Platelet-activating factor receptor
More information on this family may be found on the IUPHAR-DB family and introduction pages.
Platelet-activating factor (PAF, 1-O-alkyl-2-acetyl-sn-glycero-3-phosphocholine) is a biologically active phospholipid mediator. PAF acts by binding to a unique G protein-coupled seven transmembrane receptor (PAF-R) and activates multiple intracellular signalling pathways by coupling to the Gq/11 and Gi/o families of G proteins. PAF-R is activated by PAF and its metabolically stable analogue mc-PAF. Other suggested endogenous ligands are oxidized phosphatidylcholine [4] and lysophosphatidylcholine [7]. It may also be activated by bacterial lipopolysaccharide [6].
Unless otherwise stated all data refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Receptors 
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Honda, Z; Ishii, S; Shimizu, T. (2002) Platelet-activating factor receptor. J. Biochem., 131 (6): 773-9. [PMID:12038971]
Ishii, S; Nagase, T; Shimizu, T. (2002) Platelet-activating factor receptor. Prostaglandins Other Lipid Mediat., 68-69: 599-609. [PMID:12432946]
Ishii, S; Shimizu, T. (2000) Platelet-activating factor (PAF) receptor and genetically engineered PAF receptor mutant mice. Prog. Lipid Res., 39 (1): 41-82. [PMID:10729607]
Izumi, T; Shimizu, T. (1995) Platelet-activating factor receptor: gene expression and signal transduction. Biochim. Biophys. Acta, 1259 (3): 317-33. [PMID:8541341]
Kasperska-Zajac, A; Brzoza, Z; Rogala, B. (2008) Platelet-activating factor (PAF): a review of its role in asthma and clinical efficacy of PAF antagonists in the disease therapy. Recent Pat Inflamm Allergy Drug Discov, 2 (1): 72-6. [PMID:19075994]
Maclennan, KM; Smith, PF; Darlington, CL. (1996) Platelet-activating factor in the CNS. Prog. Neurobiol., 50 (5-6): 585-96. [PMID:9015828]
Montrucchio, G; Alloatti, G; Camussi, G. (2000) Role of platelet-activating factor in cardiovascular pathophysiology. Physiol. Rev., 80 (4): 1669-99. [PMID:11015622]
Prescott, SM; Zimmerman, GA; Stafforini, DM; McIntyre, TM. (2000) Platelet-activating factor and related lipid mediators. Annu. Rev. Biochem., 69: 419-45. [PMID:10966465]
Shimizu, T. (2009) Lipid mediators in health and disease: enzymes and receptors as therapeutic targets for the regulation of immunity and inflammation. Annu. Rev. Pharmacol. Toxicol., 49: 123-50. [PMID:18834304]
Stafforini, DM; McIntyre, TM; Zimmerman, GA; Prescott, SM. (2003) Platelet-activating factor, a pleiotrophic mediator of physiological and pathological processes. Crit Rev Clin Lab Sci, 40 (6): 643-72. [PMID:14708958]
Summers, J. B. and Albert, D. H. (1995) Platelet activating factor antagonists. Adv Pharmacol, 32: 67-168. [PMID:7748804]
1. Fukunaga, K., Ishii, S., Asano, K., Yokomizo, T., Shiomi, T., Shimizu, T. and Yamaguchi, K. (2001) Single nucleotide polymorphism of human platelet-activating factor receptor impairs G-protein activation. J Biol Chem, 276: 43025-43030. [PMID:11560941]
2. Goldring, W. P., Alexander, S. P., Kendall, D. A. and Pattenden, G. (2005) Novel phomactin analogues as PAF receptor ligands. Bioorg Med Chem Lett, 15: 3263-3266. [PMID:15922596]
3. Herbert, J. M., Laplace, M. C., Cailleau, C. and Maffrand, J. P. (1993) Effect of SR 27417 on the binding of [3H]PAF to rabbit and human platelets and human polymorphonuclear leukocytes. J Lipid Mediat, 7: 57-78. [PMID:8395255]
4. Marathe, G. K., Davies, S. S., Harrison, K. A., Silva, A. R., Murphy, R. C., Castro-Faria-Neto, H., Prescott, S. M., Zimmerman, G. A. and McIntyre, T. M. (1999) Inflammatory platelet-activating factor-like phospholipids in oxidized low density lipoproteins are fragmented alkyl phosphatidylcholines. J Biol Chem, 274: 28395-28404. [PMID:10497200]
5. Nakamura, M., Honda, Z., Izumi, T., Sakanaka, C., Mutoh, H., Minami, M., Bito, H., Seyama, Y., Matsumoto, T., Noma, M. et al.. (1991) Molecular cloning and expression of platelet-activating factor receptor from human leukocytes. J Biol Chem, 266: 20400-20405. [PMID:1657923]
6. Nakamura, M; Honda, Z; Waga, I; Matsumoto, T; Noma, M; Shimizu, T. (1992) Endotoxin transduces Ca2+ signaling via platelet-activating factor receptor. FEBS Lett., 314 (2): 125-9. [PMID:1333988]
7. Ogita, T; Tanaka, Y; Nakaoka, T; Matsuoka, R; Kira, Y; Nakamura, M; Shimizu, T; Fujita, T. (1997) Lysophosphatidylcholine transduces Ca2+ signaling via the platelet-activating factor receptor in macrophages. Am. J. Physiol., 272 (1 Pt 2): H17-24. [PMID:9038918]
8. Parent, J. L., Gouill, C. L., Escher, E., Rola-Pleszczynski, M. and Stakova, J. (1996) Identification of transmembrane domain residues determinant in the structure-function relationship of the human platelet-activating factor receptor by site-directed mutagenesis. J Biol Chem, 271: 23298-23303. [PMID:8798529]
9. Svetlov, S. and Nigam, S. (1993) Evidence for the presence of specific high affinity cytosolic binding sites for platelet-activating factor in human neutrophils. Biochem Biophys Res Commun, 190: 162-166. [PMID:8380690]
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Note that a previously recommended radioligand ([3H]apafant; Kd 44.6 nM) is currently unavailable.