Search Results - "Bünemann, Moritz"
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The pocketome of G-protein-coupled receptors reveals previously untargeted allosteric sites
Published in Nature communications (10-05-2022)“…G-protein-coupled receptors do not only feature the orthosteric pockets, where most endogenous agonists bind, but also a multitude of other allosteric pockets…”
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Voltage regulates adrenergic receptor function
Published in Proceedings of the National Academy of Sciences - PNAS (22-01-2013)“…The present study demonstrates that agonist-mediated activation of α2A adrenergic receptors (α ₂AAR) is voltage-dependent. By resolving the kinetics of…”
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DP2 receptor activity sensor suited for antagonist screening and measurement of receptor dynamics in real-time
Published in Scientific reports (08-04-2024)“…The DP2 receptor is a G-protein coupled receptor involved in allergic inflammation and is the target of recently developed antagonists already being tested in…”
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Opioid receptors: single molecule studies shed light on mechanisms of efficacy
Published in Signal transduction and targeted therapy (30-08-2024)Get full text
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Comparative Docking to Distinct G Protein-Coupled Receptor Conformations Exclusively Yields Ligands with Agonist Efficacy
Published in Molecular pharmacology (01-12-2019)“…G protein-coupled receptors exist in a whole spectrum of conformations that are stabilized by the binding of ligands with different efficacy or intracellular…”
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The Effect of Cell Surface Expression and Linker Sequence on the Recruitment of Arrestin to the GIP Receptor
Published in Frontiers in pharmacology (13-08-2020)“…The glucose-dependent insulinotropic polypeptide (GIP) and the glucagon-like peptide-1 (GLP-1) receptor are important targets in the treatment of both type 2…”
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Disentangling bias between Gq, GRK2, and arrestin3 recruitment to the M3 muscarinic acetylcholine receptor
Published in eLife (01-12-2021)“…G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular effector proteins. Different agonists can…”
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Anti-nociceptive action of peripheral mu-opioid receptors by G-beta-gamma protein-mediated inhibition of TRPM3 channels
Published in eLife (15-08-2017)“…Opioids, agonists of µ-opioid receptors (µORs), are the strongest pain killers clinically available. Their action includes a strong central component, which…”
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Differential interaction patterns of opioid analgesics with µ opioid receptors correlate with ligand-specific voltage sensitivity
Published in eLife (20-11-2023)“…The µ opioid receptor (MOR) is the key target for analgesia, but the application of opioids is accompanied by several issues. There is a wide range of opioid…”
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Orphan G Protein–Coupled Receptor GPRC5B Controls Smooth Muscle Contractility and Differentiation by Inhibiting Prostacyclin Receptor Signaling
Published in Circulation (New York, N.Y.) (07-04-2020)“…BACKGROUND:G protein–coupled receptors are important regulators of contractility and differentiation in vascular smooth muscle cells (SMCs), but the specific…”
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Structures in G proteins important for subtype selective receptor binding and subsequent activation
Published in Communications biology (27-05-2021)“…G protein-coupled receptors (GPCRs) selectively couple to specific heterotrimeric G proteins comprised of four subfamilies in order to induce appropriate…”
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Cyclic AMP Imaging in Adult Cardiac Myocytes Reveals Far-Reaching β1-Adrenergic but Locally Confined β2-Adrenergic Receptor–Mediated Signaling
Published in Circulation research (10-11-2006)“…β1- and β2-adrenergic receptors (βARs) are known to differentially regulate cardiomyocyte contraction and growth. We tested the hypothesis that these…”
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Gi Protein Activation in Intact Cells Involves Subunit Rearrangement Rather than Dissociation
Published in Proceedings of the National Academy of Sciences - PNAS (23-12-2003)“…G protein-coupled receptors transduce diverse extracellular signals, such as neurotransmitters, hormones, chemokines, and sensory stimuli, into intracellular…”
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Novel Single Chain cAMP Sensors for Receptor-induced Signal Propagation
Published in The Journal of biological chemistry (03-09-2004)“…cAMP is a universal second messenger of many G-protein-coupled receptors and regulates a wide variety of cellular events. cAMP exerts its effects via…”
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Interaction kinetics between p115-RhoGEF and Gα13 are determined by unique molecular interactions affecting agonist sensitivity
Published in Communications biology (24-11-2022)“…The three RH-RhoGEFs (Guanine nucleotide exchange factors) p115-RhoGEF, LARG (leukemia-associated RhoGEF) and PDZ-RhoGEF link G-protein coupled receptors…”
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Minireview: GPCR and G Proteins: Drug Efficacy and Activation in Live Cells
Published in Molecular endocrinology (Baltimore, Md.) (01-05-2009)“…Many biochemical pathways are driven by G protein-coupled receptors, cell surface proteins that convert the binding of extracellular chemical, sensory, and…”
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Dynamics of receptor/G protein coupling in living cells
Published in The EMBO journal (07-12-2005)“…The interaction of activated G protein‐coupled receptors with G proteins is a key event in signal transduction. Here, using a fluorescence resonance energy…”
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A reverse signaling pathway downstream of Sema4A controls cell migration via Scrib
Published in The Journal of cell biology (02-01-2017)“…Semaphorins comprise a large family of ligands that regulate key cellular functions through their receptors, plexins. In this study, we show that the…”
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Potentiation of receptor responses induced by prolonged binding of Gα13 and leukemia‐associated RhoGEF
Published in The FASEB journal (01-08-2017)“…ABSTRACT Diverse cellular functions are controlled by RhoA‐GTPases, which are activated by trimeric G proteins via RhoGEFs, among others. In this study, we…”
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The GIP receptor displays higher basal activity than the GLP-1 receptor but does not recruit GRK2 or arrestin3 effectively
Published in PloS one (05-09-2014)“…Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are important regulators of insulin secretion, and their functional loss…”
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