6bqh: Difference between revisions
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==Crystal structure of 5-HT2C in complex with ritanserin== | |||
<StructureSection load='6bqh' size='340' side='right' caption='[[6bqh]], [[Resolution|resolution]] 2.70Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[6bqh]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6BQH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6BQH FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=E2J:6-(2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl)-7-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one'>E2J</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene></td></tr> | |||
[[Category: | <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=6bqh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6bqh OCA], [http://pdbe.org/6bqh PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6bqh RCSB], [http://www.ebi.ac.uk/pdbsum/6bqh PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6bqh ProSAT]</span></td></tr> | ||
</table> | |||
== Function == | |||
[[http://www.uniprot.org/uniprot/5HT2C_HUMAN 5HT2C_HUMAN]] G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelacortin neurons and the release of CRH that then regulates the release of corticosterone. Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress. Plays a role in insulin sensitivity and glucose homeostasis.<ref>PMID:12970106</ref> <ref>PMID:18703043</ref> <ref>PMID:19057895</ref> <ref>PMID:7895773</ref> | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Bjorn-Yoshimoto, W E]] | |||
[[Category: Che, T]] | |||
[[Category: Cheng, J]] | |||
[[Category: Ding, K]] | |||
[[Category: Gloriam, D E]] | |||
[[Category: Han, G W]] | |||
[[Category: Hanson, M A]] | |||
[[Category: Harpsoe, K]] | |||
[[Category: Huang, X P]] | |||
[[Category: Jensen, A A]] | |||
[[Category: Katritch, V]] | |||
[[Category: Lansu, K]] | |||
[[Category: Liu, Z]] | |||
[[Category: McCorvy, J D]] | |||
[[Category: Nikolajse, L F]] | |||
[[Category: Peng, Y]] | |||
[[Category: Popov, P]] | |||
[[Category: Pu, M]] | |||
[[Category: Qu, L]] | |||
[[Category: Roth, B L]] | |||
[[Category: Shen, L]] | |||
[[Category: Stevens, R C]] | |||
[[Category: Wacker, D]] | |||
[[Category: Wu, Y]] | |||
[[Category: Yuan, S]] | |||
[[Category: Zhao, S]] | |||
[[Category: Bril]] | |||
[[Category: Gpcr]] | |||
[[Category: Human 5-ht2c receptor]] | |||
[[Category: Lcp]] | |||
[[Category: Membrane protein]] | |||
[[Category: Ritanserin]] | |||
[[Category: Selectivity]] | |||