title: 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.
authors.affiliation: Department of Physiology and Biophysics, Weill Medical College of Cornell University, New York, NY, USA. les2007@med.cornell.edu.
authors.forename: Mayako
authors.initials: M
authors.lastname: Michino
authors.forename: R Benjamin
authors.initials: RB
authors.lastname: Free
authors.forename: Trevor B
authors.initials: TB
authors.lastname: Doyle
authors.forename: David R
authors.initials: DR
authors.lastname: Sibley
authors.forename: Lei
authors.initials: L
authors.lastname: Shi
mesh_terms: D001549:Benzamides / Q000737:chemistry / Q000494:pharmacology; D001665:Binding Sites / Q000187:drug effects; D018492:Dopamine Antagonists / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D008024:Ligands; D056004:Molecular Dynamics Simulation; D015394:Molecular Structure; D011487:Protein Conformation / Q000187:drug effects; D017448:Receptors, Dopamine D2 / Q000737:chemistry / Q000378:metabolism*; D050637:Receptors, Dopamine D3 / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism*; D012457:Salicylamides / Q000737:chemistry / Q000494:pharmacology; D012964:Sodium / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013469:Sulpiride / Q000737:chemistry / Q000494:pharmacology
chemical_list: D001549:Benzamides; D018492:Dopamine Antagonists; D008024:Ligands; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; D012457:Salicylamides; D013469:Sulpiride; D012964:Sodium; C045989:eticlopride