[HTML][HTML] Mechanistic insights into allosteric regulation of the A2A adenosine G protein-coupled receptor by physiological cations

L Ye, C Neale, A Sljoka, B Lyda, D Pichugin… - Nature …, 2018 - nature.com
Cations play key roles in regulating G-protein-coupled receptors (GPCRs), although their
mechanisms are poorly understood. Here, 19F NMR is used to delineate the effects of …

[HTML][HTML] The role of a sodium ion binding site in the allosteric modulation of the A2A adenosine G protein-coupled receptor

H Gutiérrez-de-Terán, A Massink, D Rodríguez, W Liu… - Structure, 2013 - cell.com
The function of G protein-coupled receptors (GPCRs) can be modulated by a number of
endogenous allosteric molecules. In this study, we used molecular dynamics, radioligand …

[HTML][HTML] Delineating the conformational landscape of the adenosine A2A receptor during G protein coupling

SK Huang, A Pandey, DP Tran, NL Villanueva, A Kitao… - Cell, 2021 - cell.com
G-protein-coupled receptors (GPCRs) represent a ubiquitous membrane protein family and
are important drug targets. Their diverse signaling pathways are driven by complex …

[HTML][HTML] 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 …

[HTML][HTML] Single-molecule visualization of human A2A adenosine receptor activation by a G protein and constitutively activating mutations

S Wei, NG Pour, S Tiruvadi-Krishnan, AP Ray… - Communications …, 2023 - nature.com
Mutations that constitutively activate G protein-coupled receptors (GPCRs), known as
constitutively activating mutations (CAMs), modify cell signaling and interfere with drugs …

[HTML][HTML] Intermediate-state-trapped mutants pinpoint G protein-coupled receptor conformational allostery

X Wang, C Neale, SK Kim, WA Goddard… - Nature Communications, 2023 - nature.com
Understanding the roles of intermediate states in signaling is pivotal to unraveling the
activation processes of G protein-coupled receptors (GPCRs). However, the field is still …

Allosteric interactions at adenosine A1 and A3 receptors: new insights into the role of small molecules and receptor dimerization

SJ Hill, LT May, B Kellam… - British journal of …, 2014 - Wiley Online Library
The purine nucleoside adenosine is present in all cells in tightly regulated concentrations. It
is released under a variety of physiological and pathophysiological conditions to facilitate …

Structural basis for allosteric regulation of GPCRs by sodium ions

W Liu, E Chun, AA Thompson, P Chubukov, F Xu… - Science, 2012 - science.org
Pharmacological responses of G protein–coupled receptors (GPCRs) can be fine-tuned by
allosteric modulators. Structural studies of such effects have been limited due to the medium …

[HTML][HTML] Anionic phospholipids control mechanisms of GPCR-G protein recognition

N Thakur, AP Ray, L Sharp, B Jin, A Duong… - Nature …, 2023 - nature.com
G protein-coupled receptors (GPCRs) are embedded in phospholipids that strongly
influence drug-stimulated signaling. Anionic lipids are particularly important for GPCR …

The role of the second and third extracellular loops of the adenosine A1 receptor in activation and allosteric modulation

MC Peeters, LE Wisse, A Dinaj, B Vroling… - Biochemical …, 2012 - Elsevier
The adenosine A1 receptor is a member of the large membrane protein family that signals
through G proteins, the G protein-coupled receptors (GPCRs). GPCRs consist of seven …