G Protein‐Coupled Receptor Signaling: Transducers and Effectors

GPCR systems pharmacology: a different perspective on the development of biased therapeutics

(2022) Dylan Scott Eiger et al.   AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY

Structures of the glucocorticoid-bound adhesion receptor GPR97–Go complex

(2021) Yu-Qi Ping et al.   NATURE

Mapping Angiotensin II Type 1 Receptor-Biased Signaling Using Proximity Labeling and Proteomics Identifies Diverse Actions of Biased Agonists

(2021) Conrad T. Pfeiffer et al.   JOURNAL OF PROTEOME RESEARCH

Structural studies of phosphorylation-dependent interactions between the V2R receptor and arrestin-2

(2021) Qing-Tao He et al.   Nature Communications

Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1

(2021) Qiuyan Chen et al.   NATURE

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

(2021) Jialu Wang et al.   MOLECULAR PHARMACOLOGY

Structure of the neurotensin receptor 1 in complex with β-arrestin 1

(2020) Weijiao Huang et al.   NATURE

Structure of the M2 muscarinic receptor–β-arrestin complex in a lipid nanodisc

(2020) Dean P. Staus et al.   NATURE

Allosteric activation of proto-oncogene kinase Src by GPCR–beta-arrestin complexes

(2020) Natalia Pakharukova et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Angiotensin Analogs with Divergent Bias Stabilize Distinct Receptor Conformations

(2019) Laura M. Wingler et al.   CELL

Structural Mechanism of the Arrestin-3/JNK3 Interaction

(2019) Ji Young Park et al.   STRUCTURE

G protein-coupled receptor kinases as therapeutic targets in the heart

(2019) Jessica Pfleger et al.   Nature Reviews Cardiology

Conformational Sensors and Domain Swapping Reveal Structural and Functional Differences between β-Arrestin Isoforms

(2019) Eshan Ghosh et al.   Cell Reports

Structure of an endosomal signaling GPCR–G protein–β-arrestin megacomplex

(2019) Anthony H. Nguyen et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

G protein-coupled receptor kinases: Past, present and future

(2018) Konstantin E. Komolov et al.   CELLULAR SIGNALLING

Allosteric mechanisms underlie GPCR signaling to SH3-domain proteins through arrestin

(2018) Fan Yang et al.   Nature Chemical Biology

Arrestin-3 scaffolding of the JNK3 cascade suggests a mechanism for signal amplification

(2018) Nicole A. Perry et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

β-Arrestin2 Improves Post–Myocardial Infarction Heart Failure via Sarco(endo)plasmic Reticulum Ca 2+ -ATPase–Dependent Positive Inotropy in CardiomyocytesNovelty and Significance

(2017) Katie A. McCrink et al.   HYPERTENSION

Structural basis of arrestin-3 activation and signaling

(2017) Qiuyan Chen et al.   Nature Communications

Allosteric Modulation as a Unifying Mechanism for Receptor Function and Regulation

(2016) Jean-Pierre Changeux et al.   CELL

GPCR-G Protein-β-Arrestin Super-Complex Mediates Sustained G Protein Signaling

(2016) Alex R.B. Thomsen et al.   CELL

Prognostic Value of Lymphocyte G Protein-Coupled Receptor Kinase-2 Protein Levels in Patients With Heart FailureNovelty and Significance

(2016) Giuseppe Rengo et al.   CIRCULATION RESEARCH

Mechanistic insights into GPCR–G protein interactions

(2016) Jacob P Mahoney et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

“Canonical and non-canonical actions of GRK5 in the heart”

(2016) Christopher J. Traynham et al.   JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY

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

(2016) Mi-Hye Lee et al.   NATURE

The Inositol Trisphosphate/Calcium Signaling Pathway in Health and Disease

(2016) Michael J. Berridge   PHYSIOLOGICAL REVIEWS

β-Arrestin mediates the Frank–Starling mechanism of cardiac contractility

(2016) Dennis M. Abraham et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Atomic Structure of GRK5 Reveals Distinct Structural Features Novel for G Protein-coupled Receptor Kinases

(2015) Konstantin E. Komolov et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor

(2015) Kristoff T. Homan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Evolving Impact of G Protein-Coupled Receptor Kinases in Cardiac Health and Disease

(2015) Priscila Y. Sato et al.   PHYSIOLOGICAL REVIEWS

Phospho-selective mechanisms of arrestin conformations and functions revealed by unnatural amino acid incorporation and 19F-NMR

(2015) Fan Yang et al.   Nature Communications

Structural evidence for the role of polar core residue Arg175 in arrestin activation

(2015) Joachim Granzin et al.   Scientific Reports

Molecular Basis for Small Molecule Inhibition of G Protein-Coupled Receptor Kinases

(2014) Kristoff T. Homan et al.   ACS Chemical Biology

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

Simultaneous Adrenal and Cardiac G-Protein–Coupled Receptor-G βγ Inhibition Halts Heart Failure Progression

(2014) Fadia A. Kamal et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

GRK3 is essential for metastatic cells and promotes prostate tumor progression

(2014) W. Li et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Rab Proteins and the Compartmentalization of the Endosomal System

(2014) A. Wandinger-Ness et al.   Cold Spring Harbor Perspectives in Biology

Regulation of G Protein-Coupled Receptor Kinases by Phospholipids

(2013) K.T. Homan et al.   CURRENT MEDICINAL CHEMISTRY

Negative Impact of β-Arrestin-1 on Post-Myocardial Infarction Heart Failure via Cardiac and Adrenal-Dependent Neurohormonal Mechanisms

(2013) Ashley Bathgate-Siryk et al.   HYPERTENSION

Crystal structure of pre-activated arrestin p44

(2013) Yong Ju Kim et al.   NATURE

β-arrestin2 in Infiltrated Macrophages Inhibits Excessive Inflammation after Myocardial Infarction

(2013) Kenji Watari et al.   PLoS One

Convergence of G Protein-Coupled Receptor and S-Nitrosylation Signaling Determines the Outcome to Cardiac Ischemic Injury

(2013) Z. M. Huang et al.   Science Signaling

Paroxetine Is a Direct Inhibitor of G Protein-Coupled Receptor Kinase 2 and Increases Myocardial Contractility

(2012) David M. Thal et al.   ACS Chemical Biology

G 13 -Mediated Signaling Pathway Is Required for Pressure Overload–Induced Cardiac Remodeling and Heart Failure

(2012) Mikito Takefuji et al.   CIRCULATION

Determining the Absolute Requirement of G Protein–Coupled Receptor Kinase 5 for Pathological Cardiac Hypertrophy

(2012) Jessica I. Gold et al.   CIRCULATION RESEARCH

AAV6. ARKct cardiac gene therapy ameliorates cardiac function and normalizes the catecholaminergic axis in a clinically relevant large animal heart failure model

(2012) P. W. J. Raake et al.   EUROPEAN HEART JOURNAL

Competing G protein-coupled receptor kinases balance G protein and β-arrestin signaling

(2012) Domitille Heitzler et al.   Molecular Systems Biology

Selective recruitment of G protein-coupled receptor kinases (GRKs) controls signaling of the insulin-like growth factor 1 receptor

(2012) H. Zheng et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Molecular Mechanism for Inhibition of G Protein-Coupled Receptor Kinase 2 by a Selective RNA Aptamer

(2012) Valerie M. Tesmer et al.   STRUCTURE

Activation of G Protein-Coupled Receptor Kinase 1 Involves Interactions between Its N-Terminal Region and Its Kinase Domain

(2011) Chih-chin Huang et al.   BIOCHEMISTRY

G Protein Coupled Receptor Kinases as Therapeutic Targets in Cardiovascular Disease

(2011) Stephen L. Belmonte et al.   CIRCULATION RESEARCH

Signalling mechanisms of RhoGTPase regulation by the heterotrimeric G proteins G12 and G13

(2011) T. Kozasa et al.   JOURNAL OF BIOCHEMISTRY

Molecular Mechanism of Selectivity among G Protein-Coupled Receptor Kinase 2 Inhibitors

(2011) D. M. Thal et al.   MOLECULAR PHARMACOLOGY

The functional cycle of visual arrestins in photoreceptor cells

(2011) Vsevolod V. Gurevich et al.   PROGRESS IN RETINAL AND EYE RESEARCH

Small Molecule Disruption of Gβγ Signaling Inhibits the Progression of Heart Failure

(2010) Liam M. Casey et al.   CIRCULATION RESEARCH

Molecular basis for activation of G protein-coupled receptor kinases

(2010) Cassandra A Boguth et al.   EMBO JOURNAL

Intracardiac Injection of AdGRK5-NT Reduces Left Ventricular Hypertrophy by Inhibiting NF-κB–Dependent Hypertrophic Gene Expression

(2010) Daniela Sorriento et al.   HYPERTENSION

Structure of Human G Protein-Coupled Receptor Kinase 2 in Complex with the Kinase Inhibitor Balanol

(2010) John J. G. Tesmer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Teaching old receptors new tricks: biasing seven-transmembrane receptors

(2010) Sudarshan Rajagopal et al.   NATURE REVIEWS DRUG DISCOVERY

Role of the Amino Terminus of G Protein-Coupled Receptor Kinase 2 in Receptor Phosphorylation

(2009) Christina S. Pao et al.   BIOCHEMISTRY

GRK2 Activation by Receptors: Role of the Kinase Large Lobe and Carboxyl-Terminal Tail

(2009) Rachel Sterne-Marr et al.   BIOCHEMISTRY

A Surface of the Kinase Domain Critical for the Allosteric Activation of G Protein-coupled Receptor Kinases

(2009) Chih-chin Huang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure of an Arrestin2-Clathrin Complex Reveals a Novel Clathrin Binding Domain That Modulates Receptor Trafficking

(2009) Dong Soo Kang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

G Protein-coupled Receptor Kinases Phosphorylate LRP6 in the Wnt Pathway

(2009) Minyong Chen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

β-Arrestin-2 Mediates Anti-apoptotic Signaling through Regulation of BAD Phosphorylation

(2009) Seungkirl Ahn et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The nuts and bolts of AGC protein kinases

(2009) Laura R. Pearce et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Myocardial Adeno-Associated Virus Serotype 6–βARKct Gene Therapy Improves Cardiac Function and Normalizes the Neurohormonal Axis in Chronic Heart Failure

(2008) Giuseppe Rengo et al.   CIRCULATION

Characterization of the GNAQ promoter and association of increased Gq expression with cardiac hypertrophy in humans

(2008) Ulrich H. Frey et al.   EUROPEAN HEART JOURNAL

Structures of Rhodopsin Kinase in Different Ligand States Reveal Key Elements Involved in G Protein-coupled Receptor Kinase Activation

(2008) Puja Singh et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A new type of ERK1/2 autophosphorylation causes cardiac hypertrophy

(2008) Kristina Lorenz et al.   NATURE MEDICINE

A GRK5 polymorphism that inhibits β-adrenergic receptor signaling is protective in heart failure

(2008) Stephen B Liggett et al.   NATURE MEDICINE

Protective effect of a GRK5 polymorphismon heart failure and its interaction with β-adrenergic receptor antagonists

(2008) Mark Eijgelsheim et al.   PHARMACOGENOMICS

Uncovering G protein-coupled receptor kinase-5 as a histone deacetylase kinase in the nucleus of cardiomyocytes

(2008) J. S. Martini et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Distinct conformational changes in  -arrestin report biased agonism at seven-transmembrane receptors

(2008) A. K. Shukla et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

 -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

Agonist-selective mechanisms of GPCR desensitization

(2007) E Kelly et al.   BRITISH JOURNAL OF PHARMACOLOGY