Structural Characterization of Agonist Binding to an A3 Adenosine Receptor through Biomolecular Simulations and Mutagenesis Experiments

D Stamatis, P Lagarias, K Barkan… - Journal of medicinal …, 2019 - ACS Publications
second extracellular loop 2 (EL2) to the recognition and binding of NECA (2). These included
the mutation of residues … a glutamic acid residue in the same position. It is speculated that …

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

OHA Al-Attraqchi, M Attimarad… - Current …, 2019 - ingentaconnect.com
… of human origin consists of 412 amino acid residues, however, A2AAR cloned from species
other than humans … The 2.6 angstrom crystal structure of a human A2A adenosine receptor

[HTML][HTML] Allosteric Modulation of Adenosine A2A Receptors as a New Therapeutic Avenue

M Korkutata, L Agrawal, M Lazarus - International Journal of Molecular …, 2022 - mdpi.com
residues, histidine residue number 278 (His 278 ) in transmembrane domain 1 and glutamic
acid 13 in transmembrane domain 7 of the human … of the human A 2A adenosine receptor

[HTML][HTML] The ADORA1 mutation linked to early-onset Parkinson's disease alters adenosine A1-A2A receptor heteromer formation and function

LI Sarasola, CL Del Torrent, A Pérez-Arévalo… - Biomedicine & …, 2022 - Elsevier
… D 4 receptor (D 4 R), the adenosine receptor subtypes A 1 R … (SP) of the human metabotropic
glutamate receptor type 5, the … residues located at the end of the helix (Fig. 5 C), near the …

[HTML][HTML] Experimental and computational analysis of biased agonism on full-length and a C-terminally truncated adenosine A2A receptor

G Navarro, A Gonzalez, S Campanacci… - Computational and …, 2020 - Elsevier
… identified mammalian adenosine receptors (humans included… supplemented with 2 mM
L-glutamine, 1 mM sodium pyruvate… of adenosine derivatives with the S7.42 and H7.43 residues. …

[HTML][HTML] Identification of V6.51L as a selectivity hotspot in stereoselective A2B adenosine receptor antagonist recognition

X Wang, W Jespers, R Prieto-Díaz, M Majellaro… - Scientific Reports, 2021 - nature.com
… While this residue has been shown to be involved in ligand … , human embryonic kidney
(HEK) 293 cells were cultured as monolayers in DMEM supplemented with stable glutamine, 10% …

[HTML][HTML] Slow conformational dynamics of the human A2A adenosine receptor are temporally ordered

S Wei, N Thakur, AP Ray, B Jin, S Obeng, CR McCurdy… - Structure, 2022 - cell.com
… (TIRF) imaging to investigate the conformational dynamics of the human A 2A adenosine
receptor (A 2A AR), a class AG protein-coupled receptor (GPCR), at the single-molecule level. …

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

AP IJzerman, KA Jacobson, CE Müller… - Pharmacological …, 2022 - ASPET
… of adenosine receptors, to examine a multitude of receptor structures and novel ligands,
to gauge new pharmacology, and to evaluate clinical trials with adenosine receptor ligands. …

Classification model for the second extracellular loop of class A GPCRs

A Nicoli, A Dunkel, T Giorgino, C de Graaf… - Journal of Chemical …, 2022 - ACS Publications
… refer to the region between residues 4.57 and 5.37 as the ECL2 loop. The composition of …
the ECL2 of the adenosine receptors A1 and A2a. The ECL2 of A1 and A2a share the same …

[HTML][HTML] Pyrazolo-triazolo-pyrimidine Scaffold as a Molecular Passepartout for the Pan-Recognition of Human Adenosine Receptors

V Salmaso, M Persico, T Da Ros, G Spalluto, S Kachler… - Biomolecules, 2023 - mdpi.com
… in the hA 1 and hA 2A ARs, thanks to a glutamate residue on EL2 (E172 for hA 1 and E169
hA … hA 2B AR subtype; even if it bears a glutamate residue on EL2 as with the hA 1 and hA 2A …