Protein Information

Name EP4 receptors
Synonyms EP4; PTGER 2; EP4 receptor; EP4R; PGE receptor EP4 subtype; PTGER 4…

Compound Information

Name cycloheximide
CAS

Reference List

PubMed Abstract RScore(About this table)
16464966 Balzary RW, Cocks TM: Lipopolysaccharide induces epithelium- and prostaglandin E (2)-dependent relaxation of mouse isolated trachea through activation of cyclooxygenase (COX)-1 and COX-2. J Pharmacol Exp Ther. 2006 May;317(2):806-12. Epub 2006 Feb 7.

The LPS antagonist polymixin B; the nonselective COX inhibitor indomethacin; the selective COX-1 and COX-2 inhibitors 5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole (SC560) and 4-[5-(4-chlorophenyl)-1-(trifluoromethyl)-1H-pyrazol-1-yl]-benzenesulfonam ide (SC236), respectively; the transcription inhibitor actinomycin D; the translation inhibitor cycloheximide; the p38 mitogen-activated protein kinase (p38 MAPK) inhibitor 4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imadazole (SB203580); and a combination of the mixed DP/EP1/EP2 receptor antagonist 6-isopropoxy-9-xanthone-2-carboxylic acid (AH6809) and the EP4 receptor antagonist 4'-[3-butyl-5-oxo-1-(2-trifluoromethyl-phenyl)-1-5-dihydro-[1,2,4] triazol- 4-ylmethyl]-biphenyl-2-sulfonic acid (3-methyl-thiophene-2-carbonyl)-amide (L-161982) all abolished relaxation to LPS, giving instead slowly developing, small contractions over 60 min.
32(0,1,1,2) Details
18223264 Molloy ES, Morgan MP, Doherty GA, McDonnell B, O'Byrne J, Fitzgerald DJ, McCarthy GM: Mechanism of basic calcium phosphate crystal-stimulated matrix metalloproteinase-13 expression by osteoarthritic synovial fibroblasts: inhibition by prostaglandin E2. Ann Rheum Dis. 2008 Dec;67(12):1773-9. Epub 2008 Jan 26.


These effects of PGE2 were diminished by L-161,982, a selective EP4 receptor antagonist, and mimicked by CAY10399, a selective EP2 receptor agonist, and forskolin, an adenylate cyclase activator.
2(0,0,0,2) Details
17067562 Frias MA, Rebsamen MC, Gerber-Wicht C, Lang U: Prostaglandin E2 activates Stat3 in neonatal rat ventricular cardiomyocytes: A role in cardiac hypertrophy. Cardiovasc Res. 2007 Jan 1;73(1):57-65. Epub 2006 Sep 27.

Experiments with agonists and antagonists of the PGE2 receptor subtypes EP1-EP4 indicate that PGE2 activates Stat3 mainly through the EP4 receptor.
Nuclear Stat3 phosphorylation induced by PGE2 is also suppressed by the translation and transcription inhibitors, cycloheximide and actinomycin D, respectively.
2(0,0,0,2) Details
19671668 Huang SK, White ES, Wettlaufer SH, Grifka H, Hogaboam CM, Thannickal VJ, Horowitz JC, Peters-Golden M: Prostaglandin E (2) induces fibroblast apoptosis by modulating multiple survival pathways. FASEB J. 2009 Dec;23(12):4317-26. Epub 2009 Aug 11.

PGE (2) also potentiated apoptosis elicited by Fas ligand plus cycloheximide.
These proapoptotic actions were dependent on signaling through the EP2/EP4 receptors and by downstream activation of both caspases 8 and 9.
1(0,0,0,1) Details