Crystal structure of the prostaglandin D2 receptor CRTH2 with CAY10471Crystal structure of the prostaglandin D2 receptor CRTH2 with CAY10471

Structural highlights

6d27 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

6d27, resolution 2.74Å

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