ArticleMolecules (Basel, Switzerland)2023
Novel Xanomeline-Containing Bitopic Ligands of Muscarinic Acetylcholine Receptors: Design, Synthesis and FRET Investigation.
Carlo Matera, Michael Kauk, Davide Cirillo, Marco Maspero, Claudio Papotto, Daniela Volpato, Ulrike Holzgrabe, Marco De Amici, Carsten Hoffmann, Clelia Dallanoce
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In one paragraphArticle in Molecules (Basel, Switzerland), 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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10 authors.
Carlo MateraDepartment of Pharmaceutical Sciences, Medicinal Chemistry Section "Pietro Pratesi", University of Milan, Via L. Mangiagalli 25, 20133 Milan, Italy.ORCID 0000-0001-6939-3859 Michael KaukInstitute for Molecular Cell Biology, Center for Molecular Biomedicine, University Hospital Jena, Friedrich Schiller University Jena, Hans Knoell Str. 2, 07745 Jena, Germany.
Davide CirilloDepartment of Pharmaceutical Sciences, Medicinal Chemistry Section "Pietro Pratesi", University of Milan, Via L. Mangiagalli 25, 20133 Milan, Italy.ORCID 0000-0001-5133-0702 Marco MasperoDepartment of Pharmaceutical Sciences, Medicinal Chemistry Section "Pietro Pratesi", University of Milan, Via L. Mangiagalli 25, 20133 Milan, Italy.ORCID 0000-0002-2438-9490 Claudio PapottoDepartment of Pharmaceutical Sciences, Medicinal Chemistry Section "Pietro Pratesi", University of Milan, Via L. Mangiagalli 25, 20133 Milan, Italy.ORCID 0000-0003-1877-8331 Daniela VolpatoPharmaceutical and Medicinal Chemistry, Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.
Ulrike HolzgrabePharmaceutical and Medicinal Chemistry, Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.ORCID 0000-0002-0364-7278 Marco De AmiciDepartment of Pharmaceutical Sciences, Medicinal Chemistry Section "Pietro Pratesi", University of Milan, Via L. Mangiagalli 25, 20133 Milan, Italy.ORCID 0000-0002-0236-0662 Carsten HoffmannInstitute for Molecular Cell Biology, Center for Molecular Biomedicine, University Hospital Jena, Friedrich Schiller University Jena, Hans Knoell Str. 2, 07745 Jena, Germany.
Clelia DallanoceDepartment of Pharmaceutical Sciences, Medicinal Chemistry Section "Pietro Pratesi", University of Milan, Via L. Mangiagalli 25, 20133 Milan, Italy.ORCID 0000-0002-7383-1484 Funding
No grant is acknowledged in the PubMed record.
6 · The paper itselfAbstract
In the last few years, fluorescence resonance energy transfer (FRET) receptor sensors have contributed to the understanding of GPCR ligand binding and functional activation. FRET sensors based on muscarinic acetylcholine receptors (mAChRs) have been employed to study dual-steric ligands, allowing for the detection of different kinetics and distinguishing between partial, full, and super agonism. Herein, we report the synthesis of the two series of bitopic ligands,
Indexed as
Fluorescence Resonance Energy TransferReceptors, G-Protein-CoupledAnimalsCHO CellsCricetinaeLigandsPyridinesReceptor, Muscarinic M1Receptors, MuscarinicThiadiazolesLigandsPyridinesReceptor, Muscarinic M1Receptors, G-Protein-CoupledReceptors, MuscarinicThiadiazolesxanomeline77-LH-28-1bitopic hybrid ligandsfluorescence resonance energy transfermuscarinic acetylcholine receptorssynthesisXanomeline
Identifiers
PMID36903650
PMCPMC10005175
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