Prostaglandin F2-alpha receptor

Function

Receptor for prostaglandin F2-alpha (PGF2-alpha). The activity of this receptor is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system. Initiates luteolysis in the corpus luteum (By similarity). Isoforms 2 to 7 do not bind PGF2-alpha but are proposed to modulate signaling by participating in variant receptor complexes; heterodimers between isoform 1 and isoform 5 are proposed to be a receptor for prostamides including the synthetic analog bimatoprost.

Classification

Family (Pfam)

PF00001 7tm_1

InterPro

GPCR_Rhodpsn, GPCR_Rhodpsn_7TM, PglndnF_rcpt, Prostanoid_rcpt

Functional cluster

MFS & Drug-Efflux Transporters

Experimental structures · PDB · 8

• 8IQ4 EM 2.70A
• 8IQ6 EM 3.40A
• 8IUK EM 2.67A
• 8IUL EM 2.78A
• 8IUM EM 3.14A
• 8XJK EM 2.63A
• 8XJL EM 2.77A
• 8XJM EM 2.85A

A predicted model is available from AlphaFold.

Gene Ontology · 13

• GO:0005737 cytoplasm
• GO:0005576 extracellular region
• GO:0005886 plasma membrane
• GO:0004958 prostaglandin F receptor activity
• GO:0007189 adenylate cyclase-activating G protein-coupled receptor signaling pathway
• GO:0071799 cellular response to prostaglandin D stimulus
• GO:0007186 G protein-coupled receptor signaling pathway
• GO:0006954 inflammatory response
• GO:0007567 parturition
• GO:0008284 positive regulation of cell population proliferation
• GO:0007204 positive regulation of cytosolic calcium ion concentration
• GO:0010628 positive regulation of gene expression
• GO:0032355 response to estradiol

Drugs targeting this protein · 9

• LATANOPROST agonist
• TRAVOPROST agonist
• DINOPROST TROMETHAMINE agonist
• BIMATOPROST agonist
• CARBOPROST TROMETHAMINE agonist
• AL-12182 agonist
• TAFLUPROST agonist
• LATANOPROSTENE BUNOD agonist
• SEPETAPROST agonist

Related proteins · sequence + function similarity

• Prostaglandin F2-alpha receptor 0.99
• Prostaglandin F2-alpha receptor 0.99
• Prostaglandin F2-alpha receptor 0.99
• Prostaglandin F2-alpha receptor 0.99
• Prostaglandin E2 receptor EP3 subtype 0.93
• Prostaglandin E2 receptor EP3 subtype 0.92
• Prostaglandin E2 receptor EP3 subtype 0.90
• Prostaglandin E2 receptor EP3 subtype 0.90
• Prostaglandin E2 receptor EP3 subtype 0.90
• Prostaglandin E2 receptor EP3 subtype 0.89
• Thromboxane A2 receptor 0.89
• Prostaglandin E2 receptor EP2 subtype 0.85

Literature · 7 cited papers

• Identification and pharmacological characterization of the prostaglandin FP receptor and FP receptor variant complexes. Br. J. Pharmacol. · 2008
• 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
• Cloning and localization of hFP(S): a six-transmembrane mRNA splice variant of the human FP prostanoid receptor. Arch. Biochem. Biophys. · 2004
• Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat. Genet. · 2004
• Functional characterization of the ocular prostaglandin f2alpha (PGF2alpha) receptor. Activation by the isoprostane, 12-iso-PGF2alpha. J. Biol. Chem. · 1997
• Cloning and expression of a cDNA for the human prostanoid FP receptor. J. Biol. Chem. · 1994