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Gene Review

PTAFR  -  platelet-activating factor receptor

Homo sapiens

Synonyms: PAF-R, PAFR, PAFr, Platelet-activating factor receptor
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Disease relevance of PTAFR


Psychiatry related information on PTAFR

  • Taken together, these results demonstrate that PMS777 possesses dual activities for PAF receptor antagonism and AChE inhibition, suggesting that this compound may be a promising lead compound for further investigation related to the treatment for Alzheimer's disease [6].

High impact information on PTAFR


Chemical compound and disease context of PTAFR


Biological context of PTAFR


Anatomical context of PTAFR


Associations of PTAFR with chemical compounds

  • To investigate the specific role of dimerization in the internalization process of GPCRs, we generated a fusion protein of hPAFR and bacterial DNA gyrase B (GyrB), dimerized through the addition of coumermycin [25].
  • The presence of the PAF-R in these models resulted in an augmentation of apoptosis induced by chemotherapeutic agents etoposide and mitomycin C but not by tumor necrosis factor-related apoptosis-inducing ligand or by C(2) ceramide [20].
  • We show that, POVPC binds to cultured human macrophages via PAF-R and transduces the signals leading to the intracellular Ca(2+) fluxes and modifies the transcription levels of numerous pro-inflammatory and pro-atherogenic genes [24].
  • Sodium decreased specific (3)H-PAF and antagonist (3)H-WEB2086 binding to the PAF receptor, but the aspartate 63 residue was not involved in this regulation, contrary to cognate aspartate residues in other GPCRs [26].
  • Localization, quantification, and activation of platelet-activating factor receptor in human endometrium during the menstrual cycle: PAF stimulates NO, VEGF, and FAKpp125 [27].

Physical interactions of PTAFR


Enzymatic interactions of PTAFR


Regulatory relationships of PTAFR


Other interactions of PTAFR


Analytical, diagnostic and therapeutic context of PTAFR


  1. Platelet-activating factor receptor gene polymorphism in Japanese patients with multiple sclerosis. Osoegawa, M., Miyagishi, R., Ochi, H., Nakamura, I., Niino, M., Kikuchi, S., Murai, H., Fukazawa, T., Minohara, M., Tashiro, K., Kira, J. J. Neuroimmunol. (2005) [Pubmed]
  2. Platelet-activating factor and human meningiomas. Denizot, Y., De Armas, R., Caire, F., Pommepuy, I., Truffinet, V., Labrousse, F. Neuropathol. Appl. Neurobiol. (2006) [Pubmed]
  3. Platelet-activating factor receptor activation. An initiator step in HIV-1 neuropathogenesis. Perry, S.W., Hamilton, J.A., Tjoelker, L.W., Dbaibo, G., Dzenko, K.A., Epstein, L.G., Hannun, Y., Whittaker, J.S., Dewhurst, S., Gelbard, H.A. J. Biol. Chem. (1998) [Pubmed]
  4. Ultraviolet B radiation generates platelet-activating factor-like phospholipids underlying cutaneous damage. Marathe, G.K., Johnson, C., Billings, S.D., Southall, M.D., Pei, Y., Spandau, D., Murphy, R.C., Zimmerman, G.A., McIntyre, T.M., Travers, J.B. J. Biol. Chem. (2005) [Pubmed]
  5. Molecular cloning and expression of platelet-activating factor receptor from human leukocytes. Nakamura, M., Honda, Z., Izumi, T., Sakanaka, C., Mutoh, H., Minami, M., Bito, H., Seyama, Y., Matsumoto, T., Noma, M. J. Biol. Chem. (1991) [Pubmed]
  6. Pharmacological profile of PMS777, a new AChE inhibitor with PAF antagonistic activity. Li, J., Huang, H., Miezan Ezoulin, J.M., Gao, X.L., Massicot, F., Dong, C.Z., Heymans, F., Chen, H.Z. Int. J. Neuropsychopharmacol. (2007) [Pubmed]
  7. Platelet-activating factor receptor and ADAM10 mediate responses to Staphylococcus aureus in epithelial cells. Lemjabbar, H., Basbaum, C. Nat. Med. (2002) [Pubmed]
  8. Streptococcus pneumoniae anchor to activated human cells by the receptor for platelet-activating factor. Cundell, D.R., Gerard, N.P., Gerard, C., Idanpaan-Heikkila, I., Tuomanen, E.I. Nature (1995) [Pubmed]
  9. Novel pharmacological approaches to manage interstitial lung fibrosis in the twenty-first century. Giri, S.N. Annu. Rev. Pharmacol. Toxicol. (2003) [Pubmed]
  10. Platelet-activating factor exerts mitogenic activity and stimulates expression of interleukin 6 and interleukin 8 in human lung fibroblasts via binding to its functional receptor. Roth, M., Nauck, M., Yousefi, S., Tamm, M., Blaser, K., Perruchoud, A.P., Simon, H.U. J. Exp. Med. (1996) [Pubmed]
  11. Glycoprotein 170 induces platelet-activating factor receptor membrane expression and confers tumor cell hypersensitivity to NK-dependent cell lysis. Geromin, D., Bourge, J.F., Soulié, A., Pawliuk, R., Fleet, C., Michel, E., Denizot, Y., Berthou, C., Leboulch, P., Sigaux, F., Sasportes, M. J. Immunol. (2004) [Pubmed]
  12. Growth inhibition and differentiation of human breast cancer cells by the PAFR antagonist WEB-2086. Cellai, C., Laurenzana, A., Vannucchi, A.M., Caporale, R., Paglierani, M., Di Lollo, S., Pancrazzi, A., Paoletti, F. Br. J. Cancer (2006) [Pubmed]
  13. Positive and negative regulations of human platelet-activating factor receptor transcript 2 (tissue-type) by estrogen and TGF-beta 1. Mutoh, H., Kume, K., Sato, S., Kato, S., Shimizu, T. Biochem. Biophys. Res. Commun. (1994) [Pubmed]
  14. Amelioration of bleomycin-induced lung fibrosis by treatment with the platelet activating factor receptor antagonist WEB 2086 in hamsters. Giri, S.N., Sharma, A.K., Hyde, D.M., Wild, J.S. Exp. Lung Res. (1995) [Pubmed]
  15. Staphylococcal lipoteichoic acid inhibits delayed-type hypersensitivity reactions via the platelet-activating factor receptor. Zhang, Q., Mousdicas, N., Yi, Q., Al-Hassani, M., Billings, S.D., Perkins, S.M., Howard, K.M., Ishii, S., Shimizu, T., Travers, J.B. J. Clin. Invest. (2005) [Pubmed]
  16. Platelet-activating factor-acetylhydrolase and PAF-receptor gene haplotypes in relation to future cardiovascular event in patients with coronary artery disease. Ninio, E., Tregouet, D., Carrier, J.L., Stengel, D., Bickel, C., Perret, C., Rupprecht, H.J., Cambien, F., Blankenberg, S., Tiret, L. Hum. Mol. Genet. (2004) [Pubmed]
  17. The human platelet-activating factor receptor gene (PTAFR) contains no introns and maps to chromosome 1. Seyfried, C.E., Schweickart, V.L., Godiska, R., Gray, P.W. Genomics (1992) [Pubmed]
  18. Regional mapping of the human platelet-activating factor receptor gene (PTAFR) to 1p35-->p34.3 by fluorescence in situ hybridization. Chase, P.B., Yang, J.M., Thompson, F.H., Halonen, M., Regan, J.W. Cytogenet. Cell Genet. (1996) [Pubmed]
  19. Janus kinase 2 activation by the platelet-activating factor receptor (PAFR): roles of Tyk2 and PAFR C terminus. Lukashova, V., Chen, Z., Duhé, R.J., Rola-Pleszczynski, M., Stanková, J. J. Immunol. (2003) [Pubmed]
  20. The epidermal platelet-activating factor receptor augments chemotherapy-induced apoptosis in human carcinoma cell lines. Li, T., Southall, M.D., Yi, Q., Pei, Y., Lewis, D., Al-Hassani, M., Spandau, D., Travers, J.B. J. Biol. Chem. (2003) [Pubmed]
  21. Activation of platelet-activating factor receptor-coupled G alpha q leads to stimulation of Src and focal adhesion kinase via two separate pathways in human umbilical vein endothelial cells. Deo, D.D., Bazan, N.G., Hunt, J.D. J. Biol. Chem. (2004) [Pubmed]
  22. Regulation by IL-5 of expression of functional platelet-activating factor receptors on human eosinophils. Kishimoto, S., Shimadzu, W., Izumi, T., Shimizu, T., Fukuda, T., Makino, S., Sugiura, T., Waku, K. J. Immunol. (1996) [Pubmed]
  23. Trafficking, ubiquitination, and down-regulation of the human platelet-activating factor receptor. Dupré, D.J., Chen, Z., Le Gouill, C., Thériault, C., Parent, J.L., Rola-Pleszczynski, M., Stankova, J. J. Biol. Chem. (2003) [Pubmed]
  24. Oxidized phospholipid: POVPC binds to platelet-activating-factor receptor on human macrophages Implications in atherosclerosis. Pégorier, S., Stengel, D., Durand, H., Croset, M., Ninio, E. Atherosclerosis (2006) [Pubmed]
  25. Agonist-independent desensitization and internalization of the human platelet-activating factor receptor by coumermycin-gyrase B-induced dimerization. Perron, A., Chen, Z.G., Gingras, D., Dupre, D.J., Stankova, J., Rola-Pleszczynski, M. J. Biol. Chem. (2003) [Pubmed]
  26. Mutation of an aspartate at position 63 in the human platelet-activating factor receptor augments binding affinity but abolishes G-protein-coupling and inositol phosphate production. Parent, J.L., Le Gouill, C., Rola-Pleszczynski, M., Stanková, J. Biochem. Biophys. Res. Commun. (1996) [Pubmed]
  27. Localization, quantification, and activation of platelet-activating factor receptor in human endometrium during the menstrual cycle: PAF stimulates NO, VEGF, and FAKpp125. Ahmed, A., Dearn, S., Shams, M., Li, X.F., Sangha, R.K., Rola-Pleszczynski, M., Jiang, J. FASEB J. (1998) [Pubmed]
  28. GTP regulation of platelet-activating factor binding to human neutrophil membranes. Ng, D.S., Wong, K. Biochem. Biophys. Res. Commun. (1986) [Pubmed]
  29. Role of cytoplasmic tail phosphorylation sites of platelet-activating factor receptor in agonist-induced desensitization. Takano, T., Honda, Z., Sakanaka, C., Izumi, T., Kameyama, K., Haga, K., Haga, T., Kurokawa, K., Shimizu, T. J. Biol. Chem. (1994) [Pubmed]
  30. The platelet-activating factor receptor activates the extracellular signal-regulated kinase mitogen-activated protein kinase and induces proliferation of epidermal cells through an epidermal growth factor-receptor-dependent pathway. Marques, S.A., Dy, L.C., Southall, M.D., Yi, Q., Smietana, E., Kapur, R., Marques, M., Travers, J.B., Spandau, D.F. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  31. RGS4 inhibits platelet-activating factor receptor phosphorylation and cellular responses. Richardson, R.M., Marjoram, R.J., Barr, A.J., Snyderman, R. Biochemistry (2001) [Pubmed]
  32. Platelet-activating factor-induced clathrin-mediated endocytosis requires beta-arrestin-1 recruitment and activation of the p38 MAPK signalosome at the plasma membrane for actin bundle formation. McLaughlin, N.J., Banerjee, A., Kelher, M.R., Gamboni-Robertson, F., Hamiel, C., Sheppard, F.R., Moore, E.E., Silliman, C.C. J. Immunol. (2006) [Pubmed]
  33. Evidence for involvement of the epidermal platelet-activating factor receptor in ultraviolet-B-radiation-induced interleukin-8 production. Countryman, N.B., Pei, Y., Yi, Q., Spandau, D.F., Travers, J.B. J. Invest. Dermatol. (2000) [Pubmed]
  34. IFN-gamma up-regulates platelet-activating factor receptor gene expression in human monocytes. Ouellet, S., Müller, E., Rola-Pleszczynski, M. J. Immunol. (1994) [Pubmed]
  35. G-protein-independent activation of Tyk2 by the platelet-activating factor receptor. Lukashova, V., Asselin, C., Krolewski, J.J., Rola-Pleszczynski, M., Stanková, J. J. Biol. Chem. (2001) [Pubmed]
  36. Single nucleotide polymorphism of human platelet-activating factor receptor impairs G-protein activation. Fukunaga, K., Ishii, S., Asano, K., Yokomizo, T., Shiomi, T., Shimizu, T., Yamaguchi, K. J. Biol. Chem. (2001) [Pubmed]
  37. Cloning, expression and tissue distribution of rat platelet-activating-factor-receptor cDNA. Bito, H., Honda, Z., Nakamura, M., Shimizu, T. Eur. J. Biochem. (1994) [Pubmed]
  38. Molecular cloning and characterization of the platelet-activating factor receptor gene expressed in the human heart. Sugimoto, T., Tsuchimochi, H., McGregor, C.G., Mutoh, H., Shimizu, T., Kurachi, Y. Biochem. Biophys. Res. Commun. (1992) [Pubmed]
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