Human A2A adenosine receptors: high-affinity agonist binding to receptor-G protein complexes containing Gβ4

LJ Murphree, MA Marshall, JM Rieger… - Molecular …, 2002 - ASPET
Agonists bind with higher affinity to G protein-coupled heptahelical receptors than to
uncoupled receptors. Recombinant A1 and A3 adenosine receptors couple well to Gi/o, but …

[HTML][HTML] Glutamate residues in the second extracellular loop of the human A2a adenosine receptor are required for ligand recognition

J Kim, Q Jiang, M Glashofer, S Yehle… - Molecular …, 1996 - ncbi.nlm.nih.gov
The A 2a adenosine receptor, a member of the G protein-coupled receptor family, is
important in the regulation of dopaminergic pathways of the brain and in platelet and …

[HTML][HTML] Identification of Domains of the Human A1 Adenosine Receptor That Are Important for Binding Receptor Subtype-selective Ligands Using Chimeric A1/A2a …

SA Rivkees, ME Lasbury, H Barbhaiya - Journal of Biological Chemistry, 1995 - ASBMB
To provide new insights into the regions of the human A 1 adenosine receptor (A 1 AR)
involved in ligand binding, a series of chimeric human A 1 and rat A 1 adenosine receptors …

[HTML][HTML] Site-directed Mutagenesis Identifies Residues Involved in Ligand Recognition in the Human A2a Adenosine Receptor∗

J Kim, J Wess, AM van Rhee, T Schöneberg… - Journal of Biological …, 1995 - ASBMB
The A 2a adenosine receptor is a member of the G-protein coupled receptor family, and its
activation stimulates cyclic AMP production. To determine the residues which are involved in …

Constitutive activation of A3 adenosine receptors by site-directed mutagenesis

A Chen, ZG Gao, D Barak, BT Liang… - … and biophysical research …, 2001 - Elsevier
The objective of this study was to create constitutively active mutant human A3 adenosine
receptors (ARs) using single amino acid replacements, based on findings from other G …

[HTML][HTML] Serine and alanine mutagenesis of the nine native cysteine residues of the human A1 adenosine receptor

DJ Scholl, JN Wells - Biochemical pharmacology, 2000 - Elsevier
To examine the importance of the nine native cysteine residues in the human A1 adenosine
receptor, each cysteine was individually mutated to both serine and alanine. Saturation …

Coupling of the human A1 adenosine receptor to different heterotrimeric G proteins: evidence for agonist‐specific G protein activation

Y Cordeaux, AP IJzerman, SJ Hill - British journal of …, 2004 - Wiley Online Library
The present study investigates the effect of varying ligand structure on the ability of agonists
to activate guanine nucleotide‐binding proteins of the Gi, Gs and Gq families via the A1 …

[HTML][HTML] A2A and A2B adenosine receptors: The extracellular loop 2 determines high (A2A) or low affinity (A2B) for adenosine

E De Filippo, S Hinz, V Pellizzari, G Deganutti… - Biochemical …, 2020 - Elsevier
Abstract A 2A and A 2B adenosine receptors (ARs) are closely related G protein-coupled
receptor subtypes, which represent important (potential) drug targets. Despite their almost …

[HTML][HTML] Site-directed mutagenesis studies of human A2A adenosine receptors: involvement of Glu13 and His278 in ligand binding and sodium modulation

ZG Gao, Q Jiang, KA Jacobson, AP Ijzerman - Biochemical pharmacology, 2000 - Elsevier
To provide insights into interactions between ligands and A2A adenosine receptors, site-
directed mutagenesis was used to test the roles of a glutamic acid residue in the first …

[HTML][HTML] Identification by site-directed mutagenesis of residues involved in ligand recognition and activation of the human A3 adenosine receptor

ZG Gao, A Chen, D Barak, SK Kim, CE Müller… - Journal of Biological …, 2002 - ASBMB
Ligand recognition has been extensively explored in G protein-coupled A 1, A 2A, and A 2B
adenosine receptors but not in the A 3 receptor, which is cerebroprotective and …