Prostaglandin DP1 receptor
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Prostaglandin D2 receptor 1 (DP1) is a G protein-coupled receptor, encoded by the PTGDR1 gene, for prostaglandin D2 (PGD2).[4]
Mechanism
DP1 is a G protein-coupled receptor (GPCR). Its activity is mainly mediated by G-S proteins that stimulate adenylate cyclase resulting in an elevation of intracellular cAMP and Ca2+.
Function
Knockout studies in mice suggest that the ligand of this receptor, prostaglandin D2, functions as a mast cell-derived mediator to trigger asthmatic responses.[4] It also causes vasodilation.
Ligands
- Agonists
- Prostaglandin D2 - non-selective
- Treprostinil - non-selective
- Antagonists [5]
- Asapiprant (S-555739) - selective
- Laropiprant - selective
- Vidupiprant - dual DP1 and DP2 antagonist
See also
References
- ↑ "Drugs that physically interact with Prostaglandin D2 receptor view/edit references on wikidata".
- ↑ "Human PubMed Reference:".
- ↑ "Mouse PubMed Reference:".
- 1 2 "Entrez Gene: PTGDR prostaglandin D2 receptor (DP)".
- ↑ Norman P (Jan 2014). "Update on the status of DP2 receptor antagonists; from proof of concept through clinical failures to promising new drugs". Expert Opin Investig Drugs. 23 (1): 55–66. doi:10.1517/13543784.2013.839658. PMID 24073896.
External links
- "Prostanoid Receptors: DP1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Further reading
- Boyce JA (2004). "The role of mast cells in asthma". Prostaglandins Leukot. Essent. Fatty Acids. 69 (2–3): 195–205. doi:10.1016/S0952-3278(03)00081-4. PMID 12895603.
- Chiba T, Kanda A, Ueki S, et al. (2007). "Possible novel receptor for PGD2 on human bronchial epithelial cells". Int. Arch. Allergy Immunol. 143 Suppl 1: 23–7. doi:10.1159/000101400. PMID 17541272.
- Senior J, Sangha R, Baxter GS, et al. (1992). "In vitro characterization of prostanoid FP-, DP-, IP- and TP-receptors on the non-pregnant human myometrium". Br. J. Pharmacol. 107 (1): 215–21. doi:10.1111/j.1476-5381.1992.tb14489.x. PMC 1907618
. PMID 1422574. - Boie Y, Sawyer N, Slipetz DM, et al. (1995). "Molecular cloning and characterization of the human prostanoid DP receptor". J. Biol. Chem. 270 (32): 18910–6. doi:10.1074/jbc.270.32.18910. PMID 7642548.
- Ishikawa TO, Tamai Y, Rochelle JM, et al. (1997). "Mapping of the genes encoding mouse prostaglandin D, E, and F and prostacyclin receptors". Genomics. 32 (2): 285–8. doi:10.1006/geno.1996.0118. PMID 8833158.
- Kobayashi T, Ushikubi F, Narumiya S (2000). "Amino acid residues conferring ligand binding properties of prostaglandin I and prostaglandin D receptors. Identification by site-directed mutagenesis". J. Biol. Chem. 275 (32): 24294–303. doi:10.1074/jbc.M002437200. PMID 10827082.
- Wright DH, Ford-Hutchinson AW, Chadee K, Metters KM (2001). "The human prostanoid DP receptor stimulates mucin secretion in LS174T cells". Br. J. Pharmacol. 131 (8): 1537–45. doi:10.1038/sj.bjp.0703688. PMC 1572485. PMID 11139429.
- Gervais FG, Cruz RP, Chateauneuf A, et al. (2002). "Selective modulation of chemokinesis, degranulation, and apoptosis in eosinophils through the PGD2 receptors CRTH2 and DP". J. Allergy Clin. Immunol. 108 (6): 982–8. doi:10.1067/mai.2001.119919. PMID 11742277.
- Noguchi E, Shibasaki M, Kamioka M, et al. (2002). "New polymorphisms of haematopoietic prostaglandin D synthase and human prostanoid DP receptor genes". Clin. Exp. Allergy. 32 (1): 93–6. doi:10.1046/j.0022-0477.2001.01261.x. PMID 12002745.
- Hakonarson H, Bjornsdottir US, Halapi E, et al. (2002). "A Major Susceptibility Gene for Asthma Maps to Chromosome 14q24". Am. J. Hum. Genet. 71 (3): 483–91. doi:10.1086/342205. PMC 379187. PMID 12119603.
- Iwasaki M, Nagata K, Takano S, et al. (2002). "Association of a new-type prostaglandin D2 receptor CRTH2 with circulating T helper 2 cells in patients with atopic dermatitis". J. Invest. Dermatol. 119 (3): 609–16. doi:10.1046/j.1523-1747.2002.01862.x. PMID 12230502.
- Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932.
- Moreland RB, Nehra A, Kim NN, et al. (2003). "Expression of functional prostaglandin D (DP) receptors in human corpus cavernosum smooth muscle". Int. J. Impot. Res. 14 (6): 446–52. doi:10.1038/sj.ijir.3900900. PMID 12494276.
- Faveeuw C, Gosset P, Bureau F, et al. (2003). "Prostaglandin D2 inhibits the production of interleukin-12 in murine dendritic cells through multiple signaling pathways". Eur. J. Immunol. 33 (4): 889–98. doi:10.1002/eji.200323330. PMID 12672054.
- Angeli V, Staumont D, Charbonnier AS, et al. (2004). "Activation of the D prostanoid receptor 1 regulates immune and skin allergic responses". J. Immunol. 172 (6): 3822–9. doi:10.4049/jimmunol.172.6.3822. PMID 15004188.
- Gerhard DS, Wagner L, Feingold EA, et al. (2004). "The Status, Quality, and Expansion of the NIH Full-Length cDNA Project: The Mammalian Gene Collection (MGC)". Genome Res. 14 (10B): 2121–7. doi:10.1101/gr.2596504. PMC 528928. PMID 15489334.
- Oguma T, Palmer LJ, Birben E, et al. (2004). "Role of prostanoid DP receptor variants in susceptibility to asthma". N. Engl. J. Med. 351 (17): 1752–63. doi:10.1056/NEJMoa031785. PMID 15496624.
- Spik I, Brénuchon C, Angéli V, et al. (2005). "Activation of the prostaglandin D2 receptor DP2/CRTH2 increases allergic inflammation in mouse". J. Immunol. 174 (6): 3703–8. doi:10.4049/jimmunol.174.6.3703. PMID 15749909.
- Hirano Y, Shichijo M, Deguchi M, et al. (2007). "Synergistic effect of PGD2 via prostanoid DP receptor on TNF-alpha-induced production of MCP-1 and IL-8 in human monocytic THP-1 cells". Eur. J. Pharmacol. 560 (1): 81–8. doi:10.1016/j.ejphar.2007.01.003. PMID 17307163.
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