View source for 4ib4


==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=''>
== 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]. The August 2013 RCSB PDB [http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/index.html Molecule of the Month] feature on ''Serotonin Receptor''  by David Goodsell is [http://dx.doi.org/10.2210/rcsb_pdb/mom_2013_8 10.2210/rcsb_pdb/mom_2013_8]. 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">HTR2B ([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://pdbe.org/4ib4 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4ib4 RCSB], [http://www.ebi.ac.uk/pdbsum/4ib4 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4ib4 ProSAT]</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.

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>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 4ib4" style="background-color:#fffaf0;"></div>

==See Also==
*[[5-hydroxytryptamine receptor|5-hydroxytryptamine receptor]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Bacillus coli migula 1895]]
[[Category: RCSB PDB Molecule of the Month]]
[[Category: Serotonin Receptor]]
[[Category: Cherezov, V]]
[[Category: Chu, M]]
[[Category: GPCR, GPCR Network]]
[[Category: Han, G W]]
[[Category: Huang, X]]
[[Category: Jiang, Y]]
[[Category: Katritch, V]]
[[Category: Liu, W]]
[[Category: McCorvy, J D]]
[[Category: Roth, B L]]
[[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: Ergotamine]]
[[Category: Gpcr]]
[[Category: Gpcr dock]]
[[Category: Gpcr network]]
[[Category: Membrane protein]]
[[Category: Novel protein engineering]]
[[Category: Psi-biology]]
[[Category: Signaling protein]]
[[Category: Structural genomic]]