Biased Allosteric Modulators: New Frontiers in GPCR Drug Discovery.

[1]  W. Wetsel,et al.  β-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors , 2020, Cell.

[2]  John D. McCorvy,et al.  “TRUPATH, an Open-Source Biosensor Platform for Interrogating the GPCR Transducerome” , 2020, Nature Chemical Biology.

[3]  J. R. Lane,et al.  Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists , 2020, Science Signaling.

[4]  Shaoyong Lu,et al.  Combining Allosteric and Orthosteric Drugs to Overcome Drug Resistance. , 2020, Trends in pharmacological sciences.

[5]  M. Mckee,et al.  Estimated Research and Development Investment Needed to Bring a New Medicine to Market, 2009-2018. , 2020, JAMA.

[6]  K. Caron,et al.  Dawn of a New RAMPage. , 2020, Trends in pharmacological sciences.

[7]  Shuguang Yuan,et al.  Enhancing the Signaling of GPCRs via Orthosteric Ions , 2020, ACS central science.

[8]  G. Tall,et al.  The GPCR accessory protein MRAP2 regulates both biased signaling and constitutive activity of the ghrelin receptor GHSR1a , 2020, Science Signaling.

[9]  M. Jackson,et al.  Discovery of b-Arrestin Biased, Orally Bioavailable and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators. , 2019, Journal of medicinal chemistry.

[10]  R. Russell,et al.  Illuminating G-Protein-Coupling Selectivity of GPCRs , 2019, Cell.

[11]  Kathryn E. Livingston,et al.  The δ‐opioid receptor positive allosteric modulator BMS 986187 is a G‐protein‐biased allosteric agonist , 2019, British journal of pharmacology.

[12]  Jamie Munro,et al.  Trends in clinical success rates and therapeutic focus , 2019, Nature Reviews Drug Discovery.

[13]  A. Poupon,et al.  Biased Signaling and Allosteric Modulation at the FSHR , 2019, Front. Endocrinol..

[14]  Shaoyong Lu,et al.  Allosteric Modulator Discovery: From Serendipity to Structure-Based Design. , 2019, Journal of medicinal chemistry.

[15]  Caitlin E. Scott,et al.  Pyrimidinyl Biphenylureas Act as Allosteric Modulators to Activate Cannabinoid Receptor 1 and Initiate β-Arrestin–Dependent Responses , 2018, Molecular Pharmacology.

[16]  W. Koch,et al.  Pepducin-mediated cardioprotection via β-arrestin-biased β2-adrenergic receptor-specific signaling , 2018, Theranostics.

[17]  P. Sexton,et al.  Toward an understanding of the structural basis of allostery in muscarinic acetylcholine receptors , 2018, The Journal of general physiology.

[18]  Y. Tao,et al.  Fenoprofen-An Old Drug Rediscovered as a Biased Allosteric Enhancer for Melanocortin Receptors. , 2018, ACS chemical neuroscience.

[19]  Ryan T. Strachan,et al.  PAM-Antagonists: A Better Way to Block Pathological Receptor Signaling? , 2018, Trends in pharmacological sciences.

[20]  Paul A. Insel,et al.  G Protein-Coupled Receptors as Targets for Approved Drugs: How Many Targets and How Many Drugs? , 2018, Molecular Pharmacology.

[21]  J. Steyaert,et al.  A Genetically Encoded Biosensor Reveals Location Bias of Opioid Drug Action , 2018, Neuron.

[22]  Sudarshan Rajagopal,et al.  Biased signalling: from simple switches to allosteric microprocessors , 2018, Nature Reviews Drug Discovery.

[23]  E. Kostenis,et al.  Temporal Bias: Time-Encoded Dynamic GPCR Signaling. , 2017, Trends in pharmacological sciences.

[24]  David E. Gloriam,et al.  Trends in GPCR drug discovery: new agents, targets and indications , 2017, Nature Reviews Drug Discovery.

[25]  B. Hudson,et al.  A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias , 2017, Scientific Reports.

[26]  Kyle V. Butler,et al.  Structure-inspired design of β-arrestin-biased ligands for aminergic GPCRs , 2017, Nature chemical biology.

[27]  M. Congreve,et al.  Applying Structure-Based Drug Design Approaches to Allosteric Modulators of GPCRs. , 2017, Trends in pharmacological sciences.

[28]  J. Senard,et al.  G protein stoichiometry dictates biased agonism through distinct receptor-G protein partitioning , 2017, Scientific Reports.

[29]  T. Kenakin The Quantitative Characterization of Functional Allosteric Effects , 2017, Current protocols in pharmacology.

[30]  S. Rajagopal,et al.  A Practical Guide to Approaching Biased Agonism at G Protein Coupled Receptors , 2017, Front. Neurosci..

[31]  D. Kendall,et al.  Pyrimidinyl Biphenylureas: Identification of New Lead Compounds as Allosteric Modulators of the Cannabinoid Receptor CB1. , 2017, Journal of medicinal chemistry.

[32]  Tudor I. Oprea,et al.  A comprehensive map of molecular drug targets , 2016, Nature Reviews Drug Discovery.

[33]  T. Gamage,et al.  CB1 Allosteric Modulator Org27569 Is an Antagonist/Inverse Agonist of ERK1/2 Signaling , 2016, Cannabis and cannabinoid research.

[34]  R. Rodriguiz,et al.  Distinct cortical and striatal actions of a β-arrestin–biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties , 2016, Proceedings of the National Academy of Sciences.

[35]  M. Perretti,et al.  Old drugs with new skills: fenoprofen as an allosteric enhancer at melanocortin receptor 3 , 2016, Cellular and Molecular Life Sciences.

[36]  Ashley M. Miller,et al.  A Novel Allosteric Activator of Free Fatty Acid 2 Receptor Displays Unique Gi-functional Bias* , 2016, The Journal of Biological Chemistry.

[37]  J. Cheung,et al.  β-arrestin–biased signaling through the β2-adrenergic receptor promotes cardiomyocyte contraction , 2016, Proceedings of the National Academy of Sciences.

[38]  R. Rodriguiz,et al.  ML314: A Biased Neurotensin Receptor Ligand for Methamphetamine Abuse. , 2016, ACS chemical biology.

[39]  J. Benovic,et al.  From biased signalling to polypharmacology: unlocking unique intracellular signalling using pepducins. , 2016, Biochemical Society transactions.

[40]  Ruben Abagyan,et al.  Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor , 2016, Cell Research.

[41]  Arthur Christopoulos,et al.  The role of kinetic context in apparent biased agonism at GPCRs , 2016, Nature Communications.

[42]  B. Rosengren,et al.  AZD8797 is an allosteric non-competitive modulator of the human CX3CR1 receptor , 2015, The Biochemical journal.

[43]  P. Sexton,et al.  Biased Agonism and Biased Allosteric Modulation at the CB1 Cannabinoid Receptor , 2015, Molecular Pharmacology.

[44]  Violeta I. Pérez-Nueno,et al.  Studying the binding interactions of allosteric agonists and antagonists of the CXCR4 receptor. , 2015, Journal of molecular graphics & modelling.

[45]  Arthur Christopoulos,et al.  Novel Allosteric Modulators of G Protein-coupled Receptors* , 2015, The Journal of Biological Chemistry.

[46]  Kathryn E. Livingston,et al.  Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor. , 2015, Journal of medicinal chemistry.

[47]  Arthur Christopoulos,et al.  Endogenous Allosteric Modulators of G Protein–Coupled Receptors , 2015, The Journal of Pharmacology and Experimental Therapeutics.

[48]  Shailesh N Mistry,et al.  Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics , 2015, British journal of pharmacology.

[49]  Michel Bouvier,et al.  Development and Characterization of Pepducins as Gs-biased Allosteric Agonists*♦ , 2014, The Journal of Biological Chemistry.

[50]  J. Changeux,et al.  International Union of Basic and Clinical Pharmacology. XC. Multisite Pharmacology: Recommendations for the Nomenclature of Receptor Allosterism and Allosteric Ligands , 2014, Pharmacological Reviews.

[51]  Jens Meiler,et al.  Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders , 2014, Nature Reviews Drug Discovery.

[52]  Ryan T. Strachan,et al.  Allosteric Modulation of β-Arrestin-biased Angiotensin II Type 1 Receptor Signaling by Membrane Stretch* , 2014, The Journal of Biological Chemistry.

[53]  R. Lefkowitz,et al.  Recent developments in biased agonism. , 2014, Current opinion in cell biology.

[54]  S. Laporte,et al.  Allosteric and Biased G Protein-Coupled Receptor Signaling Regulation: Potentials for New Therapeutics , 2014, Front. Endocrinol..

[55]  L. Luttrell Minireview: More than just a hammer: ligand "bias" and pharmaceutical discovery. , 2014, Molecular endocrinology.

[56]  Bryan L. Roth,et al.  Molecular control of δ-opioid receptor signalling , 2014, Nature.

[57]  J. Benovic,et al.  Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein , 2013, Proceedings of the National Academy of Sciences.

[58]  J. Peters Polypharmacology - foe or friend? , 2013, Journal of medicinal chemistry.

[59]  M. Caron,et al.  Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor. , 2013, ACS medicinal chemistry letters.

[60]  J. Giraldo,et al.  Mechanistic analysis of the function of agonists and allosteric modulators: reconciling two‐state and operational models , 2013, British journal of pharmacology.

[61]  T. Hébert,et al.  GPCR heterodimers: asymmetries in ligand binding and signalling output offer new targets for drug discovery , 2013, British journal of pharmacology.

[62]  J. Shim,et al.  Distinct Roles of β-Arrestin 1 and β-Arrestin 2 in ORG27569-induced Biased Signaling and Internalization of the Cannabinoid Receptor 1 (CB1)* , 2013, The Journal of Biological Chemistry.

[63]  D. Bolognini,et al.  CB1 Receptor Allosteric Modulators Display Both Agonist and Signaling Pathway Specificity , 2013, Molecular Pharmacology.

[64]  S. Higashiyama,et al.  TGFα shedding assay: an accurate and versatile method for detecting GPCR activation , 2012, Nature Methods.

[65]  Brian K Shoichet,et al.  Structure-based drug screening for G-protein-coupled receptors. , 2012, Trends in pharmacological sciences.

[66]  K. Ahn,et al.  Allosteric Modulator ORG27569 Induces CB1 Cannabinoid Receptor High Affinity Agonist Binding State, Receptor Internalization, and Gi Protein-independent ERK1/2 Kinase Activation* , 2012, The Journal of Biological Chemistry.

[67]  Arthur Christopoulos,et al.  Signalling bias in new drug discovery: detection, quantification and therapeutic impact , 2012, Nature Reviews Drug Discovery.

[68]  Graeme Milligan,et al.  Allostery at G Protein-Coupled Receptor Homo- and Heteromers: Uncharted Pharmacological Landscapes , 2010, Pharmacological Reviews.

[69]  D. Devost,et al.  A Novel Biased Allosteric Compound Inhibitor of Parturition Selectively Impedes the Prostaglandin F2α-mediated Rho/ROCK Signaling Pathway* , 2010, The Journal of Biological Chemistry.

[70]  Keshava Rajagopal,et al.  Teaching old receptors new tricks: biasing seven-transmembrane receptors , 2010, Nature Reviews Drug Discovery.

[71]  Guide to Receptors and Channels (GRAC), 4th edition , 2009, British journal of pharmacology.

[72]  J. P. Kennedy,et al.  Synthesis and Structure–Activity Relationships of Allosteric Potentiators of the M4 Muscarinic Acetylcholine Receptor , 2009, ChemMedChem.

[73]  P. Sexton,et al.  Receptor activity-modifying proteins differentially modulate the G protein-coupling efficiency of amylin receptors. , 2008, Endocrinology.

[74]  H. Schiöth,et al.  Structural diversity of G protein-coupled receptors and significance for drug discovery , 2008, Nature Reviews Drug Discovery.

[75]  P. Sexton,et al.  Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology. , 2007, Trends in pharmacological sciences.

[76]  T. Fujita,et al.  An acquired hypocalciuric hypercalcemia autoantibody induces allosteric transition among active human Ca-sensing receptor conformations , 2007, Proceedings of the National Academy of Sciences.

[77]  J. Pelletier,et al.  High-Throughput Screening of G Protein-Coupled Receptor Antagonists Using a Bioluminescence Resonance Energy Transfer 1-Based β-Arrestin2 Recruitment Assay , 2005, Journal of biomolecular screening.

[78]  P. Sexton,et al.  Novel Receptor Partners and Function of Receptor Activity-modifying Proteins* , 2003, The Journal of Biological Chemistry.

[79]  S. Angers,et al.  Detection of beta 2-adrenergic receptor dimerization in living cells using bioluminescence resonance energy transfer (BRET). , 2000, Proceedings of the National Academy of Sciences of the United States of America.

[80]  T. Kenakin,et al.  Agonist-receptor efficacy. II. Agonist trafficking of receptor signals. , 1995, Trends in pharmacological sciences.

[81]  J. Changeux,et al.  ON THE NATURE OF ALLOSTERIC TRANSITIONS: A PLAUSIBLE MODEL. , 1965, Journal of molecular biology.

[82]  Claude E. Shannon,et al.  The mathematical theory of communication , 1950 .

[83]  C. E. SHANNON,et al.  A mathematical theory of communication , 1948, MOCO.

[84]  J. Giraldo Operational models of allosteric modulation: caution is needed. , 2015, Trends in pharmacological sciences.

[85]  Arthur Christopoulos,et al.  Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders , 2009, Nature Reviews Drug Discovery.