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index medicus (16) 16
animals (13) 13
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receptor, muscarinic m2 - genetics (3) 3
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adrenergic-receptor (2) 2
allosteric modulation (2) 2
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arrestin-biased agonism (2) 2
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binding (2) 2
binding-sites (2) 2
biochemistry & molecular biology (2) 2
brain (2) 2
cell line, tumor (2) 2
cell membrane - drug effects (2) 2
cell membrane - metabolism (2) 2
cells (2) 2
design (2) 2
drug inverse agonism (2) 2
drug targets (2) 2
efficacy (2) 2
functional-characterization (2) 2
g protein-coupled receptor (2) 2
gtp-binding protein alpha subunits, gq-g11 - metabolism (2) 2
hek293 cells (2) 2
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mice, knockout (2) 2
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muscarinic agonists - chemistry (2) 2
nerve tissue proteins - metabolism (2) 2
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pharmacological characterization (2) 2
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propionates - pharmacology (2) 2
protein conformation - drug effects (2) 2
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receptors, g-protein-coupled - chemistry (2) 2
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science (2) 2
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small molecule libraries - pharmacology (2) 2
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therapeutic opportunities (2) 2
transgenic animals (2) 2
transgenic mice (2) 2
abridged index medicus (1) 1
acetylcholine-receptors (1) 1
adenosine - analogs & derivatives (1) 1
adenosine - pharmacology (1) 1
adenosine monophosphate - analogs & derivatives (1) 1
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1. Full Text Functional selectivity and dualsteric/bitopic GPCR targeting
by Schrage, Ramona and Kostenis, Evi
Current Opinion in Pharmacology, ISSN 1471-4892, 2016, Volume 32, pp. 85 - 90
Highlights • GPCR-linked signaling is pleiotropic and involves multiple intracellular pathways. • Biased ligands favor particular signaling pathways at the... 
Internal Medicine | Medical Education | DESIGN | BIASED AGONISM | ALLOSTERIC MODULATORS | EFFICACY | PHOSPHORYLATION | DRUG DISCOVERY | HEART-FAILURE | PROTEIN-COUPLED RECEPTORS | PHARMACOLOGY & PHARMACY | LIGAND | MU-OPIOID RECEPTOR | Receptors, Angiotensin - metabolism | Receptors, G-Protein-Coupled - metabolism | Receptors, Opioid, mu - metabolism | Humans | Receptors, G-Protein-Coupled - agonists | Receptors, Opioid, mu - agonists | Molecular Targeted Therapy | Animals | Receptors, Angiotensin - agonists | Signal Transduction - drug effects | Drug Design | Protein Binding | Ligands | G proteins | Membrane proteins
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2. Full Text Allosteric modulators targeting CNS muscarinic receptors
by Bock, Andreas and Schrage, Ramona and Mohr, Klaus
Neuropharmacology, ISSN 0028-3908, 07/2018, Volume 136, Issue Pt C, pp. 427 - 437
Muscarinic acetylcholine receptors are G protein-coupled receptors (GPCRs) which are broadly expressed in the central nervous system (CNS) and other tissues in... 
Bitopic ligands | Biased signaling | Subtype-selectivity | Dualsteric ligands | Allosteric modulation | Muscarinic acetylcholine receptors | MLPCN PROBE MOLECULE | M-1 PAM ML137 | CONFORMATIONAL DYNAMICS | NEUROSCIENCES | ACETYLCHOLINE-RECEPTOR | SUBTYPE SELECTIVITY | PROTEIN-COUPLED RECEPTOR | DRUG DEVELOPMENT | FUNCTIONAL SELECTIVITY | PHARMACOLOGY & PHARMACY | RATIONAL DESIGN | Drug discovery | G proteins
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3. Full Text The experimental power of FR900359 to study Gq-regulated biological processes
by Schrage, Ramona and Schmitz, Anna-Lena and Gaffal, Evelyn and Annala, Suvi and Kehraus, Stefan and Wenzel, Daniela and Büllesbach, Katrin M and Bald, Tobias and Inoue, Asuka and Shinjo, Yuji and Galandrin, Ségolène and Shridhar, Naveen and Hesse, Michael and Grundmann, Manuel and Merten, Nicole and Charpentier, Thomas H and Martz, Matthew and Butcher, Adrian J and Slodczyk, Tanja and Armando, Sylvain and Effern, Maike and Namkung, Yoon and Jenkins, Laura and Horn, Velten and Stößel, Anne and Dargatz, Harald and Tietze, Daniel and Imhof, Diana and Gales, Céline and Drewke, Christel and Müller, Christa E and Hölzel, Michael and Milligan, Graeme and Tobin, Andrew B and Gomeza, Jesus and Dohlman, Henrik G and Sondek, John and Harden, T. Kendall and Bouvier, Michel and Laporte, Stéphane A and Aoki, Junken and Fleischmann, Bernd K and Mohr, Klaus and König, Gabriele M and Tüting, Thomas and Kostenis, Evi
Nature Communications, ISSN 2041-1723, 2015, Volume 6, Issue 1, pp. 10156 - 10156
Despite the discovery of heterotrimeric alpha beta gamma G proteins similar to 25 years ago, their selective perturbation by cell-permeable inhibitors remains... 
ADENYLATE-CYCLASE SYSTEM | 7-TRANSMEMBRANE RECEPTORS | ACTIVATION | HETEROTRIMERIC G-PROTEINS | G-ALPHA | SMALL-MOLECULE | MULTIDISCIPLINARY SCIENCES | PHOSPHOLIPASE-C | IN-VIVO | PROTEIN-COUPLED RECEPTORS | CYCLIC DEPSIPEPTIDE | Melanoma - metabolism | GTP-Binding Protein alpha Subunits, Gq-G11 - genetics | Signal Transduction | Humans | Models, Molecular | Depsipeptides - pharmacology | Vasoconstriction - drug effects | Animals | Ardisia - chemistry | Protein Isoforms | Tail - blood supply | Cell Line, Tumor | Protein Conformation | Mice | Molecular Structure | Gene Expression Regulation, Neoplastic - drug effects | GTP-Binding Protein alpha Subunits, Gq-G11 - metabolism | Depsipeptides - chemistry | Proteins | Signaling | Perturbation | Biological activity | Index Medicus
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4. Full Text The allosteric vestibule of a seven transmembrane helical receptor controls G-protein coupling
by Bock, Andreas and Merten, Nicole and Schrage, Ramona and Dallanoce, Clelia and Bätz, Julia and Klöckner, Jessica and Schmitz, Jens and Matera, Carlo and Simon, Katharina and Kebig, Anna and Peters, Lucas and Müller, Anke and Schrobang-Ley, Jasmin and Tränkle, Christian and Hoffmann, Carsten and De Amici, Marco and Holzgrabe, Ulrike and Kostenis, Evi and Mohr, Klaus
Nature Communications, ISSN 2041-1723, 2012, Volume 3, Issue 1, p. 1044
Seven transmembrane helical receptors (7TMRs) modulate cell function via different types of G proteins, often in a ligand-specific manner. Class A 7TMRs... 
SITE | 7-TRANSMEMBRANE RECEPTORS | ACTIVATION | LIGANDS | CRYSTAL-STRUCTURE | AMINO-ACIDS | MULTIDISCIPLINARY SCIENCES | DRUG DISCOVERY | FUNCTIONAL SELECTIVITY | MUSCARINIC ACETYLCHOLINE-RECEPTORS | LIVING CELLS | Protein Structure, Tertiary | Receptor, Muscarinic M2 - genetics | Protein Structure, Secondary | Receptor, Muscarinic M2 - metabolism | Receptors, G-Protein-Coupled - metabolism | Humans | Allosteric Site | Receptors, G-Protein-Coupled - genetics | Receptor, Muscarinic M2 - chemistry | Receptors, G-Protein-Coupled - chemistry | GTP-Binding Proteins - metabolism
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5. Full Text Expression analysis of CB2-GFP BAC transgenic mice
by Schmöle, Anne-Caroline and Lundt, Ramona and Gennequin, Benjamin and Schrage, Hanna and Beins, Eva and Krämer, Alexandra and Zimmer, Till and Limmer, Andreas and Zimmer, Andreas and Otte, David-Marian
PLoS ONE, ISSN 1932-6203, 09/2015, Volume 10, Issue 9, p. e0138986
The endocannabinoid system (ECS) is a retrograde messenger system, consisting of lipid signaling molecules that bind to at least two G-protein-coupled... 
SYSTEM | ACTIVATION | B-CELL | MARGINAL ZONE | RETENTION | MULTIDISCIPLINARY SCIENCES | CANNABINOID CB2 RECEPTORS | LYMPHOCYTES | Green Fluorescent Proteins - metabolism | Promoter Regions, Genetic | Mice, Transgenic | Green Fluorescent Proteins - blood | Green Fluorescent Proteins - genetics | Receptor, Cannabinoid, CB2 - blood | Receptor, Cannabinoid, CB2 - genetics | Brain - metabolism | Chromosomes, Artificial, Bacterial - genetics | Receptor, Cannabinoid, CB2 - metabolism | Animals | Spleen - metabolism | Mice | Thymus Gland - metabolism | B-Lymphocytes - metabolism | Physiological aspects | Genetic engineering | Research | B cells | Dendritic cells | Brain | Animal models | G protein-coupled receptors | Transcription | Trafficking | Antibodies | Fluorescence | Lymphocytes T | Macrophages | Bacterial artificial chromosomes | Cell adhesion & migration | Thymus | Receptors | Lymphocytes | Transgenic animals | Rodents | Labeling | Immune system | Spleen | Immunoglobulins | Dopamine | Cloning | Transgenic mice | Microglia | Lymphocytes B | Psychiatry
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6. Full Text Molecular Alliance—From Orthosteric and Allosteric Ligands to Dualsteric/Bitopic Agonists at G Protein Coupled Receptors
by Mohr, Klaus and Schmitz, Jens and Schrage, Ramona and Tränkle, Christian and Holzgrabe, Ulrike
Angewandte Chemie International Edition, ISSN 1433-7851, 01/2013, Volume 52, Issue 2, pp. 508 - 516
Cell‐membrane‐spanning G protein coupled receptors (GPCRs) belong to the most important therapeutic target structures. Endogenous transmitters bind from the... 
antagonists | agonists | receptors | allosterism | dualsterism | DESIGN | COMPLEX | CRYSTAL-STRUCTURE | MODULATORS | DRUG DISCOVERY | THERAPEUTIC OPPORTUNITIES | CHEMISTRY, MULTIDISCIPLINARY | MUSCARINIC ACETYLCHOLINE-RECEPTORS | OPIOID RECEPTOR | BIVALENT LIGANDS | BINDING-SITES | Receptors, G-Protein-Coupled - metabolism | Signal Transduction | Allosteric Regulation | Humans | Allosteric Site | Drug Design | Models, Molecular | Protein Binding | Ligands | Receptors, G-Protein-Coupled - chemistry
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7. Molecular Alliance--From Orthosteric and Allosteric Ligands to Dualsteric/Bitopic Agonists at GProtein Coupled Receptors
by Klaus Mohr and Jens Schmitz and Ramona Schrage and Christian Tränkle and Ulrike Holzgrabe
Angewandte Chemie, ISSN 1433-7851, 01/2013, Volume 52, Issue 2, pp. 508 - 516
  Cell-membrane-spanning Gprotein coupled receptors (GPCRs) belong to the most important therapeutic target structures. Endogenous transmitters bind from the... 
Proteins | Binding sites | Drugs | Binding | Receptors | Side effects | Activation | Selectivity | Modulators
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8. Full Text Direct targeting of Gαq and Gα11 oncoproteins in cancer cells
by Annala, Suvi and Feng, Xiaodong and Shridhar, Naveen and Eryilmaz, Funda and Patt, Julian and Yang, JuHee and Pfeil, Eva M and Cervantes-Villagrana, Rodolfo Daniel and Inoue, Asuka and Häberlein, Felix and Slodczyk, Tanja and Reher, Raphael and Kehraus, Stefan and Monteleone, Stefania and Schrage, Ramona and Heycke, Nina and Rick, Ulrike and Engel, Sandra and Pfeifer, Alexander and Kolb, Peter and König, Gabriele and Bünemann, Moritz and Tüting, Thomas and Vázquez-Prado, José and Gutkind, J. Silvio and Gaffal, Evelyn and Kostenis, Evi
Science Signaling, ISSN 1945-0877, 03/2019, Volume 12, Issue 573, p. eaau5948
Somatic gain-of-function mutations of GNAQ and GNA11, which encode α subunits of heterotrimeric Gαq/11 proteins, occur in about 85% of cases of uveal melanoma... 
Cell proliferation | Cell culture | GTP | Xenotransplantation | Guanosine | Melanoma | Radiation | Extracellular signal-regulated kinase | Patients | Mutants | Metastases | Phospholipase C | Proteins | Phospholipase | Signal transduction | Signaling | Surgery | Cell lines | Xenografts | Mutation | Inhibition | Cancer | Guanosinetriphosphatase | Tumors
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9. Full Text Correction: Expression Analysis of CB2-GFP BAC Transgenic Mice
by Schmöle, Anne-Caroline and Lundt, Ramona and Gennequin, Benjamin and Schrage, Hanna and Beins, Eva and Krämer, Alexandra and Zimmer, Till and Limmer, Andreas and Zimmer, Andreas and Otte, David-Marian
PloS one, ISSN 1932-6203, 2015, Volume 10, Issue 12, p. e0145472
Transgenic animals | Rodents | Bacterial artificial chromosomes | Transgenic mice
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10. Full Text Rational Design of Partial Agonists for the Muscarinic M1 Acetylcholine Receptor
by Chen, Xinyu and Klöckner, Jessika and Holze, Janine and Zimmermann, Cornelia and Seemann, Wiebke K and Schrage, Ramona and Bock, Andreas and Mohr, Klaus and Tränkle, Christian and Holzgrabe, Ulrike and Decker, Michael
Journal of Medicinal Chemistry, ISSN 0022-2623, 01/2015, Volume 58, Issue 2, pp. 560 - 576
Aiming to design partial agonists for a G-protein-coupled receptor based on dynamic ligand binding, we synthesized three different series of bipharmacophoric... 
Receptor, Muscarinic M1 - agonists | Animals | Cricetulus | Muscarinic Agonists - pharmacology | Drug Design | Structure-Activity Relationship | CHO Cells | Muscarinic Agonists - chemical synthesis
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11. Full Text Decoding signaling and function of the orphan g protein-coupled receptor GPR17 with a small-molecule agonist
by Hennen, Stephanie and Wang, Haibo and Peters, Lucas and Merten, Nicole and Simon, Katharina and Spinrath, Andreas and Blättermann, Stefanie and Akkari, Rhalid and Schrage, Ramona and Schröder, Ralf and Schulz, Daniel and Vermeiren, Celine and Zimmermann, Katrin and Kehraus, Stefan and Drewke, Christel and Pfeifer, Alexander and König, Gabriele M and Mohr, Klaus and Gillard, Michel and Müller, Christa E and Lu, Q. Richard and Gomeza, Jesus and Kostenis, Evi
Science Signaling, ISSN 1945-0877, 10/2013, Volume 6, Issue 298, pp. ra93 - ra93
Replacement of the lost myelin sheath is a therapeutic goal for treating demyelinating diseases of the central nervous system (CNS), such as multiple sclerosis... 
INVERSE AGONISTS | HEK-293 CELLS | 7-TRANSMEMBRANE RECEPTORS | MULTIPLE-SCLEROSIS | ARRESTIN-BIASED AGONISM | PHARMACOLOGICAL CHARACTERIZATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | P2Y RECEPTOR | DRUG TARGETS | OLIGODENDROCYTES | LIVING CELLS | CELL BIOLOGY | Immunohistochemistry | Propionates - pharmacology | Oligodendroglia - metabolism | Small Molecule Libraries - pharmacology | Cricetulus | Rats, Wistar | Receptors, G-Protein-Coupled - metabolism | Humans | Stem Cells - cytology | Receptors, G-Protein-Coupled - agonists | Stem Cells - metabolism | Arrestins - metabolism | Oligodendroglia - drug effects | HEK293 Cells | Indoles - pharmacology | Molecular Structure | Oligodendroglia - cytology | Chromones - pharmacology | CHO Cells | Cell Line | Propionates - chemistry | Cricetinae | Nerve Tissue Proteins - agonists | Cells, Cultured | Rats | Nerve Tissue Proteins - genetics | Mice, Knockout | Nerve Tissue Proteins - metabolism | Small Molecule Libraries - chemistry | Animals | Signal Transduction - drug effects | beta-Arrestins | Cell Line, Tumor | Stem Cells - drug effects | Mice | Receptors, G-Protein-Coupled - genetics | COS Cells | Indoles - chemistry
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12. Full Text The orphan receptor GPR17 is unresponsive to uracil nucleotides and cysteinyl leukotrienes
by Simon, Katharina and Meren, Nicole and Schröder, Ralf and Hennen, Stephanie and Preis, Philip and Schmitt, Nina-Katharina and Peters, Lucas and Schrage, Ramona and Vermeiren, Celine and Gillard, Michel and Mohr, Klaus and Gomeza, Jesus and Kostenis, Evi
Molecular Pharmacology, ISSN 0026-895X, 05/2017, Volume 91, Issue 5, pp. 518 - 532
Pairing orphan G protein-coupled receptors (GPCRs) with their cognate endogenous ligands is expected to have a major impact on our understanding of GPCR... 
CELLS | 7-TRANSMEMBRANE RECEPTORS | ACTIVATION | LIGANDS | PROTEIN-COUPLED RECEPTOR | ARRESTIN-BIASED AGONISM | FREE FATTY-ACIDS | PHARMACOLOGY & PHARMACY | IDENTIFICATION | DRUG TARGETS | BRAIN | Small Molecule Libraries - pharmacology | Cricetinae | Cricetulus | Receptors, G-Protein-Coupled - metabolism | Humans | Leukotrienes - pharmacology | Rats | Adenosine - pharmacology | Uracil Nucleotides - pharmacology | Nerve Tissue Proteins - metabolism | Animals | Signal Transduction - drug effects | Adenosine - analogs & derivatives | Adenosine Monophosphate - analogs & derivatives | Cysteine - pharmacology | HEK293 Cells | Ligands | Adenosine Monophosphate - pharmacology | Cell Membrane - metabolism | Mice | Cell Membrane - drug effects | CHO Cells | Index Medicus
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13. Full Text A new molecular mechanism to engineer protean agonism at a G protein-coupled receptor
by De Min, Anna and Matera, Carlo and Bock, Andreas and Holze, Janine and Kloeckner, Jessica and Muth, Mathias and Traenkle, Christian and De Amici, Marco and Kenakin, Terry and Holzgrabe, Ulrike and Dallanoce, Clelia and Kostenis, Evi and Mohr, Klaus and Schrage, Ramona
Molecular Pharmacology, ISSN 0026-895X, 04/2017, Volume 91, Issue 4, pp. 348 - 356
Protean agonists are of great pharmacological interest as their behavior may change in magnitude and direction depending on the constitutive activity of a... 
IN-VITRO | 7-TRANSMEMBRANE RECEPTORS | STRUCTURAL BASIS | PHARMACOLOGICAL CHARACTERIZATION | CONSTITUTIVE ACTIVATION | PHARMACOLOGY & PHARMACY | FUNCTIONAL-CHARACTERIZATION | ADRENERGIC-RECEPTOR | BINDING-SITES | ALLOSTERIC SITE | MUSCARINIC ACETYLCHOLINE-RECEPTORS | Cricetinae | Cricetulus | Receptor, Muscarinic M2 - metabolism | Receptors, G-Protein-Coupled - metabolism | Allosteric Regulation | Humans | Receptors, G-Protein-Coupled - agonists | Animals | Protein Engineering | Protein Binding | Ligands | CHO Cells | Tromethamine | Index Medicus
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14. Full Text Dualsteric Muscarinic Antagonists–Orthosteric Binding Pose Controls Allosteric Subtype Selectivity
by Schmitz, Jens and van der Mey, Dorina and Bermudez, Marcel and Klöckner, Jessica and Schrage, Ramona and Kostenis, Evi and Tränkle, Christian and Wolber, Gerhard and Mohr, Klaus and Holzgrabe, Ulrike
Journal of Medicinal Chemistry, ISSN 0022-2623, 08/2014, Volume 57, Issue 15, pp. 6739 - 6750
Bivalent ligands of G protein-coupled receptors have been shown to simultaneously either bind to two adjacent receptors or to bridge different parts of one... 
ACETYLCHOLINE-RECEPTORS | CHEMISTRY, MEDICINAL | LIGAND-BINDING | CRYSTAL-STRUCTURE | AMINO-ACIDS | THERAPEUTIC OPPORTUNITIES | PROTEIN-COUPLED RECEPTORS | FUNCTIONAL-CHARACTERIZATION | OXOTREMORINE-M | DERIVATIVES | GENETIC ALGORITHM | Receptor, Muscarinic M2 - agonists | Receptor, Muscarinic M2 - genetics | Cricetulus | Muscarinic Agonists - pharmacology | Stereoisomerism | Allosteric Regulation | Humans | Molecular Conformation | Atropine Derivatives - pharmacology | Phthalimides - chemistry | Structure-Activity Relationship | Muscarinic Agonists - chemical synthesis | Phthalimides - pharmacology | Naphthalimides - chemical synthesis | Phthalimides - chemical synthesis | Muscarinic Antagonists - pharmacology | Receptor, Muscarinic M2 - antagonists & inhibitors | Naphthalimides - chemistry | Radioligand Assay | Binding Sites | Scopolamine Derivatives - chemical synthesis | CHO Cells | Atropine Derivatives - chemistry | Scopolamine Derivatives - pharmacology | Muscarinic Antagonists - chemical synthesis | Scopolamine Derivatives - chemistry | Muscarinic Antagonists - chemistry | Molecular Dynamics Simulation | Animals | Naphthalimides - pharmacology | Drug Inverse Agonism | Atropine Derivatives - chemical synthesis | Molecular Docking Simulation | Muscarinic Agonists - chemistry | Mutation | Index Medicus
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