New paradigms in adenosine receptor pharmacology: allostery, oligomerization and biased agonism

A kinetic view of GPCR allostery and biased agonism

(2017) J Robert Lane et al.   Nature Chemical Biology

The IUPHAR/BPS Guide to PHARMACOLOGY in 2018: updates and expansion to encompass the new guide to IMMUNOPHARMACOLOGY

(2017) Simon D Harding et al.   NUCLEIC ACIDS RESEARCH

Crystal structure of the adenosine A2Areceptor bound to an antagonist reveals a potential allosteric pocket

(2017) Bingfa Sun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structures of Human A 1 and A 2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity

(2017) Robert K.Y. Cheng et al.   STRUCTURE

Receptor Quaternary Organization Explains G Protein-Coupled Receptor Family Structure

(2017) James H. Felce et al.   Cell Reports

Targeting Adenosine Receptors for the Treatment of Cardiac Fibrosis

(2017) Elizabeth A. Vecchio et al.   Frontiers in Pharmacology

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

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

The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling

(2016) Elizabeth A. Vecchio et al.   BIOCHEMICAL PHARMACOLOGY

Evidence for the heterotetrameric structure of the adenosine A 2A –dopamine D 2 receptor complex

(2016) Verònica Casadó-Anguera et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

(2016) Yi Zheng et al.   NATURE

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

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

Osteoblast differentiation and survival: A role for A2B adenosine receptor allosteric modulators

(2014) Maria Letizia Trincavelli et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Dopamine heteroreceptor complexes as therapeutic targets in Parkinson’s disease

(2014) Kjell Fuxe et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Synthesis and Pharmacological Evaluation of Dual Acting Ligands Targeting the Adenosine A2A and Dopamine D2 Receptors for the Potential Treatment of Parkinson’s Disease

(2014) Manuela Jörg et al.   JOURNAL OF MEDICINAL CHEMISTRY

A3Adenosine Receptor Allosteric Modulator Induces an Anti-Inflammatory Effect:In VivoStudies and Molecular Mechanism of Action

(2014) Shira Cohen et al.   MEDIATORS OF INFLAMMATION

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

Design, synthesis and biological evaluation of bivalent ligands against A1–D1 receptor heteromers

(2013) Jian Shen et al.   ACTA PHARMACOLOGICA SINICA

Allosteric modulators of human A2B adenosine receptor

(2013) Maria Letizia Trincavelli et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Adenosine A1 receptors heterodimerize with β1- and β2-adrenergic receptors creating novel receptor complexes with altered G protein coupling and signaling

(2013) P. Charukeshi Chandrasekera et al.   CELLULAR SIGNALLING

Interaction of δ and κ opioid receptors with adenosine A1 receptors mediates cardioprotection by remote ischemic preconditioning

(2013) Harinee Surendra et al.   JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY

Activation and allosteric modulation of a muscarinic acetylcholine receptor

(2013) Andrew C. Kruse et al.   NATURE

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

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

Fragment Screening of GPCRs Using Biophysical Methods: Identification of Ligands of the Adenosine A2A Receptor with Novel Biological Activity

(2012) Dan Chen et al.   ACS Chemical Biology

The role of the second and third extracellular loops of the adenosine A1 receptor in activation and allosteric modulation

(2012) M.C. Peeters et al.   BIOCHEMICAL PHARMACOLOGY

The new oral adenosine A1 receptor agonist capadenoson in male patients with stable angina

(2012) Michal Tendera et al.   Clinical Research in Cardiology

Synthesis and Characterization of Novel 2-Amino-3-benzoylthiophene Derivatives as Biased Allosteric Agonists and Modulators of the Adenosine A1 Receptor

(2012) Celine Valant et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

The Best of Both Worlds? Bitopic Orthosteric/Allosteric Ligands of G Protein–Coupled Receptors

(2011) Celine Valant et al.   Annual Review of Pharmacology and Toxicology

A2Aadenosine receptor ligand binding and signalling is allosterically modulated by adenosine deaminase

(2011) Eduard Gracia et al.   BIOCHEMICAL JOURNAL

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

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

Allosteric interactions across native adenosine-A3 receptor homodimers: quantification using single-cell ligand-binding kinetics

(2011) Lauren T. May et al.   FASEB JOURNAL

International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors--An Update

(2011) B. B. Fredholm et al.   PHARMACOLOGICAL REVIEWS

Adenosine receptor desensitization and trafficking

(2010) Stuart Mundell et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Allosteric modulation of adenosine receptors

(2010) Anikó Göblyös et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Adenosine A2A Receptor Is Involved in Cell Surface Expression of A2B Receptor

(2010) Kengo Moriyama et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Hybrid Ortho/Allosteric Ligands for the Adenosine A1Receptor

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

Antagonist Selective Modulation of Adenosine A1 and A3 Receptor Pharmacology by the Food Dye Brilliant Black BN: Evidence for Allosteric Interactions

(2010) L. T. May et al.   MOLECULAR PHARMACOLOGY

The Effect of Allosteric Modulators on the Kinetics of Agonist-G Protein-Coupled Receptor Interactions in Single Living Cells

(2010) L. T. May et al.   MOLECULAR PHARMACOLOGY

Design, synthesis and biological evaluation of a bivalent μ opiate and adenosine A1 receptor antagonist

(2009) Smitha C. Mathew et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Plasma membrane diffusion of g protein-coupled receptor oligomers

(2008) Stephen J. Briddon et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Novel pharmacological targets based on receptor heteromers

(2008) Rafael Franco et al.   BRAIN RESEARCH REVIEWS

Detection of higher-order G protein-coupled receptor oligomers by a combined BRET-BiFC technique

(2008) Jorge Gandia et al.   FEBS LETTERS

Synthesis of Bivalent β2-Adrenergic and Adenosine A1Receptor Ligands

(2008) Peter Karellas et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

N6-1,3-Diphenylurea derivatives of 2-phenyl-9-benzyladenines and 8-azaadenines: Synthesis and biological evaluation as allosteric modulators of A2A adenosine receptors

(2007) Irene Giorgi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY