated a photoswitchable (photochromic) azobenzene moiety. We characterized the photophysical properties of this ligand called BQCAAI and investigated its applicability as a pharmacological tool compound with a set of FRET techniques at the M-1 receptor. BQCAAI proved to be an unprecedented molecular tool; it is the first photoswitchable dualsteric ligand, and its activity can be regulated by light. We also applied BQCCAI to investigate the time course of several receptor activation processes.
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