6bqh: Difference between revisions

No edit summary
No edit summary
 
Line 1: Line 1:


==Crystal structure of 5-HT2C in complex with ritanserin==
==Crystal structure of 5-HT2C in complex with ritanserin==
<StructureSection load='6bqh' size='340' side='right' caption='[[6bqh]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
<StructureSection load='6bqh' size='340' side='right'caption='[[6bqh]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[6bqh]] 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=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>
<table><tr><td colspan='2'>[[6bqh]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] 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=6BQH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/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>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.7&#8491;</td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">HTR2C, HTR1C ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 "Bacillus coli" Migula 1895])</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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>
<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>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6bqh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6bqh OCA], [https://pdbe.org/6bqh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6bqh RCSB], [https://www.ebi.ac.uk/pdbsum/6bqh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6bqh ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== 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>
[https://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> [https://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX] Electron-transport protein of unknown function.
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
Line 19: Line 19:
</div>
</div>
<div class="pdbe-citations 6bqh" style="background-color:#fffaf0;"></div>
<div class="pdbe-citations 6bqh" style="background-color:#fffaf0;"></div>
==See Also==
*[[5-hydroxytryptamine receptor 3D structures|5-hydroxytryptamine receptor 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Bacillus coli migula 1895]]
[[Category: Escherichia coli]]
[[Category: Bjorn-Yoshimoto, W E]]
[[Category: Homo sapiens]]
[[Category: Che, T]]
[[Category: Large Structures]]
[[Category: Cheng, J]]
[[Category: Bjorn-Yoshimoto WE]]
[[Category: Ding, K]]
[[Category: Che T]]
[[Category: Gloriam, D E]]
[[Category: Cheng J]]
[[Category: Han, G W]]
[[Category: Ding K]]
[[Category: Hanson, M A]]
[[Category: Gloriam DE]]
[[Category: Harpsoe, K]]
[[Category: Han GW]]
[[Category: Huang, X P]]
[[Category: Hanson MA]]
[[Category: Jensen, A A]]
[[Category: Harpsoe K]]
[[Category: Katritch, V]]
[[Category: Huang XP]]
[[Category: Lansu, K]]
[[Category: Jensen AA]]
[[Category: Liu, Z]]
[[Category: Katritch V]]
[[Category: McCorvy, J D]]
[[Category: Lansu K]]
[[Category: Nikolajse, L F]]
[[Category: Liu Z]]
[[Category: Peng, Y]]
[[Category: McCorvy JD]]
[[Category: Popov, P]]
[[Category: Nikolajse LF]]
[[Category: Pu, M]]
[[Category: Peng Y]]
[[Category: Qu, L]]
[[Category: Popov P]]
[[Category: Roth, B L]]
[[Category: Pu M]]
[[Category: Shen, L]]
[[Category: Qu L]]
[[Category: Stevens, R C]]
[[Category: Roth BL]]
[[Category: Wacker, D]]
[[Category: Shen L]]
[[Category: Wu, Y]]
[[Category: Stevens RC]]
[[Category: Yuan, S]]
[[Category: Wacker D]]
[[Category: Zhao, S]]
[[Category: Wu Y]]
[[Category: Bril]]
[[Category: Yuan S]]
[[Category: Gpcr]]
[[Category: Zhao S]]
[[Category: Human 5-ht2c receptor]]
[[Category: Lcp]]
[[Category: Membrane protein]]
[[Category: Ritanserin]]
[[Category: Selectivity]]

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA