title: Adhesion G Protein-Coupled Receptors: From In Vitro Pharmacology to In Vivo Mechanisms.
abstract: The adhesion family of G protein-coupled receptors (aGPCRs) comprises 33 members in humans. aGPCRs are characterized by their enormous size and complex modular structures. While the physiologic importance of many aGPCRs has been clearly demonstrated in recent years, the underlying molecular functions have only recently begun to be elucidated. In this minireview, we present an overview of our current knowledge on aGPCR activation and signal transduction with a focus on the latest findings regarding the interplay between ligand binding, mechanical force, and the tethered agonistic Stachel sequence, as well as implications on translational approaches that may derive from understanding aGPCR pharmacology.
authors.affiliation: Department of Developmental Biology, Washington University School of Medicine, St. Louis, Missouri (K.R.M.); Department of Experimental Immunology, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands (J.H.); Department of Neurophysiology, Institute of Physiology, University of Würzburg, Würzburg, Germany (T.L.); Department of Medicinal Chemistry/Amsterdam Institute for Molecules, Medicines and Systems, VU University, Amsterdam, The Netherlands (S.N.); and Institute of Biochemistry, Molecular Biochemistry, Medical Faculty, University of Leipzig, Leipzig, Germany (T.S., I.L.).
authors.forename: Kelly R
authors.initials: KR
authors.lastname: Monk
authors.affiliation: Department of Developmental Biology, Washington University School of Medicine, St. Louis, Missouri (K.R.M.); Department of Experimental Immunology, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands (J.H.); Department of Neurophysiology, Institute of Physiology, University of Würzburg, Würzburg, Germany (T.L.); Department of Medicinal Chemistry/Amsterdam Institute for Molecules, Medicines and Systems, VU University, Amsterdam, The Netherlands (S.N.); and Institute of Biochemistry, Molecular Biochemistry, Medical Faculty, University of Leipzig, Leipzig, Germany (T.S., I.L.).
authors.forename: Jörg
authors.initials: J
authors.lastname: Hamann
authors.affiliation: Department of Developmental Biology, Washington University School of Medicine, St. Louis, Missouri (K.R.M.); Department of Experimental Immunology, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands (J.H.); Department of Neurophysiology, Institute of Physiology, University of Würzburg, Würzburg, Germany (T.L.); Department of Medicinal Chemistry/Amsterdam Institute for Molecules, Medicines and Systems, VU University, Amsterdam, The Netherlands (S.N.); and Institute of Biochemistry, Molecular Biochemistry, Medical Faculty, University of Leipzig, Leipzig, Germany (T.S., I.L.).
authors.forename: Tobias
authors.initials: T
authors.lastname: Langenhan
authors.affiliation: Department of Developmental Biology, Washington University School of Medicine, St. Louis, Missouri (K.R.M.); Department of Experimental Immunology, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands (J.H.); Department of Neurophysiology, Institute of Physiology, University of Würzburg, Würzburg, Germany (T.L.); Department of Medicinal Chemistry/Amsterdam Institute for Molecules, Medicines and Systems, VU University, Amsterdam, The Netherlands (S.N.); and Institute of Biochemistry, Molecular Biochemistry, Medical Faculty, University of Leipzig, Leipzig, Germany (T.S., I.L.).
authors.forename: Saskia
authors.initials: S
authors.lastname: Nijmeijer
authors.affiliation: Department of Developmental Biology, Washington University School of Medicine, St. Louis, Missouri (K.R.M.); Department of Experimental Immunology, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands (J.H.); Department of Neurophysiology, Institute of Physiology, University of Würzburg, Würzburg, Germany (T.L.); Department of Medicinal Chemistry/Amsterdam Institute for Molecules, Medicines and Systems, VU University, Amsterdam, The Netherlands (S.N.); and Institute of Biochemistry, Molecular Biochemistry, Medical Faculty, University of Leipzig, Leipzig, Germany (T.S., I.L.).
authors.forename: Torsten
authors.initials: T
authors.lastname: Schöneberg
authors.affiliation: Department of Developmental Biology, Washington University School of Medicine, St. Louis, Missouri (K.R.M.); Department of Experimental Immunology, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands (J.H.); Department of Neurophysiology, Institute of Physiology, University of Würzburg, Würzburg, Germany (T.L.); Department of Medicinal Chemistry/Amsterdam Institute for Molecules, Medicines and Systems, VU University, Amsterdam, The Netherlands (S.N.); and Institute of Biochemistry, Molecular Biochemistry, Medical Faculty, University of Leipzig, Leipzig, Germany (T.S., I.L.) ines.liebscher@medizin.uni-leipzig.de.
authors.forename: Ines
authors.initials: I
authors.lastname: Liebscher
mesh_terms: D000818:Animals; D002448:Cell Adhesion; D006801:Humans; D011485:Protein Binding; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000737:chemistry / Q000378:metabolism*; D018000:Receptors, Peptide / Q000819:agonists / Q000737:chemistry / Q000378:metabolism*; D015398:Signal Transduction
chemical_list: D043562:Receptors, G-Protein-Coupled; D018000:Receptors, Peptide