4.6 Article

Irreversible Antagonists for the Adenosine A2B Receptor

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Chemistry, Multidisciplinary

Single Stabilizing Point Mutation Enables High-Resolution Co-Crystal Structures of the Adenosine A2A Receptor with Preladenant Conjugates

Tobias Claff et al.

Summary: Researchers developed a new A(2A)AR construct and successfully co-crystallized it with Preladenant derivatives, providing explanations for their high potency and selectivity through crystal structures. This study is of great importance for further research on class A GPCRs.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2022)

Review Cell Biology

Caffeine and Its Neuroprotective Role in Ischemic Events: A Mechanism Dependent on Adenosine Receptors

D. Pereira-Figueiredo et al.

Summary: Ischemia is caused by insufficient blood flow to tissues, leading to inadequate oxygen and glucose supply, resulting in cell death and secondary damage. Adenosine and caffeine play important roles in CNS pathology, providing neuroprotective effects, but effective treatments are currently lacking.

CELLULAR AND MOLECULAR NEUROBIOLOGY (2022)

Review Clinical Neurology

Aspirin, paracetamol (acetaminophen) and caffeine for the treatment of acute migraine attacks: A systemic review and meta-analysis of randomized placebo-controlled trials

Hans Christoph Diener et al.

Summary: The meta-analysis found that APC is more effective than placebo in treating acute migraine attacks, with significantly higher rates of pain relief and pain-free response at 2 hours after treatment. Adverse events were more common in the APC group compared to placebo.

EUROPEAN JOURNAL OF NEUROLOGY (2022)

Review Pharmacology & Pharmacy

International Union of Basic and Clinical Pharmacology. CXII: Adenosine Receptors: A Further Update

Adriaan P. IJzerman et al.

Summary: This review provides an update on the nomenclature and classification of adenosine receptors, with a focus on emerging developments in protein structure, diversity, and modulation by small molecules. It also explores novel concepts such as target binding kinetics and biased signaling, as well as discusses the clinical trials and pharmacology of adenosine receptor ligands.

PHARMACOLOGICAL REVIEWS (2022)

Review Immunology

Adenosine-A2A Receptor Pathway in Cancer Immunotherapy

Changfa Sun et al.

Summary: The adenosine-A2AR pathway plays a crucial role in regulating immune responses and tumor progression. Blocking this pathway can inhibit tumor growth and has potential synergistic effects with CAR T cell therapy.

FRONTIERS IN IMMUNOLOGY (2022)

Article Chemistry, Medicinal

Agonist-Dependent Coupling of the Promiscuous Adenosine A2B Receptor to Gα Protein Subunits

Jan Hendrik Voss et al.

Summary: This study investigates the coupling of adenosine A(2B) receptor (A(2B)AR) to different G proteins and finds that adenosine and NECA can activate multiple G proteins, while BAY 60-6583 can only activate some of them. Adenosine deaminase enhances the efficacy of NECA and BAY 60-6583 in G alpha(i2) protein. The results suggest that A(2B)AR preferentially couples with G alpha(15), G alpha(s), and G alpha(12) proteins.

ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE (2022)

Article Immunology

Targeting purinergic receptors to suppress the cytokine storm induced by SARS-CoV-2 infection in pulmonary tissue

Julia Leao Batista Simoes et al.

Summary: COVID-19 is caused by a new member of the Coronaviridae family, the SARS-CoV-2 virus, which infects the respiratory tract by binding to ACE2 receptors. The infection triggers immune responses and cytokine storm, leading to severe respiratory symptoms and potential organ failure. Modulating purinergic receptors may offer a promising therapeutic approach to mitigate the severity of the disease.

INTERNATIONAL IMMUNOPHARMACOLOGY (2021)

Review Clinical Neurology

Istradefylline - a first generation adenosine A2A antagonist for the treatment of Parkinson's disease

Peter Jenner et al.

Summary: This narrative review focuses on the utility of adenosine A(2A) antagonists in Parkinson's disease treatment, with a specific emphasis on istradefylline. Current research supports the use of istradefylline for managing motor fluctuations in PD patients, and animal studies suggest positive results as well.

EXPERT REVIEW OF NEUROTHERAPEUTICS (2021)

Review Cell Biology

Adenosine Receptor Antagonists to Combat Cancer and to Boost Anti-Cancer Chemotherapy and Immunotherapy

Rafael Franco et al.

Summary: Extracellular adenosine accumulates in tumor environments and the A(2A) and A(2B) receptors have been identified as potential targets for cancer therapy. Research suggests that these receptors play a key role in regulating immune cells and tumor progression, making them promising candidates for enhancing anti-cancer treatment. Ongoing clinical trials are testing ligands targeting A(2A)R and A(2B)R in anti-cancer therapy, showing the growing interest in utilizing these receptors for cancer control.
Article Biochemistry & Molecular Biology

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

Reid H. J. Olsen et al.

NATURE CHEMICAL BIOLOGY (2020)

Article Pharmacology & Pharmacy

Targeting the A2AR in cancer; early lessons from the clinic

Stephen B. Willingham et al.

CURRENT OPINION IN PHARMACOLOGY (2020)

Article Chemistry, Medicinal

A2B Adenosine Receptor Antagonists with Picomolar Potency

Jie Jiang et al.

JOURNAL OF MEDICINAL CHEMISTRY (2019)

Review Biochemistry & Molecular Biology

A2B Adenosine Receptor and Cancer

Zhan-Guo Gao et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2019)

Review Chemistry, Medicinal

Efficacy and side effects of intravenous theophylline in acute asthma: a systematic review and meta-analysis

Gulixian Mahemuti et al.

DRUG DESIGN DEVELOPMENT AND THERAPY (2018)

Article Biochemistry & Molecular Biology

A covalent antagonist for the human adenosine A2A receptor

Xue Yang et al.

PURINERGIC SIGNALLING (2017)

Article Biochemistry & Molecular Biology

Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity

Alisa Glukhova et al.

Article Biochemistry & Molecular Biology

New insights into the QuikChange™ process guide the use of Phusion DNA polymerase for site-directed mutagenesis

Yongzhen Xia et al.

NUCLEIC ACIDS RESEARCH (2015)

Article Biochemistry & Molecular Biology

Synthesis and biological evaluation of pyrido[2,3-d]pyrimidine-2,4-dione derivatives as eEF-2K inhibitors

Ramakrishna Edupuganti et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2014)

Article Chemistry, Medicinal

Irreversible 4-Aminopiperidine Transglutaminase 2 Inhibitors for Huntington's Disease

Michael E. Prime et al.

ACS MEDICINAL CHEMISTRY LETTERS (2012)

Article Multidisciplinary Sciences

Structure and function of an irreversible agonist-β2 adrenoceptor complex

Daniel M. Rosenbaum et al.

NATURE (2011)

Article Neurosciences

Structure based prediction of subtype-selectivity for adenosine receptor antagonists

Vsevolod Katritch et al.

NEUROPHARMACOLOGY (2011)

Article Biochemistry & Molecular Biology

GPCR 3D homology models for ligand screening: Lessons learned from blind predictions of adenosine A2a receptor complex

Vsevolod Katritch et al.

PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS (2010)

Article Biotechnology & Applied Microbiology

Community-wide assessment of GPCR structure modelling and ligand docking: GPCR Dock 2008

Mayako Michino et al.

NATURE REVIEWS DRUG DISCOVERY (2009)

Article Pharmacology & Pharmacy

The impact of adenosine and A2B receptors on glucose homoeostasis

D. Ruesing et al.

JOURNAL OF PHARMACY AND PHARMACOLOGY (2006)

Article Pharmacology & Pharmacy

Antinociceptive effects of novel A(2B) adenosine receptor antagonists

OM Abo-Salem et al.

JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS (2004)

Article Chemistry, Medicinal

1,8-disubstituted xanthine derivatives:: Synthesis of potent A2B-selective adenosine receptor antagonists

AM Hayallah et al.

JOURNAL OF MEDICINAL CHEMISTRY (2002)

Article Biochemistry & Molecular Biology

The Protein Data Bank

HM Berman et al.

NUCLEIC ACIDS RESEARCH (2000)