Antigen: human amino acids 1-22 (MSTPGVNSSASLSPDRLNSPVTI) · Host: rabbit · Application(s): WB; other applications not attempted · The biological effects of prostaglandin E₂ (PGE₂) are mediated through interaction with four distinct membrane-bound G-protein coupled EP receptors: EP₁, EP₂, EP₃, and EP₄.^1,2 Binding of PGE₂ to the EP₄ receptor causes an increase in intracellular cAMP and subsequent relaxation of smooth muscle.^3,4,1,2 In addition to sequence differences, EP₄ receptors are distinguished from EP₂ receptors by their insensitivity to the EP₂ receptor selective agonist butaprost.^5,6 The EP₄ receptor is expressed in multiple human tissues including kidney, small intestine, thymus, ileum, uterus, and lung, as well as in peripheral blood leukocytes.^3,4 The receptor is also expressed in cultured human blood cell lines of monocytoid (U937 and THP-1) and lymphoid (MOLT-4, Jurkat, and Raji) origin.⁴

1 Bastien, L., Sawyer, N., Grygorczyk, R., et al. Cloning, functional expression, and characterization of the human prostaglandin E₂ receptor EP₂ subtype. J Biol Chem 269 11873-11877 (1994).

2 Nishigaki, N., Negishi, M., Honda, A., et al. Identification of prostaglandin E receptor 'EP₂' cloned from mastocytoma cells as EP₄ subtype. FEBS Lett 364 339-341 (1995).

3 An, S., Yang, J., Xia, M., et al. Cloning and expression of the EP₂ subtype of human receptors for prostaglandin E₂. Biochem Biophys Res Commun 197 263-270 (1993).

4 Mori, K., Tanaka, I., Kotani, M., et al. Gene expression of the human prostaglandin E receptor EP₄ subtype: Differential regulation in monocytoid and lymphoid lineage cells by phorbol ester. J Mol Med 74 333-336 (1996).

5 Coleman, R.A., Eglen, R.M., Jones, R.L., et al. Classification of prostanoid receptors IUPHAR receptor compendium. IUPHAR Compendium 1-12 (1997).

6 Regan, J.W., Bailey, T.J., Pepperl, D.J., et al. Cloning of a novel human prostaglandin receptor with characteristics of the pharmacologically defined EP₂ subtype. Mol Pharmacol 46 213-220 (1994).

Nishigaki, N., Negishi, M., Honda, A., et al. Identification of prostaglandin E receptor 'EP₂' cloned from mastocytoma cells as EP₄ subtype. FEBS Lett 364 339-341 (1995).

Cosme, R., Lublin, D., Takafuji, V., et al. Prostanoids in human colonic mucosa: Effects of inflammation on PGE₂ receptor expression . Hum Immunol 61 684-696 (2000).

Narumiya, S., Sugimoto, Y., and Ushikubi, F. Prostanoid receptors: Structures, properties, and functions. Physiol Rev 79 1193-1226 (1999).

Regan, J.W., Bailey, T.J., Pepperl, D.J., et al. Cloning of a novel human prostaglandin receptor with characteristics of the pharmacologically defined EP₂ subtype. Mol Pharmacol 46 213-220 (1994).

Mori, K., Tanaka, I., Kotani, M., et al. Gene expression of the human prostaglandin E receptor EP₄ subtype: Differential regulation in monocytoid and lymphoid lineage cells by phorbol ester. J Mol Med 74 333-336 (1996).

Coleman, R.A., Eglen, R.M., Jones, R.L., et al. Classification of prostanoid receptors IUPHAR receptor compendium. IUPHAR Compendium 1-12 (1997).

Bastien, L., Sawyer, N., Grygorczyk, R., et al. Cloning, functional expression, and characterization of the human prostaglandin E₂ receptor EP₂ subtype. J Biol Chem 269 11873-11877 (1994).

An, S., Yang, J., Xia, M., et al. Cloning and expression of the EP₂ subtype of human receptors for prostaglandin E₂. Biochem Biophys Res Commun 197 263-270 (1993).

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