Targeting adenosine A2A receptor antagonism for treatment of cancer

Inhibition of the adenosine A2a receptor modulates expression of T cell coinhibitory receptors and improves effector function for enhanced checkpoint blockade and ACT in murine cancer models

(2018) Robert D. Leone et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

CD38-mediated immunosuppression as a mechanism of tumor cell escape from PD-1/PD-L1 blockade

(2018) Limo Chen et al.   Cancer Discovery

Towards high throughput GPCR crystallography: In Meso soaking of Adenosine A2A Receptor crystals

(2018) Prakash Rucktooa et al.   Scientific Reports

Enabling STD-NMR fragment screening using stabilized native GPCR: A case study of adenosine receptor

(2018) Sébastien Igonet et al.   Scientific Reports

Cryo-EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein

(2018) Javier García-Nafría et al.   eLife

Adenosine A2A Receptor Antagonists in Neurodegenerative Diseases: Huge Potential and Huge Challenges

(2018) Rafael Franco et al.   Frontiers in Psychiatry

Structure-Based Design of Potent and Selective Ligands at the Four Adenosine Receptors

(2017) Willem Jespers et al.   MOLECULES

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

A Novel Antagonist of the Immune Checkpoint Protein Adenosine A2a Receptor Restores Tumor-Infiltrating Lymphocyte Activity in the Context of the Tumor Microenvironment

(2017) Melanie Mediavilla-Varela et al.   NEOPLASIA

Selective activation of anti-CD73 mechanisms in control of primary tumors and metastases

(2017) Dipti Vijayan et al.   OncoImmunology

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

(2016) Arabella Young et al.   CANCER CELL

Adenosine 2B Receptor Expression on Cancer Cells Promotes Metastasis

(2016) D. Mittal et al.   CANCER RESEARCH

Structurally Enabled Discovery of Adenosine A2A Receptor Antagonists

(2016) Ali Jazayeri et al.   CHEMICAL REVIEWS

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

(2016) Byron Carpenter et al.   NATURE

Targeting CD73 in the tumor microenvironment with MEDI9447

(2016) Carl M. Hay et al.   OncoImmunology

Structures of G protein-coupled receptors reveal new opportunities for drug discovery

(2015) Robert M. Cooke et al.   DRUG DISCOVERY TODAY

History and Perspectives of A2AAdenosine Receptor Antagonists as Potential Therapeutic Agents

(2015) Delia Preti et al.   MEDICINAL RESEARCH REVIEWS

A2aR antagonists: Next generation checkpoint blockade for cancer immunotherapy

(2015) Robert D. Leone et al.   Computational and Structural Biotechnology Journal

Adenosine A2A Receptors Intrinsically Regulate CD8+ T Cells in the Tumor Microenvironment

(2014) C. Cekic et al.   CANCER RESEARCH

Impact of Template Choice on Homology Model Efficiency in Virtual Screening

(2014) Krzysztof Rataj et al.   Journal of Chemical Information and Modeling

Structure-based drug design of chromone antagonists of the adenosine A2A receptor

(2014) Stephen P. Andrews et al.   MedChemComm

Targeting CD73 Enhances the Antitumor Activity of Anti-PD-1 and Anti-CTLA-4 mAbs

(2013) B. Allard et al.   CLINICAL CANCER RESEARCH

Istradefylline: First Global Approval

(2013) Rosselle Dungo et al.   DRUGS

Water Network Perturbation in Ligand Binding: Adenosine A2A Antagonists as a Case Study

(2013) Andrea Bortolato et al.   Journal of Chemical Information and Modeling

Bridging Molecular Docking to Membrane Molecular Dynamics To Investigate GPCR–Ligand Recognition: The Human A2A Adenosine Receptor as a Key Study

(2013) Davide Sabbadin et al.   Journal of Chemical Information and Modeling

Adenosine A2A Receptor as a Drug Discovery Target

(2013) Manuel de Lera Ruiz et al.   JOURNAL OF MEDICINAL CHEMISTRY

CD73 promotes anthracycline resistance and poor prognosis in triple negative breast cancer

(2013) S. Loi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Expression and clinical significance of CD73 and hypoxia-inducible factor-1α in gastric carcinoma

(2013) Xiao-Xia Lu   WORLD JOURNAL OF GASTROENTEROLOGY

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

Ligand-, structure- and pharmacophore-based molecular fingerprints: a case study on adenosine A1, A2A, A2B, and A3 receptor antagonists

(2012) Francesco Sirci et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Optimization of Adenosine 5′-Carboxamide Derivatives as Adenosine Receptor Agonists Using Structure-Based Ligand Design and Fragment Screening

(2012) Dilip K. Tosh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of Novel Adenosine A2A Receptor Antagonists by Virtual Screening

(2012) Christopher J. Langmead et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 1,2,4-Triazine Derivatives as Adenosine A2A Antagonists using Structure Based Drug Design

(2012) Miles Congreve et al.   JOURNAL OF MEDICINAL CHEMISTRY

High expression of CD73 as a poor prognostic biomarker in human colorectal cancer

(2012) Xian-Rui Wu et al.   JOURNAL OF SURGICAL ONCOLOGY

G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody

(2012) Tomoya Hino et al.   NATURE

Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions

(2012) W. Liu et al.   SCIENCE

CD73: a potent suppressor of antitumor immune responses

(2012) Paul. A. Beavis et al.   TRENDS IN IMMUNOLOGY

New insights from structural biology into the druggability of G protein-coupled receptors

(2012) Jonathan S. Mason et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Stabilised G protein-coupled receptors in structure-based drug design: a case study with adenosine A2Areceptor

(2012) Stephen P. Andrews et al.   MedChemComm

The development and immunosuppressive functions of CD4+ CD25+ FoxP3+ regulatory T cells are under influence of the adenosine-A2A adenosine receptor pathway

(2012) Akio Ohta et al.   Frontiers in Immunology

Adenosine A2A Receptor Antagonists and Parkinson’s Disease

(2011) Brian C. Shook et al.   ACS Chemical Neuroscience

CD73-Deficient Mice Have Increased Antitumor Immunity and Are Resistant to Experimental Metastasis

(2011) J. Stagg et al.   CANCER RESEARCH

Evaluation of Molecular Modeling of Agonist Binding in Light of the Crystallographic Structure of an Agonist-Bound A2A Adenosine Receptor

(2011) Francesca Deflorian et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biophysical Mapping of the Adenosine A2AReceptor

(2011) Andrei Zhukov et al.   JOURNAL OF MEDICINAL CHEMISTRY

Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation

(2011) Guillaume Lebon et al.   NATURE

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

Regadenoson

(2010) Karly P. Garnock-Jones et al.   American Journal of Cardiovascular Drugs

Biacore analysis with stabilized G-protein-coupled receptors

(2010) Rebecca L. Rich et al.   ANALYTICAL BIOCHEMISTRY

Adenosine receptors and brain diseases: Neuroprotection and neurodegeneration

(2010) Catarina V. Gomes et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Adenosine Receptor Modeling: What Does the A2A Crystal Structure Tell Us?

(2010) D. Dal Ben et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Preladenant, a selective A2A receptor antagonist, is active in primate models of movement disorders

(2010) Robert A. Hodgson et al.   EXPERIMENTAL NEUROLOGY

Structure-Based Discovery of Novel Chemotypes for Adenosine A2AReceptor Antagonists

(2010) Vsevolod Katritch et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Discovery of A2AAdenosine Receptor Ligands

(2010) Jens Carlsson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure based prediction of subtype-selectivity for adenosine receptor antagonists

(2010) Vsevolod Katritch et al.   NEUROPHARMACOLOGY

3D Pharmacophore Based Virtual Screening of A2A Adenosine Receptor Antagonists

(2010) Jing Wei et al.   PROTEIN AND PEPTIDE LETTERS

Hydration Site Thermodynamics Explain SARs for Triazolylpurines Analogues Binding to the A2A Receptor

(2010) Christopher Higgs et al.   ACS Medicinal Chemistry Letters

Adenosine regulates CD8 T-cell priming by inhibition of membrane-proximal T-cell receptor signalling

(2009) Carsten Linnemann et al.   IMMUNOLOGY

Evaluation of Homology Modeling of G-Protein-Coupled Receptors in Light of the A2AAdenosine Receptor Crystallographic Structure

(2009) Andrei A. Ivanov et al.   JOURNAL OF MEDICINAL CHEMISTRY

Characterization of the Potent and Highly Selective A2A Receptor Antagonists Preladenant and SCH 412348 [7-[2-[4-2,4-Difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine] in Rodent Models of Movement Disorders and Depression

(2009) R. A. Hodgson et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Adenosine receptors in regulation of dendritic cell differentiation and function

(2008) S. V. Novitskiy et al.   BLOOD

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

(2008) V.-P. Jaakola et al.   SCIENCE