Research ArticleArticle
A New Molecular Mechanism To Engineer Protean Agonism at a G Protein–Coupled Receptor
Anna De Min, Carlo Matera, Andreas Bock, Janine Holze, Jessica Kloeckner, Mathias Muth, Christian Traenkle, Marco De Amici, Terry Kenakin, Ulrike Holzgrabe, Clelia Dallanoce, Evi Kostenis, Klaus Mohr and Ramona Schrage
Molecular Pharmacology April 2017, 91 (4) 348-356; DOI: https://doi.org/10.1124/mol.116.107276
Anna De Min
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Carlo Matera
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Andreas Bock
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Janine Holze
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Jessica Kloeckner
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Mathias Muth
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Christian Traenkle
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Marco De Amici
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Terry Kenakin
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Ulrike Holzgrabe
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Clelia Dallanoce
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Evi Kostenis
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Klaus Mohr
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
Ramona Schrage
Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scienze Farmaceutiche, Sezione di Chimica Farmaceutica ‘Pietro Pratesi,’ Università degli Studi di Milano, Milano, Italy (C.M., M.D.A., C.D.); Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (A.B.); Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, University of Würzburg, Würzburg, Germany (J.K., M.M., U.H.); and Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, North Carolina (T.K.)
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Research ArticleArticle
Designed Dualsteric Ligands Act as Protean Agonists at M2
Anna De Min, Carlo Matera, Andreas Bock, Janine Holze, Jessica Kloeckner, Mathias Muth, Christian Traenkle, Marco De Amici, Terry Kenakin, Ulrike Holzgrabe, Clelia Dallanoce, Evi Kostenis, Klaus Mohr and Ramona Schrage
Molecular Pharmacology April 1, 2017, 91 (4) 348-356; DOI: https://doi.org/10.1124/mol.116.107276
Research ArticleArticle
Designed Dualsteric Ligands Act as Protean Agonists at M2
Anna De Min, Carlo Matera, Andreas Bock, Janine Holze, Jessica Kloeckner, Mathias Muth, Christian Traenkle, Marco De Amici, Terry Kenakin, Ulrike Holzgrabe, Clelia Dallanoce, Evi Kostenis, Klaus Mohr and Ramona Schrage
Molecular Pharmacology April 1, 2017, 91 (4) 348-356; DOI: https://doi.org/10.1124/mol.116.107276
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