Adenosine A2A receptor as a potential drug target-current status and future perspectives

OHA Al-Attraqchi, M Attimarad… - Current …, 2019 - ingentaconnect.com
Adenosine receptors (ARs) are a class of G-protein coupled receptors (GPCRs) that are
activated by the endogenous substance adenosine. ARs are classified into 4 subtype …

MicroRNAs modulate the purinergic signaling network

D Ferrari, N Bianchi, HK Eltzschig, R Gambari - Trends in molecular …, 2016 - cell.com
MicroRNAs (miRNAs) are small non-coding RNA molecules capable of silencing mRNA
targets. miRNA dysregulation has been linked to cancer development, cardiovascular and …

Photoaffinity Labeling of the Human A2A Adenosine Receptor and Cross-link Position Analysis by Mass Spectrometry

H Muranaka, T Momose, C Handa… - ACS Medicinal …, 2017 - ACS Publications
Photoaffinity labeling (PAL) is widely used for the identification of ligand-binding proteins
and elucidation of ligand-binding sites. PAL has also been employed for the characterization …

In Silico Repositioning Strategies of Theobromine and Caffeine for Psychiatric and Neurological Disorders

DRT Sari, GC Krisnamurti - Proceeding International Conference …, 2022 - sunankalijaga.org
Psychiatric and neurological disorders (PNDs) have correlated diseases and represent a
burden on public health. Several drugs are reported to repurpose PNDs therapy. Drugs with …

The adenosine A2A receptor in human sperm: its role in sperm motility and association with in vitro fertilization outcomes

H Chen, G Xing, W Xu, Y Chen, L Xia… - Frontiers in …, 2024 - frontiersin.org
Background The involvement of ATP and cAMP in sperm function has been extensively
documented, but the understanding of the role of adenosine and adenosine receptors …

Bitopic fluorescent antagonists of the A 2A adenosine receptor based on pyrazolo [4, 3-e][1, 2, 4] triazolo [1, 5-c] pyrimidin-5-amine functionalized congeners

R Duroux, A Ciancetta, P Mannes, J Yu, S Boyapati… - …, 2017 - pubs.rsc.org
A pyrazolo [4, 3-e][1, 2, 4] triazolo [1, 5-c] pyrimidin-5-amine antagonist of the A2A
adenosine receptor (AR) was functionalized as amine congeners, fluorescent conjugates …

Fluorinated Adenosine A2A Receptor Antagonists Inspired by Preladenant as Potential Cancer Immunotherapeutics

G Yuan, TC Jankins, CG Patrick Jr… - … Journal of Medicinal …, 2017 - Wiley Online Library
Antagonism of the adenosine A2A receptor on T cells blocks the hypoxia‐adenosinergic
pathway to promote tumor rejection. Using an in vivo immunoassay based on the …

Biophysical Dissection of Isolated GPCRs: The Adenosine A2A Receptor under the Bistouries

JL Banères, T Botzanowski, JA Boutin, B Calamini… - Receptors, 2023 - mdpi.com
In an effort to provide an overview of the biophysical approaches used to study G-protein-
coupled receptors, we chose to consider the adenosine A2A receptor as a model, as it is …

Identifying and quantifying allosteric drug function

T Kenakin - 2016 - books.rsc.org
2.1 Introduction: Receptor Allosterism allosteric molecules are fundamentally different from
molecules that bind to the natural receptor binding pocket for endogenous hormones and …

Structure‐based identification of dual ligands at the A2AR and PDE10A with anti‐proliferative effects in lung cancer cell‐lines

L Kalash, I Winfield, D Safitri, M Bermudez… - Journal of …, 2021 - Springer
Enhanced/prolonged cAMP signalling has been suggested as a suppressor of cancer
proliferation. Interestingly, two key modulators that elevate cAMP, the A 2A receptor (A 2A R) …