Search Results - "Löber, Stefan"

Discovery of 2‑Aminopyrimidines as Potent Agonists for the Bitter Taste Receptor TAS2R14 by Waterloo, Lukas, Hübner, Harald, Fierro, Fabrizio, Pfeiffer, Tara, Brox, Regine, Löber, Stefan, Weikert, Dorothee, Niv, Masha Y., Gmeiner, Peter

“…The bitter taste receptor TAS2R14 is a G protein-coupled receptor that is found on the tongue as well as in the human airway smooth muscle and other extraoral…”
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Rational design of agonists for bitter taste receptor TAS2R14: from modeling to bench and back by Di Pizio, Antonella, Waterloo, Lukas A. W., Brox, Regine, Löber, Stefan, Weikert, Dorothee, Behrens, Maik, Gmeiner, Peter, Niv, Masha Y.

“…Human bitter taste receptors (TAS2Rs) are a subfamily of 25 G protein-coupled receptors that mediate bitter taste perception. TAS2R14 is the most broadly tuned…”
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Structure-based development of caged dopamine D2/D3 receptor antagonists by Gienger, Marie, Hübner, Harald, Löber, Stefan, König, Burkhard, Gmeiner, Peter

“…Dopamine is a neurotransmitter of great physiological relevance. Disorders in dopaminergic signal transduction are associated with psychiatric and neurological…”
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The Bitter Taste Receptor TAS2R14 as a Drug Target by Waterloo, Lukas A W, Löber, Stefan, Gmeiner, Peter

“…G protein-coupled receptors (GPCRs) mediate most of our physiological responses to hormones, neurotransmitters and environmental stimulants. Besides human…”
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Presynaptic vesicular accumulation is required for antipsychotic efficacy in psychotic-like rats by Uzuneser, Taygun C, Weiss, Eva-Maria, Dahlmanns, Jana, Kalinichenko, Liubov S, Amato, Davide, Kornhuber, Johannes, Alzheimer, Christian, Hellmann, Jan, Kaindl, Jonas, Hübner, Harald, Löber, Stefan, Gmeiner, Peter, Grömer, Teja W, Müller, Christian P

“…Background: The therapeutic effects of antipsychotic drugs (APDs) are mainly attributed to their postsynaptic inhibitory functions on the dopamine D2 receptor,…”
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Bioisosteric Replacement Leading to Biologically Active [2.2]Paracyclophanes with Altered Binding Profiles for Aminergic G-Protein-Coupled Receptors by Skultety, Marika, Hübner, Harald, Löber, Stefan, Gmeiner, Peter

“…Exploring the chemical diversity space of GPCR ligands, we recently discovered [2.2]paracyclophanes as valuable atypical bioisosteres for secondary affinity…”
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Discovery of dopamine D4 receptor antagonists with planar chirality by Sanna, Fabrizio, Ortner, Birgit, Hübner, Harald, Löber, Stefan, Tschammer, Nuska, Gmeiner, Peter

“…Employing the D4 selective phenylpiperazine 2 as a lead compound, planar chiral analogs with paracyclophane substructure were synthesized and evaluated for…”
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A Chimeric Ligand Approach Leading to Potent Antiprion Active Acridine Derivatives:  Design, Synthesis, and Biological Investigations by Dollinger, Silke, Löber, Stefan, Klingenstein, Ralf, Korth, Carsten, Gmeiner, Peter

“…Human transmissible neurodegenerations including Creutzfeldt−Jakob disease are unique, since they are caused by prions, an infectious agent that replicates…”
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Synthesis, Radiofluorination, and In Vitro Evaluation of Pyrazolo[1,5-a]pyridine-Based Dopamine D4 Receptor Ligands: Discovery of an Inverse Agonist Radioligand for PET by Prante, Olaf, Tietze, Rainer, Hocke, Carsten, Löber, Stefan, Hübner, Harald, Kuwert, Torsten, Gmeiner, Peter

“…A series of fluoro-substituted analogs structurally derived from the aminomethyl-substituted pyrazolo[1,5-a]pyridine lead compounds 9 (FAUC 113) and 10 (FAUC…”
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Bivalent molecular probes for dopamine D2-like receptors by Huber, Daniela, Löber, Stefan, Hübner, Harald, Gmeiner, Peter

“…Merging two arylamidoalkyl substituted phenylpiperazines as prototypical recognition elements for dopamine D2-like receptors by oligoethylene glycol linkers…”
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Tricyclic antidepressants, quinacrine and a novel, synthetic chimera thereof clear prions by destabilizing detergent‐resistant membrane compartments by Klingenstein, Ralf, Löber, Stefan, Kujala, Pekka, Godsave, Susan, Leliveld, S. Rutger, Gmeiner, Peter, Peters, Peter J., Korth, Carsten

“…Prion diseases are invariably fatal, neurodegenerative diseases transmitted by an infectious agent, PrPSc, a pathogenic, conformational isoform of the normal…”
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Click chemistry on solid support: synthesis of a new REM resin and application for the preparation of tertiary amines by Löber, Stefan, Gmeiner, Peter

“…1,3-Dipolar cycloaddition was employed for the synthesis of a highly practical REM resin. Exploiting this concept, the resulting triazolylmethyl acrylate (TMA)…”
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Recent advances in the search for D3 - and D4 -selective drugs: probes, models and candidates by Löber, Stefan, Hübner, Harald, Tschammer, Nuska, Gmeiner, Peter

“…Dopamine D2 -like receptors (including D2 , D3 and D4 ) belong to the ‘rhodopsin-like’ family of G protein-coupled receptors (GPCRs), which represent the…”
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Novel azulene derivatives for the treatment of erectile dysfunction by Löber, Stefan, Hübner, Harald, Buschauer, Armin, Sanna, Fabrizio, Argiolas, Antonio, Melis, Maria Rosaria, Gmeiner, Peter

“…Based on the dopamine D4 receptor partial agonist FAUC 3019, a series of azulenylmethylpiperazines was synthesized and affinities for the monoaminergic GPCRs…”
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Quinpramine ameliorates rat experimental autoimmune neuritis and redistributes MHC class II molecules by Meyer zu Hörste, Gerd, Mausberg, Anne K, Müller, Johanna I, Lehmann, Helmar C, Löber, Stefan, Gmeiner, Peter, Hartung, Hans-Peter, Stüve, Olaf, Korth, Carsten, Kieseier, Bernd C

“…Activation of inflammatory cells is central to the pathogenesis of autoimmune demyelinating diseases of the peripheral nervous system. The novel chimeric…”
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Rationally Based Efficacy Tuning of Selective Dopamine D4 Receptor Ligands Leading to the Complete Antagonist 2-[4-(4-Chlorophenyl)piperazin-1- ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213) by Löber, Stefan, Hübner, Harald, Utz, Wolfgang, Gmeiner, Peter

“…Structure dependent efficacy studies in the field of selective D4 ligands led to the 2-aminomethyl substituted azaindole 2 (FAUC 213) that displayed strong D4…”
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Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype by Hocke, Carsten, Prante, Olaf, Löber, Stefan, Hübner, Harald, Gmeiner, Peter, Kuwert, Torsten

“…Highly selective dopamine D3 receptor radioligands were synthesized. The benzofuran derivative 11b displayed D3 selectivity of 560-fold over D2 ( K i 5.7 nM)…”
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18F-Labeled FAUC 346 and BP 897 Derivatives as Subtype-Selective Potential PET Radioligands for the Dopamine D3 Receptor by Hocke, Carsten, Prante, Olaf, Salama, Ismael, Hübner, Harald, Löber, Stefan, Kuwert, Torsten, Gmeiner, Peter

“…Disturbances of neutrotransmission at the dopamine D3 receptor are related to several neuropsychiatric diseases and in particular to drug addiction. Herein, we…”
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GPCR crystal structures: Medicinal chemistry in the pocket by Shonberg, Jeremy, Kling, Ralf C., Gmeiner, Peter, Löber, Stefan

“…[Display omitted] Recent breakthroughs in GPCR structural biology have significantly increased our understanding of drug action at these therapeutically…”
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Structure-based discovery of opioid analgesics with reduced side effects by Manglik, Aashish, Lin, Henry, Aryal, Dipendra K., McCorvy, John D., Dengler, Daniela, Corder, Gregory, Levit, Anat, Kling, Ralf C., Bernat, Viachaslau, Hübner, Harald, Huang, Xi-Ping, Sassano, Maria F., Giguère, Patrick M., Löber, Stefan, Da Duan, Scherrer, Grégory, Kobilka, Brian K., Gmeiner, Peter, Roth, Bryan L., Shoichet, Brian K.

“…Morphine is an alkaloid from the opium poppy used to treat pain. The potentially lethal side effects of morphine and related opioids—which include fatal…”
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