6d26: Difference between revisions

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'''Unreleased structure'''


The entry 6d26 is ON HOLD until Paper Publication
==Crystal structure of the prostaglandin D2 receptor CRTH2 with fevipiprant==
 
<StructureSection load='6d26' size='340' side='right' caption='[[6d26]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
Authors:  
== Structural highlights ==
 
<table><tr><td colspan='2'>[[6d26]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D26 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D26 FirstGlance]. <br>
Description:  
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=FSY:fevipiprant'>FSY</scene>, <scene name='pdbligand=OLA:OLEIC+ACID'>OLA</scene>, <scene name='pdbligand=PGE:TRIETHYLENE+GLYCOL'>PGE</scene>, <scene name='pdbligand=PGO:S-1,2-PROPANEDIOL'>PGO</scene>, <scene name='pdbligand=SIN:SUCCINIC+ACID'>SIN</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
[[Category: Unreleased Structures]]
<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=YCM:S-(2-AMINO-2-OXOETHYL)-L-CYSTEINE'>YCM</scene></td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[6d27|6d27]]</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=6d26 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d26 OCA], [http://pdbe.org/6d26 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d26 RCSB], [http://www.ebi.ac.uk/pdbsum/6d26 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d26 ProSAT]</span></td></tr>
</table>
== Function ==
[[http://www.uniprot.org/uniprot/PD2R2_HUMAN PD2R2_HUMAN]] Receptor for prostaglandin D2 (PGD2). Coupled to the G(i)-protein. Receptor activation may result in pertussis toxin-sensitive decreases in cAMP levels and Ca(2+) mobilization. PI3K signaling is also implicated in mediating PTGDR2 effects. PGD2 induced receptor internalization. CRTH2 internalization can be regulated by diverse kinases such as, PKC, PKA, GRK2, GPRK5/GRK5 and GRK6. Receptor activation is responsible, at least in part, in immune regulation and allergic/inflammation responses.<ref>PMID:11208866</ref> <ref>PMID:11535533</ref> <ref>PMID:17196174</ref>  
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Deepak, K]]
[[Category: Fan, H]]
[[Category: Gong, W]]
[[Category: Liu, H]]
[[Category: Wang, L]]
[[Category: Wei, Z]]
[[Category: Yao, D]]
[[Category: Zhang, C]]
[[Category: Gpcr]]
[[Category: Membrane protein-antagonist complex]]

Revision as of 10:46, 3 October 2018

Crystal structure of the prostaglandin D2 receptor CRTH2 with fevipiprantCrystal structure of the prostaglandin D2 receptor CRTH2 with fevipiprant

Structural highlights

6d26 is a 1 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:, , , , ,
NonStd Res:
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[PD2R2_HUMAN] Receptor for prostaglandin D2 (PGD2). Coupled to the G(i)-protein. Receptor activation may result in pertussis toxin-sensitive decreases in cAMP levels and Ca(2+) mobilization. PI3K signaling is also implicated in mediating PTGDR2 effects. PGD2 induced receptor internalization. CRTH2 internalization can be regulated by diverse kinases such as, PKC, PKA, GRK2, GPRK5/GRK5 and GRK6. Receptor activation is responsible, at least in part, in immune regulation and allergic/inflammation responses.[1] [2] [3]

References

  1. Hirai H, Tanaka K, Yoshie O, Ogawa K, Kenmotsu K, Takamori Y, Ichimasa M, Sugamura K, Nakamura M, Takano S, Nagata K. Prostaglandin D2 selectively induces chemotaxis in T helper type 2 cells, eosinophils, and basophils via seven-transmembrane receptor CRTH2. J Exp Med. 2001 Jan 15;193(2):255-61. PMID:11208866
  2. Monneret G, Gravel S, Diamond M, Rokach J, Powell WS. Prostaglandin D2 is a potent chemoattractant for human eosinophils that acts via a novel DP receptor. Blood. 2001 Sep 15;98(6):1942-8. PMID:11535533
  3. Xue L, Gyles SL, Barrow A, Pettipher R. Inhibition of PI3K and calcineurin suppresses chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2)-dependent responses of Th2 lymphocytes to prostaglandin D(2). Biochem Pharmacol. 2007 Mar 15;73(6):843-53. doi: 10.1016/j.bcp.2006.11.021. Epub, 2006 Dec 1. PMID:17196174 doi:http://dx.doi.org/10.1016/j.bcp.2006.11.021

6d26, resolution 2.80Å

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OCA