3pbl | pdb_00003pbl

Structure of the human dopamine D3 receptor in complex with eticlopride

spinqualitylabelsall models 3pbl, resolution 2.89Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3pbl is a 2 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: ETQ, MAL Gene: DRD3, E (HUMAN) Activity: Lysozyme, with EC number 3.2.1.17 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Disease [DRD3_HUMAN] Hereditary essential tremor. Disease susceptibility is associated with variations affecting the gene represented in this entry. Function [DRD3_HUMAN] Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation. Publication Abstract from PubMed Dopamine modulates movement, cognition, and emotion through activation of dopamine G protein-coupled receptors in the brain. The crystal structure of the human dopamine D3 receptor (D3R) in complex with the small molecule D2R/D3R-specific antagonist eticlopride reveals important features of the ligand binding pocket and extracellular loops. On the intracellular side of the receptor, a locked conformation of the ionic lock and two distinctly different conformations of intracellular loop 2 are observed. Docking of R-22, a D3R-selective antagonist, reveals an extracellular extension of the eticlopride binding site that comprises a second binding pocket for the aryl amide of R-22, which differs between the highly homologous D2R and D3R. This difference provides direction to the design of D3R-selective agents for treating drug abuse and other neuropsychiatric indications. Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist.,Chien EY, Liu W, Zhao Q, Katritch V, Han GW, Hanson MA, Shi L, Newman AH, Javitch JA, Cherezov V, Stevens RC Science. 2010 Nov 19;330(6007):1091-5. PMID:21097933 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Dopamine Receptors Lysozyme 3D structures

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