Structural basis for Na+-sensitivity in dopamine D2 and D3 receptors

Mayako Michino; R. Benjamin Free; Trevor B. Doyle; David R. Sibley; Lei Shi

doi:10.1039/C5CC02204E

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Structural basis for Na⁺-sensitivity in dopamine D2 and D3 receptors†

Mayako Michino,^ab R. Benjamin Free,^c Trevor B. Doyle,^c David R. Sibley^c and Lei Shi*^abd

Author affiliations

* Corresponding authors

^a Department of Physiology and Biophysics, Weill Medical College of Cornell University, New York, NY, USA
E-mail: les2007@med.cornell.edu

^b Computational Chemistry and Molecular Biophysics Unit, National Institute on Drug Abuse – Intramural Research Program, National Institutes of Health, Baltimore, MD, USA

^c Molecular Neuropharmacology Section, National Institute of Neurologic Disorders and Stroke, National Institutes of Health, Bethesda, MD, USA

^d Institute for Computational Biomedicine, Weill Medical College of Cornell University, New York, NY, USA

Abstract

To understand the structural basis for the Na⁺-sensitivity of ligand binding to dopamine D2-like receptors, using computational analysis in combination with binding assays, we identified interactions critical in propagating the impact of Na⁺ on receptor conformations and on the ligand-binding site. Our findings expand the pharmacologically-relevant conformational spectrum of these receptors.

This article is part of the themed collection: Identification and Optimization of GPCR Ligands in the 21st Century

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Article information

DOI: https://doi.org/10.1039/C5CC02204E
Article type: Communication
Submitted: 16 Mar 2015
Accepted: 07 Apr 2015
First published: 07 Apr 2015

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Chem. Commun., 2015,51, 8618-8621

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Structural basis for Na⁺-sensitivity in dopamine D2 and D3 receptors

M. Michino, R. B. Free, T. B. Doyle, D. R. Sibley and L. Shi, Chem. Commun., 2015, 51, 8618 DOI: 10.1039/C5CC02204E

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