3pbl
From Proteopedia
Structure of the human dopamine D3 receptor in complex with eticlopride
Structural highlights
DiseaseDRD3_HUMAN Hereditary essential tremor. Disease susceptibility is associated with variations affecting the gene represented in this entry. FunctionENLYS_BPT4 Endolysin with lysozyme activity that degrades host peptidoglycans and participates with the holin and spanin proteins in the sequential events which lead to the programmed host cell lysis releasing the mature viral particles. Once the holin has permeabilized the host cell membrane, the endolysin can reach the periplasm and break down the peptidoglycan layer.[1] DRD3_HUMAN Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.[2] Publication Abstract from PubMedDopamine 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[3] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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Categories: Escherichia virus T4 | Homo sapiens | Large Structures | Cherezov V | Chien EYT | Han GW | Katritch V | Liu W | Stevens RC | Zhao Q
