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Article

Sodium ion binding pocket mutations and adenosine A2A receptor function.

Molecular pharmacology - 1 Feb 2015

Massink Arnault, Gutiérrez-de-Terán Hugo, Lenselink Eelke B, Ortiz Zacarías Natalia V, Xia Lizi, Heitman Laura H, Katritch Vsevolod, Stevens Raymond C, IJzerman Adriaan P

Abstract excerpt

Recently we identified a sodium ion binding pocket in a high-resolution structure of the human adenosine A2A receptor. In the present study we explored this binding site through site-directed mutagenesis and molecular dynamics simulations. Amino acids in the pocket were mutated to alanine, and their influence on agonist and antagonist affinity, allosterism by sodium ions and amilorides, and receptor functionality...

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Identifiers

PMID: 25473121
DOI: 10.1124/mol.114.095737
PMCID: PMC6067640

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