EP₄ Receptor (C-Term) Polyclonal 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 thought to be a subtype of the EP₂ receptor but 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 Antibody can be used for immunocytochemistry (ICC), immunohistochemistry (IHC), and Western blot (WB) 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).

Otake, S., Yoshida, K., Seira, N., et al. Cellular density-dependent fown-regulation of EP₄ prostanoid receptors via the up-regulation of hypoxia-inducible factor-1a in HCA-7 human colon cancer cells. Pharm. Res. Prespect. 3(1), e00083 (2014).

George, R.J., Sturmoski, M.A., Anant, S., et al. EP₄ mediates PGE₂ dependent cell survival through the PI3 kinase/AKT pathway. Prostaglandins Other Lipid Mediat. 83(1-2), 112-120 (2007).