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


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.

SUBMITTER: Michino M 

PROVIDER: S-EPMC5234269 | biostudies-literature | 2015 May

REPOSITORIES: biostudies-literature

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

Michino Mayako M   Free R Benjamin RB   Doyle Trevor B TB   Sibley David R DR   Shi Lei L  

Chemical communications (Cambridge, England) 20150501 41


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. ...[more]

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