3pbl

From Proteopedia

(Difference between revisions)

Current revision

Structure of the human dopamine D3 receptor in complex with eticlopride

Structural highlights

3pbl is a 2 chain structure with sequence from Escherichia virus T4 and Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 2.89Å
Ligands:	, ,
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

ENLYS_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 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^[3]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Moussa SH, Kuznetsov V, Tran TA, Sacchettini JC, Young R. Protein determinants of phage T4 lysis inhibition. Protein Sci. 2012 Apr;21(4):571-82. doi: 10.1002/pro.2042. Epub 2012 Mar 2. PMID:22389108 doi:http://dx.doi.org/10.1002/pro.2042
↑ Villar VA, Jones JE, Armando I, Palmes-Saloma C, Yu P, Pascua AM, Keever L, Arnaldo FB, Wang Z, Luo Y, Felder RA, Jose PA. G protein-coupled receptor kinase 4 (GRK4) regulates the phosphorylation and function of the dopamine D3 receptor. J Biol Chem. 2009 Aug 7;284(32):21425-34. Epub 2009 Jun 11. PMID:19520868 doi:10.1074/jbc.M109.003665
↑ Chien EY, Liu W, Zhao Q, Katritch V, Han GW, Hanson MA, Shi L, Newman AH, Javitch JA, Cherezov V, Stevens RC. Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist. Science. 2010 Nov 19;330(6007):1091-5. PMID:21097933 doi:10.1126/science.1197410

1 Structural highlights
2 Disease
3 Function
4 Publication Abstract from PubMed
5 See Also
6 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/3pbl"

@@ Line 1: / Line 1: @@
-[[Image:3pbl.png|left|200px]]
-{{STRUCTURE_3pbl|  PDB=3pbl  |  SCENE=  }}
+==Structure of the human dopamine D3 receptor in complex with eticlopride==
+<StructureSection load='3pbl' size='340' side='right'caption='[[3pbl]], [[Resolution|resolution]] 2.89&Aring;' scene=''>
+== Structural highlights ==
+<table><tr><td colspan='2'>[[3pbl]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_virus_T4 Escherichia virus T4] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PBL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PBL FirstGlance]. <br>
+</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.89&#8491;</td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ETQ:3-CHLORO-5-ETHYL-N-{[(2S)-1-ETHYLPYRROLIDIN-2-YL]METHYL}-6-HYDROXY-2-METHOXYBENZAMIDE'>ETQ</scene>, <scene name='pdbligand=GLC:ALPHA-D-GLUCOSE'>GLC</scene>, <scene name='pdbligand=PRD_900001:alpha-maltose'>PRD_900001</scene></td></tr>
+<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3pbl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3pbl OCA], [https://pdbe.org/3pbl PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3pbl RCSB], [https://www.ebi.ac.uk/pdbsum/3pbl PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3pbl ProSAT]</span></td></tr>
+</table>
+== Disease ==
+[https://www.uniprot.org/uniprot/DRD3_HUMAN DRD3_HUMAN] Hereditary essential tremor. Disease susceptibility is associated with variations affecting the gene represented in this entry.
+== Function ==
+[https://www.uniprot.org/uniprot/ENLYS_BPT4 ENLYS_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.<ref>PMID:22389108</ref> [https://www.uniprot.org/uniprot/DRD3_HUMAN DRD3_HUMAN] Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.<ref>PMID:19520868</ref>
+<div style="background-color:#fffaf0;">
+== 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 eticlopride===
+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<ref>PMID:21097933</ref>
-{{ABSTRACT_PUBMED_21097933}}
+From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
+</div>
-==About this Structure==
+<div class="pdbe-citations 3pbl" style="background-color:#fffaf0;"></div>
-[[3pbl]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Enterobacteria_phage_t4 Enterobacteria phage t4]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PBL OCA].
 ==See Also==
-*[[G protein-coupled receptor|G protein-coupled receptor]]
+*[[Dopamine receptor|Dopamine receptor]]
-*[[Hen Egg-White (HEW) Lysozyme|Hen Egg-White (HEW) Lysozyme]]
+*[[Dopamine receptor 3D structures|Dopamine receptor 3D structures]]
-*[[Human dopamine d3 receptor|Human dopamine d3 receptor]]
+*[[Lysozyme 3D structures|Lysozyme 3D structures]]
+*[[Neurotransmitters|Neurotransmitters]]
-==Reference==
+== References ==
-<ref group="xtra">PMID:021097933</ref><references group="xtra"/>
+<references/>
-[[Category: Enterobacteria phage t4]]
+__TOC__
-[[Category: Lysozyme]]
+</StructureSection>
-[[Category: ATCG3D, Accelerated Technologies Center for Gene to 3D Structure.]]
+[[Category: Escherichia virus T4]]
-[[Category: Cherezov, V.]]
+[[Category: Homo sapiens]]
-[[Category: Chien, E Y.T.]]
+[[Category: Large Structures]]
-[[Category: GPCR, GPCR Network.]]
+[[Category: Cherezov V]]
-[[Category: Han, G W.]]
+[[Category: Chien EYT]]
-[[Category: Katritch, V.]]
+[[Category: Han GW]]
-[[Category: Liu, W.]]
+[[Category: Katritch V]]
-[[Category: Stevens, R C.]]
+[[Category: Liu W]]
-[[Category: Zhao, Q.]]
+[[Category: Stevens RC]]
-[[Category: 7tm]]
+[[Category: Zhao Q]]
-[[Category: Accelerated technologies center for gene to 3d structure]]
-[[Category: Atcg3d]]
-[[Category: Chimera]]
-[[Category: Dopamine]]
-[[Category: Eticlopride]]
-[[Category: G protein-coupled receptor]]
-[[Category: Gpcr]]
-[[Category: Gpcr network]]
-[[Category: Hydrolase]]
-[[Category: Hydrolase-hydrolase inhibitor complex]]
-[[Category: Membrane protein]]
-[[Category: Neurotransmitter]]
-[[Category: Protein structure initiative]]
-[[Category: Psi-2]]
-[[Category: Psi-biology]]
-[[Category: Signal transduction]]
-[[Category: Structural genomic]]
-[[Category: T4l fusion]]
-[[Category: Transmembrane]]

3pbl

From Proteopedia

Current revision

Structure of the human dopamine D3 receptor in complex with eticlopride

Structural highlights

Disease

Function

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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