Functional selectivity profiling of the angiotensin II type 1 receptor using pathway-wide BRET signaling sensors

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Angiotensin II Signal Transduction: An Update on Mechanisms of Physiology and Pathophysiology

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Lifetime of muscarinic receptor–G-protein complexes determines coupling efficiency and G-protein subtype selectivity

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Structure and dynamics of GPCR signaling complexes

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Manifold roles of β-arrestins in GPCR signaling elucidated with siRNA and CRISPR/Cas9

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Type 2 diabetes–associated variants of the MT2melatonin receptor affect distinct modes of signaling

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FZD5 is a Gαq-coupled receptor that exhibits the functional hallmarks of prototypical GPCRs

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Biased ligand of the angiotensin II type 1 receptor in patients with acute heart failure: a randomized, double-blind, placebo-controlled, phase IIB, dose ranging trial (BLAST-AHF)

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Signaling bias in drug discovery

(2017) Terry Kenakin   Expert Opinion on Drug Discovery

Conformational Profiling of the AT1 Angiotensin II Receptor Reflects Biased Agonism, G Protein Coupling, and Cellular Context

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A kinetic view of GPCR allostery and biased agonism

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Evolutionary action and structural basis of the allosteric switch controlling β2AR functional selectivity

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G protein stoichiometry dictates biased agonism through distinct receptor-G protein partitioning

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Ang-(1-7) is an endogenous β-arrestin-biased agonist of the AT1 receptor with protective action in cardiac hypertrophy

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Cardioprotective Angiotensin-(1–7) Peptide Acts as a Natural-Biased Ligand at the Angiotensin II Type 1 ReceptorNovelty and Significance

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Quantifying biased signaling in GPCRs using BRET-based biosensors

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The conformational signature of β-arrestin2 predicts its trafficking and signalling functions

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Monitoring G protein-coupled receptor and β-arrestin trafficking in live cells using enhanced bystander BRET

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The role of kinetic context in apparent biased agonism at GPCRs

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Structural Insights into the Dynamic Process of β 2 -Adrenergic Receptor Signaling

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Identification of Distinct Conformations of the Angiotensin-II Type 1 Receptor Associated with the Gq/11Protein Pathway and the β-Arrestin Pathway Using Molecular Dynamics Simulations

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Structural Basis for Ligand Recognition and Functional Selectivity at Angiotensin Receptor

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Elucidation of G-protein and β-arrestin functional selectivity at the dopamine D2 receptor

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Distinct profiles of functional discrimination among G proteins determine the actions of G protein–coupled receptors

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The experimental power of FR900359 to study Gq-regulated biological processes

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Distinct profiles of functional discrimination among G proteins determine the actions of G protein–coupled receptors

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A century old renin–angiotensin system still grows with endless possibilities: AT1 receptor signaling cascades in cardiovascular physiopathology

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Angiotensin II Type I and Prostaglandin F2α Receptors Cooperatively Modulate Signaling in Vascular Smooth Muscle Cells

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The Dynamic Process of β2-Adrenergic Receptor Activation

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Structure of the Human Angiotensin II Type 1 (AT1) Receptor Bound to Angiotensin II from Multiple Chemoselective Photoprobe Contacts Reveals a Unique Peptide Binding Mode

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Insights into AT1 Receptor Activation through AngII Binding Studies

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First Clinical Experience with TRV027: Pharmacokinetics and Pharmacodynamics in Healthy Volunteers

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

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Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein

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AT1mutations and risk of atrial fibrillation based on genotypes from 71 000 individuals from the general population

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Deciphering biased-agonism complexity reveals a new active AT1 receptor entity

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Differential  -Arrestin-Dependent Conformational Signaling and Cellular Responses Revealed by Angiotensin Analogs

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Expression of G protein-coupled receptors and related proteins in HEK293, AtT20, BV2, and N18 cell lines as revealed by microarray analysis

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Protein Kinase C: The "Masters" of Calcium and Lipid

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Differential association modes of the thrombin receptor PAR1 with Gαi1, Gα12, and β-arrestin 1

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Selectively Engaging  -Arrestins at the Angiotensin II Type 1 Receptor Reduces Blood Pressure and Increases Cardiac Performance

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A single-nucleotide polymorphism of alanine to threonine at position 163 of the human angiotensin II type 1 receptor impairs Losartan affinity

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Therapeutic potential of β-arrestin- and G protein-biased agonists

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Functional Selectivity of Natural and Synthetic Prostaglandin EP4 Receptor Ligands

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G protein βγ subunits: Central mediators of G protein-coupled receptor signaling

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