Novel Allosteric Modulators of G Protein-coupled Receptors

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Allosteric proteins and cellular control systems

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The ensemble nature of allostery

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Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

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G Protein-Coupled Receptor Allosterism and Complexing

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Activation and allosteric modulation of a muscarinic acetylcholine receptor

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Trends in the exploitation of novel drug targets

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Signalling bias in new drug discovery: detection, quantification and therapeutic impact

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Structure of the CCR5 Chemokine Receptor–HIV Entry Inhibitor Maraviroc Complex

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Biased Signaling Pathways in β 2 -Adrenergic Receptor Characterized by 19 F-NMR

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Allosteric binding sites on cell-surface receptors: novel targets for drug discovery

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Molecular Mechanism of β-Arrestin-Biased Agonism at Seven-Transmembrane Receptors

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Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

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Structure of a Class C GPCR Metabotropic Glutamate Receptor 1 Bound to an Allosteric Modulator

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l -Amino acid sensing by the extracellular Ca 2+ -sensing receptor

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Emerging paradigms in GPCR allostery: implications for drug discovery

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Structure of class B GPCR corticotropin-releasing factor receptor 1

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Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs

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Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain

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Beyond Desensitization: Physiological Relevance of Arrestin-Dependent Signaling

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Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology

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Modification of the binding properties of muscarinic receptors by gallamine.

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G protein‐coupled receptor hetero‐dimerization: contribution to pharmacology and function

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Allostery: an illustrated definition for the ‘second secret of life’

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New Concepts in Drug Discovery: Collateral Efficacy and Permissive Antagonism

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Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders

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THE INHIBITORY EFFECT OF GALLAMINE ON MUSCARINIC RECEPTORS

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Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs

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International Union of Basic and Clinical Pharmacology. XC. Multisite Pharmacology: Recommendations for the Nomenclature of Receptor Allosterism and Allosteric Ligands

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Allosteric modulation of the muscarinic M 4 receptor as an approach to treating schizophrenia

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Structural basis of function in heterotrimeric G proteins

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Agonist-Receptor-Arrestin, an Alternative Ternary Complex with High Agonist Affinity

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An allosteric modulator to control endogenous G protein-coupled receptors with light

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Discovery of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Reveals Chemical and Functional Diversity and In Vivo Activity in Rat Behavioral Models of Anxiolytic and Antipsychotic Activity

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A Novel Mechanism of G Protein-coupled Receptor Functional Selectivity

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A nonpeptidic agonist of glucagon-like peptide 1 receptors with efficacy in diabetic db / db mice

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A Novel Selective Allosteric Modulator Potentiates the Activity of Native Metabotropic Glutamate Receptor Subtype 5 in Rat Forebrain

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The Best of Both Worlds? Bitopic Orthosteric/Allosteric Ligands of G Protein–Coupled Receptors

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Molecular Mechanisms of Action and In Vivo Validation of an M4 Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties

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“Molecular Switches” on mGluR Allosteric Ligands That Modulate Modes of Pharmacology

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Endogenous Allosteric Modulators of G Protein–Coupled Receptors

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Reversing systemic inflammatory response syndrome with chemokine receptor pepducins

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BRET analysis of GPCR oligomerization: newer does not mean better

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Functional Impact of Allosteric Agonist Activity of Selective Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 in Regulating Central Nervous System Function

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Subtype-Selective Positive Cooperative Interactions between Brucine Analogues and Acetylcholine at Muscarinic Receptors: Radioligand Binding Studies

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Allosteric modulation of metabotropic glutamate receptors: Structural insights and therapeutic potential

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Structure of C lass B GPCRs : new horizons for drug discovery

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Rational design of dualsteric GPCR ligands: quests and promise

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Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist

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Proteinase‐activated receptor‐4: evaluation of tethered ligand‐derived peptides as probes for receptor function and as inflammatory agonists in vivo

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Allosteric Modulation of Muscarinic Acetylcholine Receptors

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ALLOSTERIC INTERACTIONS AT MUSCARINIC CHOLINOCEPTORS

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Allosteric Interactions of Staurosporine and Other Indolocarbazoles withN-[methyl-3H]Scopolamine and Acetylcholine at Muscarinic Receptor Subtypes: Identification of a Second Allosteric Site

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Three Adjacent Serines in the Extracellular Domains of the CaR Are Required for l-Amino Acid-mediated Potentiation of Receptor Function

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Thiochrome Enhances Acetylcholine Affinity at Muscarinic M4 Receptors: Receptor Subtype Selectivity via Cooperativity Rather than Affinity

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Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 5 Have Differential Effects on Different Signaling Pathways in Cortical Astrocytes

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Advancing the Drug Discovery and Development Process

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N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hydroxybenzamide (CPPHA) Acts through a Novel Site as a Positive Allosteric Modulator of Group 1 Metabotropic Glutamate Receptors

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A Novel Multivalent Ligand That Bridges the Allosteric and Orthosteric Binding Sites of the M2 Muscarinic Receptor

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Fluorine-19 NMR of integral membrane proteins illustrated with studies of GPCRs

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Advancing the Drug Discovery and Development Process

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Mechanisms of steric and cooperative actions of alcuronium on cardiac muscarinic acetylcholine receptors.

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Analogs of WIN 62,577 Define a Second Allosteric Site on Muscarinic Receptors

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Conformational Rearrangements and Signaling Cascades Involved in Ligand-Biased Mitogen-Activated Protein Kinase Signaling through the β1-Adrenergic Receptor

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An Intracellular Allosteric Site for a Specific Class of Antagonists of the CC Chemokine G Protein-Coupled Receptors CCR4 and CCR5

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Interaction of Novel Positive Allosteric Modulators of Metabotropic Glutamate Receptor 5 with the Negative Allosteric Antagonist Site Is Required for Potentiation of Receptor Responses

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A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification

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Differential Activation and Modulation of the Glucagon-Like Peptide-1 Receptor by Small Molecule Ligands

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A common intracellular allosteric binding site for antagonists of the CXCR2 receptor

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Identification of a Putative Intracellular Allosteric Antagonist Binding-Site in the CXC Chemokine Receptors 1 and 2

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Inhibition of the actions of carbachol and DFP on guinea pig isolated atria by alkane-bis-ammonium compounds

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A Fully Human, Allosteric Monoclonal Antibody That Activates the Insulin Receptor and Improves Glycemic Control

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A Novel Metabotropic Glutamate Receptor 5 Positive Allosteric Modulator Acts at a Unique Site and Confers Stimulus Bias to mGlu5 Signaling

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A Virtual Screening Hit Reveals New Possibilities for Developing Group III Metabotropic Glutamate Receptor Agonists

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Discovery of a Novel Chemical Class of mGlu 5 Allosteric Ligands with Distinct Modes of Pharmacology

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Challenges in the development of mGluR5 positive allosteric modulators: The discovery of CPPHA

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Allosteric Modulation of β-Arrestin-biased Angiotensin II Type 1 Receptor Signaling by Membrane Stretch

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Allostery in GPCRs: ‘MWC’ revisited

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A Double Mutation in the Extracellular Ca2+-sensing Receptor's Venus Flytrap Domain That Selectively Disables l-Amino Acid Sensing

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Pharmacological folding chaperones act as allosteric ligands of Frizzled4

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Detailed Mechanistic Analysis of Gevokizumab, an Allosteric Anti–IL-1β Antibody with Differential Receptor-Modulating Properties

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