EP₄ Receptor (C-Term) Polyclonal PE Antibody

Prostaglandin E₂ (PGE₂) binds to four receptor subtypes: EP₁, EP₂, EP₃, and EP₄, which are all membrane-bound G protein-coupled receptors (GPCRs).^1,2,3 The EP₄ receptor was originally classified as the EP₂ receptor but was not activated by the EP₂ agonist butaprost (Item Nos. 13740 | 13741) and was later found to be a distinct receptor with sequence differences.^4,5 It is expressed in many tissues, including the intestine, heart, kidney, lungs, and brain, and is also expressed in peripheral blood leukocytes and macrophages.³ The EP₄ receptor is coupled to Gα_s, and its activation increases intracellular cAMP levels, leading to tissue-specific effects. It induces smooth muscle relaxation, angiogenesis, T cell expansion, osteoblast differentiation, and bone resorption and inhibits TNF-α production in monocytes and macrophages, among other activities. PTGER4, the gene encoding the EP₄ receptor, is overexpressed in a variety of cancers, and antagonism of the receptor in animal models inhibits tumor growth and angiogenesis.⁶ In contrast, EP₄ receptor activation has anti-inflammatory and neuroprotective activities in vitro and in animal models.^7,8 Cayman’s EP₄ Receptor (C-Term) Polyclonal PE Antibody can be used for flow cytometry (FC) and immunofluorescence (IF) applications.

WARNING This product is not for human or veterinary use.

1. Narumiya, S., Sugimoto, Y., and Ushikubi, F. Prostanoid receptors: Structures, properties, and functions. Physiol. Rev. 79(4), 1193-1226 (1999).

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

3. Yokoyama, U., Iwatsubo, K., Umemura, M., et al. The prostanoid EP₄ receptor and its signaling pathway. Pharmacol. Rev. 65(3), 1010-1052 (2013).

4. Nishigaki, N., Negishi, M., Honda, A., et al. Identification of prostaglandin E receptor 'EP₂' cloned from mastocytoma cells as EP₄ subtype. FEBS Lett. 364(4), 339-341 (1995).

5. 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(2), 213-220 (1994).

6. Ching, M.M., Reader, J., and Fulton, A.M. Eicosanoids in cancer: Prostaglandin E₂ receptor 4 in cancer therapeutics and immunotherapy. Front. Pharmacol. 11, 819 (2020).

7. Tang, E.H.C., Libby, P., Vanhoutte, P.M., et al. Anti-inflammation therapy by activation of prostaglandin EP₄ receptor in cardiovascular and other inflammatory diseases. J. Cardiovasc. Pharmacol. 59(2), 116-123 (2012).

8. Pradhan, S.S., Salinas, K., Garduno, A.C., et al. Anti-inflammatory and neuroprotective effects of PGE₂ EP₄ signaling in models of Parkinson’s disease. J. Neuroimmune Pharmacol. 12(2), 292-304 (2017).