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 …

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 …

[HTML][HTML] Structure of the adenosine A1 receptor reveals the basis for subtype selectivity

A Glukhova, DM Thal, AT Nguyen, EA Vecchio, M Jörg… - Cell, 2017 - cell.com
The adenosine A 1 receptor (A 1-AR) is a G-protein-coupled receptor that plays a vital role in
cardiac, renal, and neuronal processes but remains poorly targeted by current drugs. We …

Xanomeline displays concomitant orthosteric and allosteric binding modes at the M4 mAChR

WAC Burger, V Pham, Z Vuckovic, AS Powers… - Nature …, 2023 - nature.com
The M4 muscarinic acetylcholine receptor (M4 mAChR) has emerged as a drug target of
high therapeutic interest due to its expression in regions of the brain involved in the …

Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength

E Segala, D Guo, RKY Cheng, A Bortolato… - Journal of medicinal …, 2016 - ACS Publications
The association and dissociation kinetics of ligands binding to proteins vary considerably,
but the mechanisms behind this variability are poorly understood, limiting their utilization for …

Cryo-EM structure of the human adenosine A2B receptor–Gs signaling complex

Y Chen, J Zhang, Y Weng, Y Xu, W Lu, W Liu, M Liu… - Science …, 2022 - science.org
The human adenosine A2B receptor (A2BR) is a class AG protein–coupled receptor that is
involved in several major physiological and pathological processes throughout the body …

Unbiased molecular dynamics of 11 min timescale drug unbinding reveals transition state stabilizing interactions

SD Lotz, A Dickson - Journal of the American Chemical Society, 2018 - ACS Publications
Ligand (un) binding kinetics is being recognized as a determinant of drug specificity and
efficacy in an increasing number of systems. However, the calculation of kinetics and the …

Predicting binding affinities for GPCR ligands using free-energy perturbation

EB Lenselink, J Louvel, AF Forti… - ACS …, 2016 - ACS Publications
The rapid growth of structural information for G-protein-coupled receptors (GPCRs) has led
to a greater understanding of their structure, function, selectivity, and ligand binding …

Human Adenosine A2A Receptor: Molecular Mechanism of Ligand Binding and Activation

B Carpenter, G Lebon - Frontiers in pharmacology, 2017 - frontiersin.org
Adenosine receptors (ARs) comprise the P1 class of purinergic receptors and belong to the
largest family of integral membrane proteins in the human genome, the G protein-coupled …

[HTML][HTML] Genetic characteristics involving the PD-1/PD-L1/L2 and CD73/A2aR axes and the immunosuppressive microenvironment in DLBCL

T Zhang, H Liu, L Jiao, Z Zhang, J He, L Li… - … for Immunotherapy of …, 2022 - ncbi.nlm.nih.gov
Background Targeting the PD-1/PD-L1/L2 (programmed cell death protein 1/programmed
cell death ligand 1/ligand 2) pathway combined with other immunosuppressive signalings …