The role of kinetic context in apparent biased agonism at GPCRs
暂无分享,去创建一个
Arthur Christopoulos | Patrick M Sexton | Jonathan A Javitch | Ben Capuano | Thomas Coudrat | Meritxell Canals | P. Sexton | A. Christopoulos | J. R. Lane | J. Javitch | S. Charlton | P. Donthamsetti | D. Sykes | P. Scammells | M. Canals | Jeremy Shonberg | Jeremy Shonberg | B. Capuano | J Robert Lane | Thomas Coudrat | Steven J Charlton | Peter J Scammells | Prashant Donthamsetti | David A Sykes | Carmen Klein Herenbrink | Carmen Klein Herenbrink | R. Lane | Meritxell Canals
[1] Arthur Christopoulos,et al. Biased Agonism at G Protein‐Coupled Receptors: The Promise and the Challenges—A Medicinal Chemistry Perspective , 2014, Medicinal research reviews.
[2] M. Dowling,et al. Investigating the molecular mechanisms through which FTY 720P causes persistent S 1 P 1 receptor internalisation 1 , 2014 .
[3] L. Mahan,et al. Correction to “The Kinetics of Competitive Radioligand Binding Predicted by the Law of Mass Action” , 2014, Molecular Pharmacology.
[4] J. Violin,et al. Erratum: Biased ligands at G protein-coupled receptors: promise and progress:[Trends in Pharmacological Sciences 35 (2014) 308-316] , 2014 .
[5] J. Vilardaga. ENDOSOMAL GENERATION OF cAMP in GPCR SIGNALING , 2014, Nature chemical biology.
[6] J. Violin,et al. Biased ligands at G-protein-coupled receptors: promise and progress. , 2014, Trends in pharmacological sciences.
[7] Ralf C. Kling,et al. Functionally selective dopamine D₂, D₃ receptor partial agonists. , 2014, Journal of medicinal chemistry.
[8] O. Nosjean,et al. Prolonged Calcitonin Receptor Signaling by Salmon, but Not Human Calcitonin, Reveals Ligand Bias , 2014, PloS one.
[9] Arthur Christopoulos,et al. Quantification of Ligand Bias for Clinically Relevant β2-Adrenergic Receptor Ligands: Implications for Drug Taxonomy , 2014, Molecular Pharmacology.
[10] S. Durgam,et al. An evaluation of the safety and efficacy of cariprazine in patients with acute exacerbation of schizophrenia: A phase II, randomized clinical trial , 2014, Schizophrenia Research.
[11] I. Gaidarov,et al. Kinetics of 5-HT2B Receptor Signaling: Profound Agonist-Dependent Effects on Signaling Onset and Duration , 2013, The Journal of Pharmacology and Experimental Therapeutics.
[12] A. Christopoulos,et al. A structure-activity analysis of biased agonism at the dopamine D2 receptor. , 2013, Journal of medicinal chemistry.
[13] J. Violin,et al. Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. , 2013, Journal of medicinal chemistry.
[14] John Saunders,et al. Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists. , 2013, Journal of medicinal chemistry.
[15] R. Stevens,et al. Structural Features for Functional Selectivity at Serotonin Receptors , 2013, Science.
[16] A Multiplexed Fluorescent Calcium and NFAT Reporter Gene Assay to Identify GPCR Agonists , 2013, Current chemical genomics and translational medicine.
[17] Jonathan R. Tomshine,et al. Conformational biosensors reveal GPCR signalling from endosomes , 2013, Nature.
[18] Arthur Christopoulos,et al. Signalling bias in new drug discovery: detection, quantification and therapeutic impact , 2012, Nature Reviews Drug Discovery.
[19] R. Leurs,et al. Analysis of Multiple Histamine H4 Receptor Compound Classes Uncovers Gαi Protein- and β-Arrestin2-Biased Ligands , 2012, Molecular Pharmacology.
[20] J. L. Hansen,et al. Deciphering biased-agonism complexity reveals a new active AT1 receptor entity. , 2012, Nature chemical biology.
[21] A. IJzerman,et al. Functional efficacy of adenosine A2A receptor agonists is positively correlated to their receptor residence time , 2012, British journal of pharmacology.
[22] L. Carboni,et al. Slow dissociation of partial agonists from the D₂ receptor is linked to reduced prolactin release. , 2012, The international journal of neuropsychopharmacology.
[23] Christopher G. Tate,et al. Crystal Structures of a Stabilized β1-Adrenoceptor Bound to the Biased Agonists Bucindolol and Carvedilol , 2012, Structure.
[24] Eric Trinquet,et al. Structural insights into biased G protein-coupled receptor signaling revealed by fluorescence spectroscopy , 2012, Proceedings of the National Academy of Sciences.
[25] Arthur Christopoulos,et al. A simple method for quantifying functional selectivity and agonist bias. , 2012, ACS chemical neuroscience.
[26] Kurt Wüthrich,et al. Biased Signaling Pathways in β2-Adrenergic Receptor Characterized by 19F-NMR , 2012, Science.
[27] J. Dorn,et al. Impedance Responses Reveal β2-Adrenergic Receptor Signaling Pluridimensionality and Allow Classification of Ligands with Distinct Signaling Profiles , 2012, PloS one.
[28] Simon C. Potter,et al. A Genome-Wide Association Search for Type 2 Diabetes Genes in African Americans , 2012, PLoS ONE.
[29] Maria F. Sassano,et al. Discovery of β-Arrestin–Biased Dopamine D2 Ligands for Probing Signal Transduction Pathways Essential for Antipsychotic Efficacy , 2011, Proceedings of the National Academy of Sciences.
[30] Kunhong Xiao,et al. Multiple ligand-specific conformations of the β2-adrenergic receptor. , 2011, Nature chemical biology.
[31] Sudarshan Rajagopal,et al. Quantifying Ligand Bias at Seven-Transmembrane Receptors , 2011, Molecular Pharmacology.
[32] O. Rascol,et al. Pardoprunox in early Parkinson's disease: Results from 2 large, randomized double‐blind trials , 2011, Movement disorders : official journal of the Movement Disorder Society.
[33] R. Lefkowitz,et al. Therapeutic potential of β-arrestin- and G protein-biased agonists. , 2011, Trends in molecular medicine.
[34] P. Gmeiner,et al. Histidine 6.55 Is a Major Determinant of Ligand-Biased Signaling in Dopamine D2L Receptor , 2011, Molecular Pharmacology.
[35] Gaël Varoquaux,et al. Scikit-learn: Machine Learning in Python , 2011, J. Mach. Learn. Res..
[36] S. Charlton,et al. Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays , 2010, British journal of pharmacology.
[37] S. Charlton,et al. μ-Opioid Receptors: Correlation of Agonist Efficacy for Signalling with Ability to Activate Internalization , 2010, Molecular Pharmacology.
[38] P. Molinari,et al. Morphine-like Opiates Selectively Antagonize Receptor-Arrestin Interactions* , 2010, The Journal of Biological Chemistry.
[39] G. Cottrell,et al. Endosomes: A legitimate platform for the signaling train , 2009, Proceedings of the National Academy of Sciences.
[40] M. Dowling,et al. Exploring the Mechanism of Agonist Efficacy: A Relationship between Efficacy and Agonist Dissociation Rate at the Muscarinic M3 Receptor , 2009, Molecular Pharmacology.
[41] Bin Wang,et al. Sustained cyclic AMP production by parathyroid hormone receptor endocytosis. , 2009, Nature chemical biology.
[42] Heng Tao Shen,et al. Principal Component Analysis , 2009, Encyclopedia of Biometrics.
[43] R. Gainetdinov,et al. Antagonism of dopamine D2 receptor/β-arrestin 2 interaction is a common property of clinically effective antipsychotics , 2008, Proceedings of the National Academy of Sciences.
[44] S. Kapur,et al. Emerging drugs for schizophrenia , 2008, Expert opinion on emerging drugs.
[45] R. Copeland,et al. Residence time of receptor-ligand complexes and its effect on biological function. , 2008, Biochemistry.
[46] Robert J. Lefkowitz,et al. β-Arrestin-biased Agonism at the β2-Adrenergic Receptor* , 2008, Journal of Biological Chemistry.
[47] J. Violin,et al. beta-arrestin-biased agonism at the beta2-adrenergic receptor. , 2008, The Journal of biological chemistry.
[48] Robert J. Lefkowitz,et al. A unique mechanism of β-blocker action: Carvedilol stimulates β-arrestin signaling , 2007, Proceedings of the National Academy of Sciences.
[49] F. Ehlert,et al. Estimation of Agonist Activity at G Protein-Coupled Receptors: Analysis of M2 Muscarinic Receptor Signaling through Gi/o,Gs, and G15 , 2007, Journal of Pharmacology and Experimental Therapeutics.
[50] S. Rees,et al. Protean Agonism at the Dopamine D2 Receptor: (S)-3-(3-Hydroxyphenyl)-N-propylpiperidine Is an Agonist for Activation of Go1 but an Antagonist/Inverse Agonist for Gi1,Gi2, and Gi3 , 2007, Molecular Pharmacology.
[51] Arthur Christopoulos,et al. Functional Selectivity and Classical Concepts of Quantitative Pharmacology , 2007, Journal of Pharmacology and Experimental Therapeutics.
[52] J. Violin,et al. A unique mechanism of beta-blocker action: carvedilol stimulates beta-arrestin signaling. , 2007, Proceedings of the National Academy of Sciences of the United States of America.
[53] R. Mailman,et al. Aripiprazole has Functionally Selective Actions at Dopamine D2 Receptor-Mediated Signaling Pathways , 2007, Neuropsychopharmacology.
[54] John P. Overington,et al. How many drug targets are there? , 2006, Nature Reviews Drug Discovery.
[55] M. Bouvier,et al. Distinct Signaling Profiles of β1 and β2 Adrenergic Receptor Ligands toward Adenylyl Cyclase and Mitogen-Activated Protein Kinase Reveals the Pluridimensionality of Efficacy , 2006, Molecular Pharmacology.
[56] Olivier Lichtarge,et al. β-Arrestin-dependent, G Protein-independent ERK1/2 Activation by the β2 Adrenergic Receptor* , 2006, Journal of Biological Chemistry.
[57] Olivier Lichtarge,et al. beta-arrestin-dependent, G protein-independent ERK1/2 activation by the beta2 adrenergic receptor. , 2006, The Journal of biological chemistry.
[58] R. Langer,et al. Exploring polyethylenimine‐mediated DNA transfection and the proton sponge hypothesis , 2005, The journal of gene medicine.
[59] R. Lefkowitz,et al. Differential Kinetic and Spatial Patterns of β-Arrestin and G Protein-mediated ERK Activation by the Angiotensin II Receptor* , 2004, Journal of Biological Chemistry.
[60] S. Nickolls,et al. Functional coupling of the human dopamine D2 receptor with Gαi1, Gαi2, Gαi3 and Gαo G proteins: evidence for agonist regulation of G protein selectivity , 2003 .
[61] S. Nickolls,et al. 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. , 2003, British journal of pharmacology.
[62] C. Tamminga,et al. Antipsychotic Properties of the Partial Dopamine Agonist (−)-3-(3-Hydroxyphenyl)-N-n-Propylpiperidine (Preclamol) in Schizophrenia , 1998, Biological Psychiatry.
[63] Abraham Nudelman,et al. NMR Chemical Shifts of Common Laboratory Solvents as Trace Impurities. , 1997, The Journal of organic chemistry.
[64] C. Marsden,et al. The thermodynamics of agonist and antagonist binding to dopamine D-2 receptors. , 1986, Molecular pharmacology.
[65] J. Black,et al. Operational models of pharmacological agonism , 1983, Proceedings of the Royal Society of London. Series B. Biological Sciences.
[66] D. Sibley,et al. Dopamine receptor binding on intact cells. Absence of a high-affinity agonist-receptor binding state. , 1983, Molecular Pharmacology.
[67] D. Mackay. A Critical Survey of Receptor Theories of Drug Action , 1977 .
[68] Y. Cheng,et al. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. , 1973, Biochemical pharmacology.
[69] A. Hill. The mode of action of nicotine and curari, determined by the form of the contraction curve and the method of temperature coefficients , 1909, The Journal of physiology.