Gerwe, HubertSchaller, EvaSortino, RosalbaOpar, EkinMartinez Tambella, JoaquinBermudez, MarcelLane, J RobertGorostiza Langa, Pablo IgnacioDecker, Michael2025-01-092025-01-092024-10-081433-7851https://hdl.handle.net/2445/217335The field of G protein-coupled receptor (GPCR) research has greatly benefited from the spatiotemporal resolution provided by light controllable, i.e., photoswitchable ligands. Most of the developed tools have targeted the Rhodopsin-like family (Class A), the largest family of GPCRs. However, to date, all such Class A photoswitchable ligands were designed to act at the orthosteric binding site of these receptors. Herein, we report the development of the first photoswitchable allosteric modulators of Class A GPCRs, designed to target the M-1 muscarinic acetylcholine receptor. The presented benzyl quinolone carboxylic acid (BQCA) derivatives, Photo-BQCisA and Photo-BQCtrAns, exhibit complementary photopharmacological behavior and allow reversible control of the receptor using light as an external stimulus. This makes them valuable tools to further investigate M-1 receptor signaling and a proof of concept for photoswitchable allosteric modulators at Class A receptors.9 p.application/pdfengcc-by (c) Gerwe, Hubert et al., 2024http://creativecommons.org/licenses/by/3.0/es/FotofarmacologiaEnzims al·lostèricsPhotopharmacologyAllosteric enzymesinfo:eu-repo/semantics/article2025-01-08info:eu-repo/semantics/openAccess670287439136071