Platelet-activating factor receptor explained

The platelet-activating factor receptor (PAF-R) is a G-protein coupled receptor which binds platelet-activating factor.^{[1] [2]} It is encoded in the human by the PTAFR gene.

The PAF receptor shows structural characteristics of the rhodopsin (MIM 180380) gene family and binds platelet-activating factor (PAF). PAF is a phospholipid (1-0-alkyl-2-acetyl-sn-glycero-3-phosphorylcholine) that has been implicated as a mediator in diverse pathologic processes, such as allergy, asthma, septic shock, arterial thrombosis, and inflammatory processes.[supplied by OMIM]^[3] Its pathogenetic role in chronic kidney failure has also been reported recently.^[4]

Ligands

Agonists

• Platelet activating factor

Antagonists

• Apafant (WEB-2086)
• Israpafant (Y-24180)
• Lexipafant
• Rupatadine

References

1. Seyfried CE, Schweickart VL, Godiska R, Gray PW . The human platelet-activating factor receptor gene (PTAFR) contains no introns and maps to chromosome 1 . Genomics . 13 . 3 . 832–4 . 1992 . 1322356 . 10.1016/0888-7543(92)90162-L .
2. Ishii S, Nagase T, Shimizu T . Platelet-activating factor receptor . Prostaglandins Other Lipid Mediat. . 68-69 . 599–609 . 2002 . 12432946 . 10.1016/S0090-6980(02)00058-8 .
3. Web site: Entrez Gene: PTAFR platelet-activating factor receptor.
4. Correa-Costa M . Activation of platelet-activating factor receptor exacerbates renal inflammation and promotes fibrosis. . Lab. Invest. . 94 . 4 . Apr 2014 . 24492283 . 455–466 . 10.1038/labinvest.2013.155. free .

Further reading

• Shukla SD . Platelet-activating factor receptor and signal transduction mechanisms. . FASEB J. . 6 . 6 . 2296–301 . 1992 . 1312046 . 10.1096/fasebj.6.6.1312046. free . 6000303 .
• Sugimoto T, Tsuchimochi H, McGregor CG, etal . Molecular cloning and characterization of the platelet-activating factor receptor gene expressed in the human heart. . Biochem. Biophys. Res. Commun. . 189 . 2 . 617–24 . 1993 . 1281995 . 10.1016/0006-291X(92)92245-S .
• Seyfried CE, Schweickart VL, Godiska R, Gray PW . The human platelet-activating factor receptor gene (PTAFR) contains no introns and maps to chromosome 1. . Genomics . 13 . 3 . 832–4 . 1992 . 1322356 . 10.1016/0888-7543(92)90162-L .
• Kunz D, Gerard NP, Gerard C . The human leukocyte platelet-activating factor receptor. cDNA cloning, cell surface expression, and construction of a novel epitope-bearing analog. . J. Biol. Chem. . 267 . 13 . 9101–6 . 1992 . 10.1016/S0021-9258(19)50394-5 . 1374385 . free .
• Ye RD, Prossnitz ER, Zou AH, Cochrane CG . Characterization of a human cDNA that encodes a functional receptor for platelet activating factor. . Biochem. Biophys. Res. Commun. . 180 . 1 . 105–11 . 1991 . 1656963 . 10.1016/S0006-291X(05)81261-6 .
• Nakamura M, Honda Z, Izumi T, etal . Molecular cloning and expression of platelet-activating factor receptor from human leukocytes. . J. Biol. Chem. . 266 . 30 . 20400–5 . 1991 . 10.1016/S0021-9258(18)54936-X . 1657923 . free .
• Book: Haslam RJ, Williams KA, Davidson MM . Mechanisms of Stimulus—Response Coupling in Platelets . Receptor-Effector Coupling in Platelets: Roles of Guanine Nucleotides . 192 . 265–80 . 3010668 . 10.1007/978-1-4615-9442-0_19 . Advances in Experimental Medicine and Biology . 1985 . 978-1-4615-9444-4 .
• Valone FH . Isolation of a platelet membrane protein which binds the platelet-activating factor 1-0-hexadecyl-2-acetyl-SN-glycero-3-phosphorylcholine. . Immunology . 52 . 1 . 169–74 . 1984 . 6325330 . 1454573 .
• Cundell DR, Gerard NP, Gerard C, etal . Streptococcus pneumoniae anchor to activated human cells by the receptor for platelet-activating factor. . Nature . 377 . 6548 . 435–8 . 1995 . 7566121 . 10.1038/377435a0 . 1995Natur.377..435C . 4318257 .
• Izumi T, Kishimoto S, Takano T, etal . Expression of human platelet-activating factor receptor gene in EoL-1 cells following butyrate-induced differentiation. . 305 . Biochem. J. . (Pt 3) . 3. 829–35 . 1995 . 7848283 . 10.1042/bj3050829. 1136334 .
• Bito H, Honda Z, Nakamura M, Shimizu T . Cloning, expression and tissue distribution of rat platelet-activating-factor-receptor cDNA. . Eur. J. Biochem. . 221 . 1 . 211–8 . 1994 . 8168510 . 10.1111/j.1432-1033.1994.tb18731.x . free .
• Chase PB, Halonen M, Regan JW . Cloning of a human platelet-activating factor receptor gene: evidence for an intron in the 5'-untranslated region. . Am. J. Respir. Cell Mol. Biol. . 8 . 3 . 240–4 . 1993 . 8383507 . 10.1165/ajrcmb/8.3.240.
• Mutoh H, Bito H, Minami M, etal . Two different promoters direct expression of two distinct forms of mRNAs of human platelet-activating factor receptor. . FEBS Lett. . 322 . 2 . 129–34 . 1993 . 8387031 . 10.1016/0014-5793(93)81552-B . 44640249 . free .
• Nakamura M, Honda Z, Matsumoto T, etal . Isolation and properties of platelet-activating factor receptor cDNAs. . Journal of Lipid Mediators . 6 . 1–3 . 163–8 . 1993 . 8395240 .
• Kishimoto S, Shimadzu W, Izumi T, etal . Regulation by IL-5 of expression of functional platelet-activating factor receptors on human eosinophils. . J. Immunol. . 157 . 9 . 4126–32 . 1996 . 10.4049/jimmunol.157.9.4126 . 8892648 . free .
• Chase PB, Yang JM, Thompson FH, etal . Regional mapping of the human platelet-activating factor receptor gene (PTAFR) to 1p35→p34.3 by fluorescence in situ hybridization. . Cytogenet. Cell Genet. . 72 . 2–3 . 205–7 . 1997 . 8978777 . 10.1159/000134190 .
• Le Gouill C, Parent JL, Rola-Pleszczynski M, Stanková J . Role of the Cys90, Cys95 and Cys173 residues in the structure and function of the human platelet-activating factor receptor. . FEBS Lett. . 402 . 2–3 . 203–8 . 1997 . 9037196 . 10.1016/S0014-5793(96)01531-1 . 21074692 . free .
• Ahmed A, Dearn S, Shams M, etal . Localization, quantification, and activation of platelet-activating factor receptor in human endometrium during the menstrual cycle: PAF stimulates NO, VEGF, and FAKpp125. . FASEB J. . 12 . 10 . 831–43 . 1998 . 9657523 . 10.1096/fasebj.12.10.831. free . 17474972 .
• Cargill M, Altshuler D, Ireland J, etal . Characterization of single-nucleotide polymorphisms in coding regions of human genes. . Nat. Genet. . 22 . 3 . 231–8 . 1999 . 10391209 . 10.1038/10290 . 195213008 .

External links

• Web site: Platelet-Activating Factor Receptor . IUPHAR Database of Receptors and Ion Channels . International Union of Basic and Clinical Pharmacology . 2007-10-25 . 2016-03-03 . https://web.archive.org/web/20160303205650/http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1348 . dead .