Prostaglandin DP2 receptor

Prostaglandin D2 receptor 2
Identifiers
Symbols	PTGDR2 ; CD294; CRTH2; DL1R; DP2; GPR44
External IDs	OMIM: 604837 MGI: 1330275 HomoloGene: 3508 IUPHAR: 339 ChEMBL: 5071 GeneCards: PTGDR2 Gene
Gene ontology Molecular function • prostaglandin J receptor activity • G-protein coupled receptor activity • prostaglandin D receptor activity • prostaglandin F receptor activity • neuropeptide binding Cellular component • intracellular • plasma membrane • integral component of plasma membrane • neuron projection Biological process • chemotaxis • immune response • G-protein coupled receptor signaling pathway • G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger • adenylate cyclase-inhibiting G-protein coupled receptor signaling pathway • neuropeptide signaling pathway • synaptic transmission • calcium-mediated signaling • positive regulation of G-protein coupled receptor protein signaling pathway • negative regulation of male germ cell proliferation Sources: Amigo / QuickGO
RNA expression pattern
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	11251	14764
Ensembl	ENSG00000183134	ENSMUSG00000034117
UniProt	Q9Y5Y4	Q9Z2J6
RefSeq (mRNA)	NM_004778	NM_009962
RefSeq (protein)	NP_004769	NP_034092
Location (UCSC)	Chr 11: 60.85 – 60.86 Mb	Chr 19: 10.94 – 10.94 Mb
PubMed search

Prostaglandin D₂ receptor 2 (DP₂) is a human protein encoded by the PTGDR2 gene.^[1] DP₂ has also been designated as CD294 (cluster of differentiation 294).

Function

G protein-coupled receptors (GPCRs), such as DP₂, are integral membrane proteins containing 7 putative transmembrane domains (TMs). These proteins mediate signals to the interior of the cell via activation of heterotrimeric G proteins that in turn activate various effector proteins, ultimately resulting in a physiologic response.[supplied by OMIM]^[1]

DP₂ has recently been found when activated by elevated level of prostaglandin D₂ (PGD₂), it could inhibit hair growth. This suggests the DP₂ pathway as a potential target for bald treatment.^[2] A particularly promising compound for blocking the DP₂ pathway is a compound known as TM30089, which exhibits a "functional insurmountability" of PGD2 expression.^[3]

Ligands

Agonists

• Indometacin - non-selective
• Prostaglandin D₂ - non-selective

Antagonists

• ADC-3680 - selective
• AZD-1981 - selective
• Bay U3405 - non-selective
• Fevipiprant - selective
• MK-1029 - selective
• MK-7246 - selective
• OC-459 - selective
• OC000459 - selective
• QAV-680 - selective
• Ramatroban - non-selective
• Setipiprant - selective
• TM30089 - selective
• Vidupiprant - non-selective

See also

• Prostaglandin DP₁ receptor
• Eicosanoid receptor

References

1. "Entrez Gene: GPR44 G protein-coupled receptor 44".
2. Prostaglandin D2 Inhibits Hair Growth and Is Elevated in Bald Scalp of Men with Androgenetic Alopecia
3. http://molpharm.aspetjournals.org/content/69/4/1441

Further reading

• Nagata K (2004). "CRTH2". Journal of Biological Regulators and Homeostatic Agents 17 (4): 334–7. PMID 15065763.
• Chiba T, Kanda A, Ueki S, Ito W, Yamaguchi K, Kamada Y, Takeda M, Tanigai T, Oyamada H, Kayaba H, Chihara J (2007). "Possible novel receptor for PGD2 on human bronchial epithelial cells". International Archives of Allergy and Immunology. 143 Suppl 1: 23–7. doi:10.1159/000101400. PMID 17541272.
• Nagata K, Tanaka K, Ogawa K, Kemmotsu K, Imai T, Yoshie O, Abe H, Tada K, Nakamura M, Sugamura K, Takano S (Feb 1999). "Selective expression of a novel surface molecule by human Th2 cells in vivo". Journal of Immunology 162 (3): 1278–86. PMID 9973380.
• Marchese A, Sawzdargo M, Nguyen T, Cheng R, Heng HH, Nowak T, Im DS, Lynch KR, George SR, O'dowd BF (Feb 1999). "Discovery of three novel orphan G-protein-coupled receptors". Genomics 56 (1): 12–21. doi:10.1006/geno.1998.5655. PMID 10036181.
• Hirai H, Tanaka K, Yoshie O, Ogawa K, Kenmotsu K, Takamori Y, Ichimasa M, Sugamura K, Nakamura M, Takano S, Nagata K (Jan 2001). "Prostaglandin D2 selectively induces chemotaxis in T helper type 2 cells, eosinophils, and basophils via seven-transmembrane receptor CRTH2". The Journal of Experimental Medicine 193 (2): 255–61. doi:10.1084/jem.193.2.255. PMC 2193345. PMID 11208866.
• Hirai H, Tanaka K, Takano S, Ichimasa M, Nakamura M, Nagata K (Feb 2002). "Cutting edge: agonistic effect of indomethacin on a prostaglandin D2 receptor, CRTH2". Journal of Immunology 168 (3): 981–5. doi:10.4049/jimmunol.168.3.981. PMID 11801628.
• Iwasaki M, Nagata K, Takano S, Takahashi K, Ishii N, Ikezawa Z (Sep 2002). "Association of a new-type prostaglandin D2 receptor CRTH2 with circulating T helper 2 cells in patients with atopic dermatitis". The Journal of Investigative Dermatology 119 (3): 609–16. doi:10.1046/j.1523-1747.2002.01862.x. PMID 12230502.
• Böhm E, Sturm GJ, Weiglhofer I, Sandig H, Shichijo M, McNamee A, Pease JE, Kollroser M, Peskar BA, Heinemann A (Feb 2004). "11-Dehydro-thromboxane B2, a stable thromboxane metabolite, is a full agonist of chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2) in human eosinophils and basophils". The Journal of Biological Chemistry 279 (9): 7663–70. doi:10.1074/jbc.M310270200. PMID 14668348.
• Huang JL, Gao PS, Mathias RA, Yao TC, Chen LC, Kuo ML, Hsu SC, Plunkett B, Togias A, Barnes KC, Stellato C, Beaty TH, Huang SK (Nov 2004). "Sequence variants of the gene encoding chemoattractant receptor expressed on Th2 cells (CRTH2) are associated with asthma and differentially influence mRNA stability". Human Molecular Genetics 13 (21): 2691–7. doi:10.1093/hmg/ddh279. PMID 15345705.
• Venet F, Lepape A, Debard AL, Bienvenu J, Bohé J, Monneret G (Dec 2004). "The Th2 response as monitored by CRTH2 or CCR3 expression is severely decreased during septic shock". Clinical Immunology 113 (3): 278–84. doi:10.1016/j.clim.2004.07.005. PMID 15507393.
• Gazi L, Gyles S, Rose J, Lees S, Allan C, Xue L, Jassal R, Speight G, Gamble V, Pettipher R (Jan 2005). "Delta12-prostaglandin D2 is a potent and selective CRTH2 receptor agonist and causes activation of human eosinophils and Th2 lymphocytes". Prostaglandins & Other Lipid Mediators 75 (1-4): 153–67. doi:10.1016/j.prostaglandins.2004.11.003. PMID 15789622.
• Hata AN, Lybrand TP, Breyer RM (Sep 2005). "Identification of determinants of ligand binding affinity and selectivity in the prostaglandin D2 receptor CRTH2". The Journal of Biological Chemistry 280 (37): 32442–51. doi:10.1074/jbc.M502563200. PMID 16030019.
• Sandig H, Andrew D, Barnes AA, Sabroe I, Pease J (Jan 2006). "9alpha,11beta-PGF2 and its stereoisomer PGF2alpha are novel agonists of the chemoattractant receptor, CRTH2". FEBS Letters 580 (2): 373–9. doi:10.1016/j.febslet.2005.11.052. PMID 16378605.
• Schratl P, Royer JF, Kostenis E, Ulven T, Sturm EM, Waldhoer M, Hoefler G, Schuligoi R, Lippe IT, Peskar BA, Heinemann A (Oct 2007). "The role of the prostaglandin D2 receptor, DP, in eosinophil trafficking". Journal of Immunology 179 (7): 4792–9. doi:10.4049/jimmunol.179.7.4792. PMID 17878378.

External links

• "Prostanoid Receptors: DP₂". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
• GPR44 protein, human at the US National Library of Medicine Medical Subject Headings (MeSH)

This article incorporates text from the United States National Library of Medicine, which is in the public domain.