International union of basic and clinical pharmacology. CXII: adenosine receptors: a further update

AP IJzerman, KA Jacobson, CE Müller… - Pharmacological …, 2022 - Elsevier
Abstract Our previous International Union of Basic and Clinical Pharmacology report on the
nomenclature and classification of adenosine receptors (2011) contained a number of …

Pharmacology of adenosine receptors: the state of the art

PA Borea, S Gessi, S Merighi… - Physiological …, 2018 - journals.physiology.org
Adenosine is a ubiquitous endogenous autacoid whose effects are triggered through the
enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Due to the rapid …

Comparative studies of AlphaFold, RoseTTAFold and Modeller: a case study involving the use of G-protein-coupled receptors

C Lee, BH Su, YJ Tseng - Briefings in bioinformatics, 2022 - academic.oup.com
Neural network (NN)-based protein modeling methods have improved significantly in recent
years. Although the overall accuracy of the two non-homology-based modeling methods …

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

J García-Nafría, Y Lee, X Bai, B Carpenter, CG Tate - elife, 2018 - elifesciences.org
The adenosine A2A receptor (A2AR) is a prototypical G protein-coupled receptor (GPCR)
that couples to the heterotrimeric G protein GS. Here, we determine the structure by electron …

Allosteric coupling of drug binding and intracellular signaling in the A2A adenosine receptor

MT Eddy, MY Lee, ZG Gao, KL White, T Didenko… - Cell, 2018 - cell.com
Signaling across cellular membranes, the 826 human G protein-coupled receptors (GPCRs)
govern a wide range of vital physiological processes, making GPCRs prominent drug …

Small molecule allosteric modulators of G-protein-coupled receptors: drug–target interactions

S Lu, J Zhang - Journal of medicinal chemistry, 2018 - ACS Publications
G-protein-coupled receptors (GPCRs) are the largest class of signaling receptors that are
most frequently targeted by therapeutic drugs. Allosteric modulators bound to GPCRs at …

Adenosine receptor antagonists: Recent advances and therapeutic perspective

A Saini, R Patel, S Gaba, G Singh, GD Gupta… - European Journal of …, 2022 - Elsevier
Adenosine is an endogenous purine-based nucleoside expressed nearly in all body tissues.
It regulates various body functions by activating four G-protein coupled receptors, A 1, A 2A …

A2A adenosine receptor functional states characterized by 19F-NMR

L Sušac, MT Eddy, T Didenko… - Proceedings of the …, 2018 - National Acad Sciences
The human proteome contains 826 G protein-coupled receptors (GPCR), which control a
wide array of key physiological functions, making them important drug targets. GPCR …

Adenosine A2A receptor antagonists: from caffeine to selective non‐xanthines

KA Jacobson, ZG Gao, P Matricon… - British journal of …, 2022 - Wiley Online Library
A long evolution of knowledge of the psychostimulant caffeine led in the 1960s to another
purine natural product, adenosine and its A2A receptor. Adenosine is a short‐lived …

Adenosine A2A Receptor Antagonists for Cancer Immunotherapy: Miniperspective

F Yu, C Zhu, Q Xie, Y Wang - Journal of Medicinal Chemistry, 2020 - ACS Publications
Currently, the most promising therapeutic modality for cancer treatment is the blockade of
immune checkpoint pathways, which has revolutionized cancer therapy in the past 15 years …