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{{STRUCTURE_4ib4|  PDB=4ib4  |  SCENE=  }}
==Crystal structure of the chimeric protein of 5-HT2B-BRIL in complex with ergotamine==
===Crystal structure of the chimeric protein of 5-HT2B-BRIL in complex with ergotamine===
<StructureSection load='4ib4' size='340' side='right' caption='[[4ib4]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
{{ABSTRACT_PUBMED_23519215}}
== Structural highlights ==
<table><tr><td colspan='2'>[[4ib4]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/"bacillus_coli"_migula_1895 "bacillus coli" migula 1895]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4IB4 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4IB4 FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=ERM:ERGOTAMINE'>ERM</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLB:(2S)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLB</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene>, <scene name='pdbligand=PLM:PALMITIC+ACID'>PLM</scene></td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">5HT2B_HUMAN, cybC ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 "Bacillus coli" Migula 1895])</td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ib4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ib4 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ib4 RCSB], [http://www.ebi.ac.uk/pdbsum/4ib4 PDBsum]</span></td></tr>
</table>
== Function ==
[[http://www.uniprot.org/uniprot/5HT2B_HUMAN 5HT2B_HUMAN]] This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Plays a role in the regulation of impulsive behavior.
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Drugs active at G protein-coupled receptors (GPCRs) can differentially modulate either canonical or noncanonical signaling pathways via a phenomenon known as functional selectivity or biased signaling. We report biochemical studies that show that the hallucinogen lysergic acid diethylamide (LSD), its precursor ergotamine (ERG), and related ergolines display strong functional selectivity for beta-arrestin signaling at the 5-hydroxytryptamine (5-HT) receptor 5-HT2B, while being relatively unbiased at the 5-HT1B receptor. To investigate the structural basis for biased signaling, we determined the crystal structure of the human 5-HT2B receptor bound to ERG, and compared it with the 5-HT1B/ERG structure. Given the relatively poor understanding of GPCR structure-function to date, insight into different GPCR signaling pathways is important to better understand both adverse and favorable therapeutic activities.


==Function==
Structural Features for Functional Selectivity at Serotonin Receptors.,Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W, Xu HE, Cherezov V, Roth BL, Stevens RC Science. 2013 Mar 21. PMID:23519215<ref>PMID:23519215</ref>
[[http://www.uniprot.org/uniprot/5HT2B_HUMAN 5HT2B_HUMAN]] This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Plays a role in the regulation of impulsive behavior.  


==About this Structure==
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
[[4ib4]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4IB4 OCA].
</div>
[[Category: Cherezov, V.]]
== References ==
[[Category: Chu, M.]]
<references/>
[[Category: GPCR, GPCR Network.]]
__TOC__
[[Category: Han, G W.]]
</StructureSection>
[[Category: Huang, X.]]
[[Category: Bacillus coli migula 1895]]
[[Category: Jiang, Y.]]
[[Category: Cherezov, V]]
[[Category: Katritch, V.]]
[[Category: Chu, M]]
[[Category: Liu, W.]]
[[Category: GPCR, GPCR Network]]
[[Category: McCorvy, J D.]]
[[Category: Han, G W]]
[[Category: Roth, B L.]]
[[Category: Huang, X]]
[[Category: Siu, F Y.]]
[[Category: Jiang, Y]]
[[Category: Stevens, R C.]]
[[Category: Katritch, V]]
[[Category: Vardy, E.]]
[[Category: Liu, W]]
[[Category: Wacker, D.]]
[[Category: McCorvy, J D]]
[[Category: Wang, C.]]
[[Category: Roth, B L]]
[[Category: Xu, H E.]]
[[Category: Siu, F Y]]
[[Category: Stevens, R C]]
[[Category: Vardy, E]]
[[Category: Wacker, D]]
[[Category: Wang, C]]
[[Category: Xu, H E]]
[[Category: Electron transport]]
[[Category: Electron transport]]
[[Category: Ergotamine]]
[[Category: Ergotamine]]

Revision as of 14:51, 25 December 2014

Crystal structure of the chimeric protein of 5-HT2B-BRIL in complex with ergotamineCrystal structure of the chimeric protein of 5-HT2B-BRIL in complex with ergotamine

Structural highlights

4ib4 is a 1 chain structure with sequence from "bacillus_coli"_migula_1895 "bacillus coli" migula 1895. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:, , , , , ,
Gene:5HT2B_HUMAN, cybC ("Bacillus coli" Migula 1895)
Resources:FirstGlance, OCA, RCSB, PDBsum

Function

[5HT2B_HUMAN] This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Plays a role in the regulation of impulsive behavior.

Publication Abstract from PubMed

Drugs active at G protein-coupled receptors (GPCRs) can differentially modulate either canonical or noncanonical signaling pathways via a phenomenon known as functional selectivity or biased signaling. We report biochemical studies that show that the hallucinogen lysergic acid diethylamide (LSD), its precursor ergotamine (ERG), and related ergolines display strong functional selectivity for beta-arrestin signaling at the 5-hydroxytryptamine (5-HT) receptor 5-HT2B, while being relatively unbiased at the 5-HT1B receptor. To investigate the structural basis for biased signaling, we determined the crystal structure of the human 5-HT2B receptor bound to ERG, and compared it with the 5-HT1B/ERG structure. Given the relatively poor understanding of GPCR structure-function to date, insight into different GPCR signaling pathways is important to better understand both adverse and favorable therapeutic activities.

Structural Features for Functional Selectivity at Serotonin Receptors.,Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W, Xu HE, Cherezov V, Roth BL, Stevens RC Science. 2013 Mar 21. PMID:23519215[1]

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

References

  1. ↑ Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W, Xu HE, Cherezov V, Roth BL, Stevens RC. Structural Features for Functional Selectivity at Serotonin Receptors. Science. 2013 Mar 21. PMID:23519215 doi:http://dx.doi.org/10.1126/science.1232808

4ib4, resolution 2.70Å

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