Analyzing biased responses of GPCR ligands

Urban, 2007, Functional selectivity and classical concepts of quantitative pharmacology, J Pharmacol Exp Ther, 320, 1, 10.1124/jpet.106.104463 Kenakin, 2007, Functional selectivity through protean and biased agonism: who steers the ship?, Mol Pharmacol, 72, 1393, 10.1124/mol.107.040352 Violin, 2014, Biased ligands at G-protein-coupled receptors: promise and progress, Trends Pharmacol Sci, 35, 308, 10.1016/j.tips.2014.04.007 Kenakin, 2012, A simple method for quantifying functional selectivity and agonist bias, ACS Chem Neurosci, 3, 193, 10.1021/cn200111m Stott, 2016, Unravelling intrinsic efficacy and ligand bias at G protein coupled receptors: a practical guide to assessing functional data, Biochem Pharmacol, 101, 1, 10.1016/j.bcp.2015.10.011 Kenakin, 2013, Measurements of ligand bias and functional affinity, Nat Rev Drug Discov, 12, 483, 10.1038/nrd3954-c2 Ferrandon, 2009, Sustained cyclic AMP production by parathyroid hormone receptor endocytosis, Nat Chem Biol, 5, 734, 10.1038/nchembio.206 Irannejad, 2013, Conformational biosensors reveal GPCR signalling from endosomes, Nature, 495, 534, 10.1038/nature12000 Klein Herenbrink, 2016, The role of kinetic context in apparent biased agonism at GPCRs, Nat Commun, 7, 10842, 10.1038/ncomms10842 Thompson, 2016, Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor, Biochem Pharmacol, 113, 70, 10.1016/j.bcp.2016.05.014 Charfi, 2014, Ligand- and cell-dependent determinants of internalization and cAMP modulation by delta opioid receptor (DOR) agonists, Cell Mol Life Sci, 71, 1529, 10.1007/s00018-013-1461-7 Kenakin, 2010, Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery, Pharmacol Rev, 62, 265, 10.1124/pr.108.000992 Kofuku, 2012, Efficacy of the beta(2)-adrenergic receptor is determined by conformational equilibrium in the transmembrane region, Nat Commun, 3, 1045, 10.1038/ncomms2046 Nygaard, 2013, The dynamic process of beta(2)-adrenergic receptor activation, Cell, 152, 532, 10.1016/j.cell.2013.01.008 Sounier, 2015, Propagation of conformational changes during mu-opioid receptor activation, Nature, 524, 375, 10.1038/nature14680 Manglik, 2015, Structural insights into the dynamic process of beta2-adrenergic receptor signaling, Cell, 161, 1101, 10.1016/j.cell.2015.04.043 Staus, 2016, Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation, Nature, 535, 448, 10.1038/nature18636 Rasmussen, 2011, Crystal structure of the beta2 adrenergic receptor-Gs protein complex, Nature, 477, 549, 10.1038/nature10361 Kang, 2015, Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser, Nature, 523, 561, 10.1038/nature14656 Okude, 2015, Identification of a conformational equilibrium that determines the efficacy and functional selectivity of the mu-opioid receptor, Angew Chem Int Ed Engl, 54, 15771, 10.1002/anie.201508794 Alvarez, 2002, mu-Opioid receptors: ligand-dependent activation of potassium conductance, desensitization, and internalization, J Neurosci, 22, 5769, 10.1523/JNEUROSCI.22-13-05769.2002 Ostrom, 2012, Choreographing the adenylyl cyclase signalosome: sorting out the partners and the steps, Naunyn Schmiedebergs Arch Pharmacol, 385, 5, 10.1007/s00210-011-0696-9 Thompson, 2015, Biased agonism of endogenous opioid peptides at the mu-opioid receptor, Mol Pharmacol, 88, 335, 10.1124/mol.115.098848 Shenoy, 2006, Beta-arrestin-dependent, G protein-independent ERK1/2 activation by the beta2 adrenergic receptor, J Biol Chem, 281, 1261, 10.1074/jbc.M506576200 Blanchet, 2002, Desensitization of mu-opioid receptor-evoked potassium currents: initiation at the receptor, expression at the effector, Proc Natl Acad Sci U S A, 99, 4674, 10.1073/pnas.072075399 Guo, 2014, Drug-target residence time—a case for G protein-coupled receptors, Med Res Rev, 34, 856, 10.1002/med.21307 Masuho, 2015, Distinct profiles of functional discrimination among G proteins determine the actions of G protein-coupled receptors, Sci Signal, 8, ra123, 10.1126/scisignal.aab4068 Raehal, 2005, Morphine side effects in beta-arrestin 2 knockout mice, J Pharmacol Exp Ther, 314, 1195, 10.1124/jpet.105.087254 DeWire, 2013, A G protein-biased ligand at the mu-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine, J Pharmacol Exp Ther, 344, 708, 10.1124/jpet.112.201616 Manglik, 2016, Structure-based discovery of opioid analgesics with reduced side effects, Nature, 537, 185, 10.1038/nature19112 Soergel, 2014, Biased agonism of the mu-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: a randomized, double-blind, placebo-controlled, crossover study in healthy volunteers, Pain, 155, 1829, 10.1016/j.pain.2014.06.011 Viscusi, 2016, A randomized, phase 2 study investigating TRV130, a biased ligand of the mu-opioid receptor, for the intravenous treatment of acute pain, Pain, 157, 264, 10.1097/j.pain.0000000000000363 Allen, 2011, Discovery of beta-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy, Proc Natl Acad Sci U S A, 108, 18488, 10.1073/pnas.1104807108 Rankovic, 2016, Biased agonism: an emerging paradigm in GPCR drug discovery, Bioorg Med Chem Lett, 26, 241, 10.1016/j.bmcl.2015.12.024 Wacker, 2013, Structural features for functional selectivity at serotonin receptors, Science, 340, 615, 10.1126/science.1232808 Allouche, 1999, Differential G-protein activation by alkaloid and peptide opioid agonists in the human neuroblastoma cell line SK-N-BE, Biochem J, 342, 71, 10.1042/bj3420071 Soto, 2015, N-linked glycosylation of protease-activated receptor-1 at extracellular loop 2 regulates G-protein signaling bias, Proc Natl Acad Sci U S A, 112, E3600, 10.1073/pnas.1508838112 Gazi, 2003, Functional coupling of the human dopamine D2 receptor with G alpha i1, G alpha i2, G alpha i3 and G alpha o G proteins: evidence for agonist regulation of G protein selectivity, Br J Pharmacol, 138, 775, 10.1038/sj.bjp.0705116 Karpinsky-Semper, 2014, Differential effects of the Gbeta5-RGS7 complex on muscarinic M3 receptor-induced Ca2+ influx and release, Mol Pharmacol, 85, 758, 10.1124/mol.114.091843 Lin, 2011, Understanding molecular recognition by G protein betagamma subunits on the path to pharmacological targeting, Mol Pharmacol, 80, 551, 10.1124/mol.111.073072 Pineyro, 2009, Membrane signalling complexes: implications for development of functionally selective ligands modulating heptahelical receptor signalling, Cell Signal, 21, 179, 10.1016/j.cellsig.2008.08.013 Nikolaev, 2006, Molecular basis of partial agonism at the neurotransmitter alpha2 A-adrenergic receptor and Gi-protein heterotrimer, J Biol Chem, 281, 24506, 10.1074/jbc.M603266200 Gales, 2005, Real-time monitoring of receptor and G-protein interactions in living cells, Nat Methods, 2, 177, 10.1038/nmeth743 Audet, 2008, Bioluminescence resonance energy transfer assays reveal ligand-specific conformational changes within preformed signaling complexes containing delta-opioid receptors and heterotrimeric G proteins, J Biol Chem, 283, 15078, 10.1074/jbc.M707941200 Richard-Lalonde, 2013, Conformational dynamics of Kir3.1/Kir3.2 channel activation via delta-opioid receptors, Mol Pharmacol, 83, 416, 10.1124/mol.112.081950 Riven, 2006, GIRK channel activation involves a local rearrangement of a preformed G protein channel complex, Neuron, 51, 561, 10.1016/j.neuron.2006.08.017 Zimmerman, 2012, Differential beta-arrestin-dependent conformational signaling and cellular responses revealed by angiotensin analogs, Sci Signal, 5, ra33, 10.1126/scisignal.2002522 Ko, 2014, Concise review: drug discovery in the age of the induced pluripotent stem cell, Stem Cells Transl Med, 3, 500, 10.5966/sctm.2013-0162 Stallaert, 2012, Impedance responses reveal beta(2)-adrenergic receptor signaling pluridimensionality and allow classification of ligands with distinct signaling profiles, PLoS ONE, 7, e29420, 10.1371/journal.pone.0029420 Morse, 2013, Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family, BMC Pharmacol Toxicol, 14, 17, 10.1186/2050-6511-14-17