Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity.

doi:10.1124/mol.116.105015

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Article

Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity.

Molecular pharmacology - 1 Dec 2016

Nguyen Anh T N, Vecchio Elizabeth A, Thomas Trayder, Nguyen Toan D, Aurelio Luigi, Scammells Peter J, White Paul J, Sexton Patrick M, Gregory Karen J, May Lauren T, Christopoulos Arthur

Abstract excerpt

Allosteric modulation of adenosine A1 receptors (A1ARs) offers a novel therapeutic approach for the treatment of numerous central and peripheral disorders; however, despite decades of research, there is a relative paucity of structural information regarding the A1AR allosteric site and mechanisms governing cooperativity with orthosteric ligands. We combined alanine-scanning mutagenesis of the A1AR second...

Topics

Adenosine
Alanine
Allosteric Regulation
Allosteric Site
Animals
Binding Sites
CHO Cells
Cricetinae
Cricetulus
Cyclic AMP
Humans
Ligands
Molecular Dynamics Simulation

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Mutation

Protein Structure, Secondary

Receptor, Adenosine A1

Signal Transduction

Structural Homology, Protein

Source

Open in PubMed

Identifiers

PMID: 27683013
DOI: 10.1124/mol.116.105015

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 30 Aug 2026.