Prostaglandin E2 receptor EP4 subtype

Function

Receptor for prostaglandin E2 (PGE2). The activity of this receptor is mediated by G(s) proteins that stimulate adenylate cyclase. Has a relaxing effect on smooth muscle. May play an important role in regulating renal hemodynamics, intestinal epithelial transport, adrenal aldosterone secretion, and uterine function.

Classification

Family (Pfam)

PF00001 7tm_1

InterPro

GPCR_Rhodpsn, GPCR_Rhodpsn_7TM, Prost_EP4_rcpt, Prostanoid_rcpt, Prostglndn_DP_rcpt

Functional cluster

Membrane Transporters & GPCRs

Experimental structures · PDB · 10

• 5YHL X-ray 4.20A
• 5YWY X-ray 3.20A
• 7D7M EM 3.30A
• 8GCM EM 3.50A
• 8GCP EM 3.10A
• 8GD9 EM 3.20A
• 8GDA EM 3.30A
• 8GDB EM 3.10A
• 9JQY EM 2.92A
• 9JQZ EM 2.65A

A predicted model is available from AlphaFold.

Gene Ontology · 24

• GO:0016020 membrane
• GO:0005886 plasma membrane
• GO:0004957 prostaglandin E receptor activity
• GO:0007189 adenylate cyclase-activating G protein-coupled receptor signaling pathway
• GO:0007193 adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
• GO:0007188 adenylate cyclase-modulating G protein-coupled receptor signaling pathway
• GO:0060348 bone development
• GO:0071260 cellular response to mechanical stimulus
• GO:0071380 cellular response to prostaglandin E stimulus
• GO:0070371 ERK1 and ERK2 cascade
• GO:0006955 immune response
• GO:0006954 inflammatory response
• GO:0007254 JNK cascade
• GO:0001818 negative regulation of cytokine production
• GO:2000420 negative regulation of eosinophil extravasation
• GO:0050728 negative regulation of inflammatory response
• GO:0033624 negative regulation of integrin activation
• GO:0001819 positive regulation of cytokine production
• GO:0007204 positive regulation of cytosolic calcium ion concentration
• GO:0050729 positive regulation of inflammatory response
• GO:0051492 regulation of stress fiber assembly
• GO:0009612 response to mechanical stimulus
• GO:0034695 response to prostaglandin E
• GO:0042093 T-helper cell differentiation

Drugs targeting this protein · 4

• GRAPIPRANT antagonist
• RIVENPROST agonist
• DINOPROSTONE agonist
• VORBIPIPRANT antagonist

Related proteins · sequence + function similarity

• Prostaglandin E2 receptor EP4 subtype 1.00
• Prostaglandin E2 receptor EP4 subtype 0.98
• Prostaglandin E2 receptor EP4 subtype 0.98
• Prostaglandin E2 receptor EP4 subtype 0.98
• Prostaglandin E2 receptor EP4 subtype 0.97
• Prostaglandin E2 receptor EP2 subtype 0.89
• Prostaglandin E2 receptor EP2 subtype 0.88
• Prostaglandin E2 receptor EP2 subtype 0.88
• Prostaglandin E2 receptor EP2 subtype 0.87
• Prostaglandin E2 receptor EP3 subtype 0.86
• Prostaglandin F2-alpha receptor 0.86
• Prostaglandin E2 receptor EP3 subtype 0.86

Co-cited proteins · studied together in the literature

• Protein fem-1 homolog A 1 shared papers

Literature · 8 cited papers

• A novel prostaglandin E receptor 4-associated protein participates in antiinflammatory signaling. Circ. Res. · 2006
• The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
• Identification of a Ser/Thr cluster in the C-terminal domain of the human prostaglandin receptor EP4 that is essential for agonist-induced beta-arrestin1 recruitment but differs from the apparent principal phosphorylation site. Biochem. J. · 2004
• Sequestration and phosphorylation of the prostaglandin E2 EP4 receptor: dependence on the C-terminal tail. Biochem. Pharmacol. · 2001
• Gene expression of the human prostaglandin E receptor EP4 subtype: differential regulation in monocytoid and lymphoid lineage cells by phorbol ester. J. Mol. Med. · 1996
• The structure of the prostaglandin EP4 receptor gene and related pseudogenes. Genomics · 1996
• Cloning and expression of the EP2 subtype of human receptors for prostaglandin E2. Biochem. Biophys. Res. Commun. · 1993
• Cloning, functional expression, and characterization of the human prostaglandin E2 receptor EP2 subtype. J. Biol. Chem. · 1994