Biased agonism at adenosine receptors

TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome

(2020) Reid H. J. Olsen et al.   Nature Chemical Biology

Assessment of biased agonism at the A3 adenosine receptor using β-arrestin and miniGαi recruitment assays

(2020) Eline Pottie et al.   BIOCHEMICAL PHARMACOLOGY

Historical and Current Adenosine Receptor Agonists in Preclinical and Clinical Development

(2019) Kenneth A. Jacobson et al.   Frontiers in Cellular Neuroscience

Effect of Neladenoson Bialanate on Exercise Capacity Among Patients With Heart Failure With Preserved Ejection Fraction

(2019) Sanjiv J. Shah et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Safety and efficacy of the partial adenosine A1 receptor agonist neladenoson bialanate in patients with chronic heart failure with reduced ejection fraction: a phase IIb, randomized, double‐blind, placebo‐controlled trial

(2019) Adriaan A. Voors et al.   EUROPEAN JOURNAL OF HEART FAILURE

Molecular dissection of the human A 3 adenosine receptor coupling with β-arrestin2

(2018) Jolien Storme et al.   BIOCHEMICAL PHARMACOLOGY

On the G protein-coupling selectivity of the native A 2B adenosine receptor

(2018) Zhan-Guo Gao et al.   BIOCHEMICAL PHARMACOLOGY

Mini G protein probes for active G protein–coupled receptors (GPCRs) in live cells

(2018) Qingwen Wan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Structure–Activity Relationship Study of Bitopic N6-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists

(2018) Luigi Aurelio et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

Development of novel biosensors to study receptor-mediated activation of the G-protein α subunits Gsand Golf

(2017) Hideaki Yano et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2017) Lauriane Onfroy et al.   Scientific Reports

Actinin-1 binds to the C-terminus of A2B adenosine receptor (A2BAR) and enhances A2BAR cell-surface expression

(2016) Y. Sun et al.   BIOCHEMICAL JOURNAL

Quantification of adenosine A 1 receptor biased agonism: Implications for drug discovery

(2016) Jo-Anne Baltos et al.   BIOCHEMICAL PHARMACOLOGY

Co-inhibition of CD73 and A2AR Adenosine Signaling Improves Anti-tumor Immune Responses

(2016) Arabella Young et al.   CANCER CELL

The adenosine metabolite inosine is a functional agonist of the adenosine A2A receptor with a unique signaling bias

(2016) Ajith A. Welihinda et al.   CELLULAR SIGNALLING

Structure of the adenosine A2A receptor bound to an engineered G protein

(2016) Byron Carpenter et al.   NATURE

A Metabolic Immune Checkpoint: Adenosine in Tumor Microenvironment

(2016) Akio Ohta   Frontiers in Immunology

Adenosine A1receptor activation attenuates cardiac hypertrophy and fibrosis in response to α1-adrenoceptor stimulationin vivo

(2015) S-L Puhl et al.   BRITISH JOURNAL OF PHARMACOLOGY

A1 adenosine receptor-mediated GIRK channels contribute to the resting conductance of CA1 neurons in the dorsal hippocampus

(2015) Chung Sub Kim et al.   JOURNAL OF NEUROPHYSIOLOGY

Cardioprotective potential of annexin-A1 mimetics in myocardial infarction

(2015) Chengxue Qin et al.   PHARMACOLOGY & THERAPEUTICS

Probing biased/partial agonism at the G protein-coupled A2B adenosine receptor

(2014) Zhan-Guo Gao et al.   BIOCHEMICAL PHARMACOLOGY

Endogenous adenosine A3 receptor activation selectively alleviates persistent pain states

(2014) Joshua W. Little et al.   BRAIN

Myeloid Expression of Adenosine A2A Receptor Suppresses T and NK Cell Responses in the Solid Tumor Microenvironment

(2014) C. Cekic et al.   CANCER RESEARCH

Antimetastatic Effects of Blocking PD-1 and the Adenosine A2A Receptor

(2014) D. Mittal et al.   CANCER RESEARCH

An Adenosine A1 Agonist 2-Chloro-N6 Cyclopentyladenosine Inhibits the Angiotensin II-Induced Cardiomyocyte Hypertrophy through the Calcineurin Pathway

(2014) Xingliang Zhang et al.   CARDIOLOGY

Adenosine A2A Receptor Antagonists in Parkinson’s Disease: Progress in Clinical Trials from the Newly Approved Istradefylline to Drugs in Early Development and Those Already Discontinued

(2014) Annalisa Pinna   CNS DRUGS

Biased Ligand Modulation of Seven Transmembrane Receptors (7TMRs): Functional Implications for Drug Discovery

(2014) Craig C. Correll et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2014) C. Valant et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Biased ligands at G-protein-coupled receptors: promise and progress

(2014) Jonathan D. Violin et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Chronic Therapy With a Partial Adenosine A1-Receptor Agonist Improves Left Ventricular Function and Remodeling in Dogs With Advanced Heart Failure

(2013) Hani N. Sabbah et al.   Circulation-Heart Failure

GIRK Channel Activation Via Adenosine or Muscarinic Receptors Has Similar Effects on Rat Atrial Electrophysiology

(2013) Xiaodong Wang et al.   JOURNAL OF CARDIOVASCULAR PHARMACOLOGY

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

(2013) Terry Kenakin et al.   NATURE REVIEWS DRUG DISCOVERY

CF102 for the Treatment of Hepatocellular Carcinoma: A Phase I/II, Open-Label, Dose-Escalation Study

(2013) S. M. Stemmer et al.   ONCOLOGIST

A2A Adenosine Receptors Are Differentially Modulated by Pharmacological Treatments in Rheumatoid Arthritis Patients and Their Stimulation Ameliorates Adjuvant-Induced Arthritis in Rats

(2013) Fabrizio Vincenzi et al.   PLoS One

Blockade of A2Areceptors potently suppresses the metastasis of CD73+tumors

(2013) Paul A. Beavis et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Synthesis and structure–activity relationships of 2-hydrazinyladenosine derivatives as A2A adenosine receptor ligands

(2012) Ali El-Tayeb et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Adenosine A2A Antagonists in Parkinson’s Disease: What’s Next?

(2012) Patrick Hickey et al.   Current Neurology and Neuroscience Reports

Controlling murine and rat chronic pain through A3 adenosine receptor activation

(2012) Zhoumou Chen et al.   FASEB JOURNAL

Transcriptional control of adenosine signaling by hypoxia-inducible transcription factors during ischemic or inflammatory disease

(2012) Jens M. Poth et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Functional selectivity of adenosine A1 receptor ligands?

(2012) Ellen V. Langemeijer et al.   Purinergic Signalling

Bridging the gap: bitopic ligands of G-protein-coupled receptors

(2012) J. Robert Lane et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Functionally biased modulation of A3 adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers

(2011) Zhan-Guo Gao et al.   BIOCHEMICAL PHARMACOLOGY

Real-time visualization of heterotrimeric G protein Gq activation in living cells

(2011) Merel JW Adjobo-Hermans et al.   BMC BIOLOGY

G protein-coupled receptor kinases: More than just kinases and not only for GPCRs

(2011) Eugenia V. Gurevich et al.   PHARMACOLOGY & THERAPEUTICS

Functional selectivity of adenosine receptor ligands

(2011) Dennis Verzijl et al.   Purinergic Signalling

Structure of an Agonist-Bound Human A2A Adenosine Receptor

(2011) F. Xu et al.   SCIENCE

Structure of the Adenosine A2A Receptor in Complex with ZM241385 and the Xanthines XAC and Caffeine

(2011) Andrew S. Doré et al.   STRUCTURE

Adenosine and its receptors in the heart: Regulation, retaliation and adaptation

(2010) John P. Headrick et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Recent developments in adenosine receptor ligands and their potential as novel drugs

(2010) Christa E. Müller et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

The role of conformational ensembles of seven transmembrane receptors in functional selectivity

(2010) Nagarajan Vaidehi et al.   CURRENT OPINION IN PHARMACOLOGY

CF102 an A3 adenosine receptor agonist mediates anti-tumor and anti-inflammatory effects in the liver

(2010) S. Cohen et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Effects of BG9928, an Adenosine A1Receptor Antagonist, in Patients With Congestive Heart Failure

(2010) Stephen S. Gottlieb et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Hybrid Ortho/Allosteric Ligands for the Adenosine A1Receptor

(2010) Rajeshwar Narlawar et al.   JOURNAL OF MEDICINAL CHEMISTRY

Delineating the Mode of Action of Adenosine A1 Receptor Allosteric Modulators

(2010) C. Valant et al.   MOLECULAR PHARMACOLOGY

Excitatory synaptic transmission in the spinal substantia gelatinosa is under an inhibitory tone of endogenous adenosine

(2010) Li Tian et al.   NEUROSCIENCE LETTERS

Rolofylline, an Adenosine A1−Receptor Antagonist, in Acute Heart Failure

(2010) Barry M. Massie et al.   NEW ENGLAND JOURNAL OF MEDICINE

Adenosine receptors interacting proteins (ARIPs): Behind the biology of adenosine signaling

(2009) Francisco Ciruela et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Synthetic studies on selective adenosine A2A receptor antagonists: Synthesis and structure–activity relationships of novel benzofuran derivatives

(2009) Osamu Saku et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Reciprocal Regulation of Myocardial microRNAs and Messenger RNA in Human Cardiomyopathy and Reversal of the microRNA Signature by Biomechanical Support

(2009) Scot J. Matkovich et al.   CIRCULATION

Cardio-Renal Effects of the A1 Adenosine Receptor Antagonist SLV320 in Patients With Heart Failure

(2009) Veselin Mitrovic et al.   Circulation-Heart Failure

A2A adenosine receptor overexpression and functionality, as well as TNF-α levels, correlate with motor symptoms in Parkinson’s disease

(2009) Katia Varani et al.   FASEB JOURNAL

Allosteric Modulators of the Adenosine A1Receptor: Synthesis and Pharmacological Evaluation of 4-Substituted 2-Amino-3-benzoylthiophenes

(2009) Luigi Aurelio et al.   JOURNAL OF MEDICINAL CHEMISTRY

A2A Adenosine Receptor and its Modulators: Overview on a Druggable GPCR and on Structure-Activity Relationship Analysis and Binding Requirements of Agonists and Antagonists

(2008) G. Cristalli et al.   CURRENT PHARMACEUTICAL DESIGN

Translocation of arrestin induced by human A3 adenosine receptor ligands in an engineered cell line: Comparison with G protein-dependent pathways

(2008) Z GAO et al.   PHARMACOLOGICAL RESEARCH

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE