Prostaglandin DP2 receptor
View/Edit Human | View/Edit Mouse |
Prostaglandin D2 receptor 2 (DP2) is a human protein encoded by the PTGDR2 gene.[4] 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][4]
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.[5] A particularly promising compound for blocking the DP2 pathway is a compound known as TM30089, which exhibits a "functional insurmountability" of PGD2 expression.[6]
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
References
- ↑ "Drugs that physically interact with Prostaglandin D2 receptor 2 view/edit references on wikidata".
- ↑ "Human PubMed Reference:".
- ↑ "Mouse PubMed Reference:".
- 1 2 "Entrez Gene: GPR44 G protein-coupled receptor 44".
- ↑ Garza LA, Liu Y, Yang Z, Alagesan B, Lawson JA, Norberg SM, Loy DE, Zhao T, Blatt HB, Stanton DC, Carrasco L, Ahluwalia G, Fischer SM, FitzGerald GA, Cotsarelis G (March 2012). "Prostaglandin D2 inhibits hair growth and is elevated in bald scalp of men with androgenetic alopecia". Science Translational Medicine. 4 (126): 126ra34. doi:10.1126/scitranslmed.3003122. PMC 3319975. PMID 22440736.
- ↑ Mathiesen JM, Christopoulos A, Ulven T, Royer JF, Campillo M, Heinemann A, Pardo L, Kostenis E (April 2006). "On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2". Molecular Pharmacology. 69 (4): 1441–53. doi:10.1124/mol.105.017681. PMID 16418339.
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 (February 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 (February 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 (January 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 (February 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 (September 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 (February 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 (November 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 (December 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 (January 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 (September 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 (January 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 (October 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.