Unique Positive Cooperativity Between the β-Arrestin–Biased β-Blocker Carvedilol and a Small Molecule Positive Allosteric Modulator of the β2-Adrenergic Receptor

β-Arrestin–Biased Allosteric Modulator Potentiates Carvedilol-Stimulated β Adrenergic Receptor Cardioprotection

(2021) Jialu Wang et al.   MOLECULAR PHARMACOLOGY

The β-arrestin-biased β-adrenergic receptor blocker carvedilol enhances skeletal muscle contractility

(2020) Jihee Kim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Mechanism of β2AR regulation by an intracellular positive allosteric modulator

(2019) Xiangyu Liu et al.   SCIENCE

Toward G protein-coupled receptor structure-based drug design using X-ray lasers

(2019) Andrii Ishchenko et al.   IUCrJ

Small-Molecule Positive Allosteric Modulators of theβ2-Adrenoceptor Isolated from DNA-Encoded Libraries

(2018) Seungkirl Ahn et al.   MOLECULAR PHARMACOLOGY

Structure and dynamics of GPCR signaling complexes

(2018) Daniel Hilger et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Sortase ligation enables homogeneous GPCR phosphorylation to reveal diversity in β-arrestin coupling

(2018) Dean P. Staus et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure and dynamics of GPCR signaling complexes

(2018) Daniel Hilger et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

G-Protein–Coupled Receptors in Heart Disease

(2018) Jialu Wang et al.   CIRCULATION RESEARCH

Structural insights into G-protein-coupled receptor allostery

(2018) David M. Thal et al.   NATURE

Mechanisms of signalling and biased agonism in G protein-coupled receptors

(2018) Denise Wootten et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

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

(2018) Louis M. Luttrell et al.   Science Signaling

G protein–coupled receptor kinases (GRKs) orchestrate biased agonism at the β2-adrenergic receptor

(2018) Minjung Choi et al.   Science Signaling

Mechanism of intracellular allosteric β2AR antagonist revealed by X-ray crystal structure

(2017) Xiangyu Liu et al.   NATURE

Allosteric “beta-blocker” isolated from a DNA-encoded small molecule library

(2017) Seungkirl Ahn et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Gαi is required for carvedilol-induced β1 adrenergic receptor β-arrestin biased signaling

(2017) Jialu Wang et al.   Nature Communications

Allosteric coupling from G protein to the agonist-binding pocket in GPCRs

(2016) Brian T. DeVree et al.   NATURE

Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation

(2016) Dean P. Staus et al.   NATURE

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

(2015) Aashish Manglik et al.   CELL

Novel Allosteric Modulators of G Protein-coupled Receptors

(2015) Patrick R. Gentry et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Divergent Transducer-specific Molecular Efficacies Generate Biased Agonism at a G Protein-coupled Receptor (GPCR)

(2014) Ryan T. Strachan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Recent developments in biased agonism

(2013) James W Wisler et al.   CURRENT OPINION IN CELL BIOLOGY

Structure of active β-arrestin-1 bound to a G-protein-coupled receptor phosphopeptide

(2013) Arun K. Shukla et al.   NATURE

Adrenaline-activated structure of β2-adrenoceptor stabilized by an engineered nanobody

(2013) Aaron M. Ring et al.   NATURE

Emerging paradigms in GPCR allostery: implications for drug discovery

(2013) Denise Wootten et al.   NATURE REVIEWS DRUG DISCOVERY

MARCH2 promotes endocytosis and lysosomal sorting of carvedilol-bound β2-adrenergic receptors

(2012) Sang-oh Han et al.   JOURNAL OF CELL BIOLOGY

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

(2012) J. J. Liu et al.   SCIENCE

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

(2011) Eric Reiter et al.   Annual Review of Pharmacology and Toxicology

Structure of a nanobody-stabilized active state of the β2 adrenoceptor

(2011) Søren G. F. Rasmussen et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

(2011) Søren G. F. Rasmussen et al.   NATURE

Multiple ligand-specific conformations of the β2-adrenergic receptor

(2011) Alem W Kahsai et al.   Nature Chemical Biology

β-arrestin-mediated receptor trafficking and signal transduction

(2011) Sudha K. Shenoy et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor

(2010) Michael P. Bokoch et al.   NATURE

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

(2010) Erin J. Whalen et al.   TRENDS IN MOLECULAR MEDICINE

Arrestin Development: Emerging Roles for β-arrestins in Developmental Signaling Pathways

(2009) Jeffrey J. Kovacs et al.   DEVELOPMENTAL CELL

 -Blockers alprenolol and carvedilol stimulate  -arrestin-mediated EGFR transactivation

(2008) I.-M. Kim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA