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

Pharmacological reviews, 2010-06, Vol.62 (2), p.265-304

2010

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Structural Basis for Allosteric Modulation of Class B G Protein-Coupled Receptors

Annual review of pharmacology and toxicology, 2020-01, Vol.60 (1), p.89-107

2020

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Changes in the plasma membrane in metabolic disease: impact of the membrane environment on G protein‐coupled receptor structure and function

British journal of pharmacology, 2018-11, Vol.175 (21), p.4009-4025

2018

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Phase-plate cryo-EM structure of a class B GPCR-G-protein complex

Nature (London), 2017-06, Vol.546 (7656), p.118-123

2017

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Allostery and Biased Agonism at Class B G Protein-Coupled Receptors

Chemical reviews, 2017-01, Vol.117 (1), p.111-138

2017

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Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor–Gs complex

Nature (London), 2018-03, Vol.555 (7694), p.121-125

2018

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Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes

Pharmacological reviews, 2016-10, Vol.68 (4), p.954-1013

2016

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The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism

Cell, 2016-06, Vol.165 (7), p.1632-1643

2016

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Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists

Molecular cell, 2020-11, Vol.80 (3), p.485-500.e7

2020

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Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor

Nature (London), 2018-09, Vol.561 (7724), p.492-497

2018

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Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations

Proceedings of the National Academy of Sciences - PNAS, 2013-03, Vol.110 (13), p.5211-5216

2013

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Activation of the GLP-1 receptor by a non-peptidic agonist

Nature (London), 2020-01, Vol.577 (7790), p.432-436

2020

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Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity

PLoS biology, 2021-06, Vol.19 (6), p.e3001295

2021

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Targeting VIP and PACAP Receptor Signaling: New Insights into Designing Drugs for the PACAP Subfamily of Receptors

International journal of molecular sciences, 2022-07, Vol.23 (15), p.8069

2022

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Impact of secretin receptor homo-dimerization on natural ligand binding

Nature communications, 2024-05, Vol.15 (1), p.4390-4390, Article 4390

2024

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Crystal structure of the Frizzled 4 receptor in a ligand-free state

Nature (London), 2018-08, Vol.560 (7720), p.666-670

2018

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Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening

Molecular pharmacology, 2010-09, Vol.78 (3), p.456-465

2010

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Wnt5a promotes Frizzled-4 signalosome assembly by stabilizing cysteine-rich domain dimerization

Genes & development, 2017-05, Vol.31 (9), p.916-926

2017

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Structure and dynamics of the active Gs-coupled human secretin receptor

Nature communications, 2020-08, Vol.11 (1), p.1-17, Article 4137

2020

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Cholesterol-dependent dynamic changes in the conformation of the type 1 cholecystokinin receptor affect ligand binding and G protein coupling

PLoS biology, 2024-07, Vol.22 (7), p.e3002673

2024

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Spatial intensity distribution analysis quantifies the extent and regulation of homodimerization of the secretin receptor

Biochemical journal, 2017-05, Vol.474 (11), p.1879-1895

2017

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Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery

Pharmacological reviews, 2010-06, Vol.62 (2), p.265

2010

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Roles of Cholecystokinin in the Nutritional Continuum. Physiology and Potential Therapeutics

Frontiers in endocrinology (Lausanne), 2021-06, Vol.12, p.684656-684656

2021

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Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation

Molecular pharmacology, 2011-09, Vol.80 (3), p.486-497

2011

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Mechanism of Action and Structure-Activity Relationships of Tetracyclic Small Molecules Acting as Universal Positive Allosteric Modulators of the Cholecystokinin Receptor

Membranes (Basel), 2023-01, Vol.13 (2), p.150

2023

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

Structural Basis for Allosteric Modulation of Class B G Protein-Coupled Receptors

Changes in the plasma membrane in metabolic disease: impact of the membrane environment on G protein‐coupled receptor structure and function

Phase-plate cryo-EM structure of a class B GPCR-G-protein complex

Allostery and Biased Agonism at Class B G Protein-Coupled Receptors

Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor–Gs complex

Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes

The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism

Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists

Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor

Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations

Activation of the GLP-1 receptor by a non-peptidic agonist

Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity

Targeting VIP and PACAP Receptor Signaling: New Insights into Designing Drugs for the PACAP Subfamily of Receptors

Impact of secretin receptor homo-dimerization on natural ligand binding

Crystal structure of the Frizzled 4 receptor in a ligand-free state

Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening

Wnt5a promotes Frizzled-4 signalosome assembly by stabilizing cysteine-rich domain dimerization

Structure and dynamics of the active Gs-coupled human secretin receptor

Cholesterol-dependent dynamic changes in the conformation of the type 1 cholecystokinin receptor affect ligand binding and G protein coupling

Spatial intensity distribution analysis quantifies the extent and regulation of homodimerization of the secretin receptor

Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery

Roles of Cholecystokinin in the Nutritional Continuum. Physiology and Potential Therapeutics

Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation

Mechanism of Action and Structure-Activity Relationships of Tetracyclic Small Molecules Acting as Universal Positive Allosteric Modulators of the Cholecystokinin Receptor

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