Prostaglandin E2 receptor EP3 subtype

Function

Receptor for prostaglandin E2 (PGE2). The activity of this receptor can couple to both the inhibition of adenylate cyclase mediated by G(i) proteins, and to an elevation of intracellular calcium. Required for normal development of fever in response to pyrinogens, including IL1B, prostaglandin E2 and bacterial lipopolysaccharide (LPS). Required for normal potentiation of platelet aggregation by prostaglandin E2, and thus plays a role in the regulation of blood coagulation. Required for increased HCO3(-) secretion in the duodenum in response to mucosal acidification, and thereby contributes to the protection of the mucosa against acid-induced ulceration. Not required for normal kidney function, normal urine volume and osmolality (By similarity).

Classification

Family (Pfam)

PF00001 7tm_1

InterPro

EP3_rcpt_2, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM, Prostanoid_rcpt, Prostglndn_DP_rcpt, Prostglndn_EP3_rcpt

Functional cluster

Membrane Transporters & GPCRs

Experimental structures · PDB · 4

• 6AK3 X-ray 2.90A
• 6M9T X-ray 2.50A
• 7WU9 EM 3.38A
• 8GDC EM 3.50A

A predicted model is available from AlphaFold.

Gene Ontology · 13

• GO:0016020 membrane
• GO:0005635 nuclear envelope
• GO:0005886 plasma membrane
• GO:0004957 prostaglandin E receptor activity
• GO:0007189 adenylate cyclase-activating G protein-coupled receptor signaling pathway
• GO:0008219 cell death
• GO:0007186 G protein-coupled receptor signaling pathway
• GO:0006954 inflammatory response
• GO:0014827 intestine smooth muscle contraction
• GO:0060455 negative regulation of gastric acid secretion
• GO:0007200 phospholipase C-activating G protein-coupled receptor signaling pathway
• GO:0007204 positive regulation of cytosolic calcium ion concentration
• GO:0031622 positive regulation of fever generation

Drugs targeting this protein · 3

• SEPETAPROST agonist
• DINOPROSTONE agonist
• MISOPROSTOL agonist

Related proteins · sequence + function similarity

• Prostaglandin E2 receptor EP3 subtype 0.98
• Prostaglandin E2 receptor EP3 subtype 0.98
• Prostaglandin E2 receptor EP3 subtype 0.98
• Prostaglandin E2 receptor EP3 subtype 0.98
• Prostaglandin E2 receptor EP3 subtype 0.97
• Prostaglandin E2 receptor EP2 subtype 0.91
• Thromboxane A2 receptor 0.91
• Prostaglandin E2 receptor EP2 subtype 0.91
• Prostaglandin F2-alpha receptor 0.91
• Thromboxane A2 receptor 0.91
• Prostaglandin F2-alpha receptor 0.91
• Prostaglandin E2 receptor EP2 subtype 0.90

Literature · 13 cited papers

• Human protein factory for converting the transcriptome into an in vitro-expressed proteome. Nat. Methods · 2008
• A new mRNA splice variant coding for the human EP3-I receptor isoform. Prostaglandins Leukot. Essent. Fatty Acids · 2007
• The DNA sequence and biological annotation of human chromosome 1. Nature · 2006
• The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
• Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat. Genet. · 2004
• Structural organization of the human prostaglandin EP3 receptor subtype gene (PTGER3). Genomics · 1997
• Cloning and expression of three isoforms of the human EP3 prostanoid receptor. FEBS Lett. · 1994
• Cloning and expression of a prostaglandin E receptor EP3 subtype from human erythroleukaemia cells. Biochem. J. · 1994
• Cloning and expression of the EP3-subtype of human receptors for prostaglandin E2. Biochem. Biophys. Res. Commun. · 1994
• Molecular cloning and expression of human EP3 receptors: evidence of three variants with differing carboxyl termini. Br. J. Pharmacol. · 1994
• Isoforms of the EP3 subtype of human prostaglandin E2 receptor transduce both intracellular calcium and cAMP signals. Biochemistry · 1994
• Splice variants of the human EP3 receptor for prostaglandin E2. Eur. J. Biochem. · 1995
• … and 1 more in the literature graph