PGE2

Synonyms

PGE2 receptor EP2 subtype, Prostanoid EP2 receptor, PGE receptor EP2 subtype, PTGER2, Prostaglandin E Receptor 2, Prostaglandin E Receptor 2 (Subtype EP2), 53kDa, Prostaglandin E Receptor 2 (Subtype EP2), 53kD, Prostaglandin E2 Receptor EP2 Subtype, EP2, Receptors, Prostaglandin E, EP2 Subtype

Description

The activity of PTGER2 (Prostanoid EP2 receptor) is mediated by G(s) proteins that stimulate adenylate cyclase. The subsequent raise in intracellular cAMP is responsible for the relaxing effect of this receptor on smooth muscle.

KO Status

F0

Drug Information

Launched drugs: 6
Drug in clinical trials: 1
Latest Research Phase: Approved

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Mifepristone/Misoprostol

Approved

Sun Pharmaceutical

Terminate pregnancy

Diclofenac Sodium/Misoprostol

KP-107

Approved

Pfizer Pharmaceuticals Ltd (China)

Arthritis, Rheumatoid, Osteoarthritis

Misoprostol

SC-29333, XP-16J

Approved

Pfizer Pharmaceuticals Ltd (China)

Labor, Induced, Stomach Neoplasms, Duodenal Ulcer, Stomach Ulcer, Peptic Ulcer

Limaprost alfadex

OP-1206, OP-1206.alpha-CD, Ono-1206.alpha-CD

Approved

Peripheral Vascular Diseases

Misoprostol/Naproxen

Approved

Pfizer Inc

Arthritis

Omidenepag isopropyl

DE-117, G0G0H52U6K

Approved

Ube Industries Ltd, Santen

Glaucoma, Open-Angle, Ocular Hypertension, Glaucoma

ONO-8055

ONO-8055

Phase 1 Clinical

Ono Pharmaceutical Co Ltd

Urinary Bladder, Underactive

TPST-1495

TPST-1495

Phase 1 Clinical

Tempest Therapeutics

Solid tumours, Squamous Cell Carcinoma of Head and Neck, Stomach Neoplasms, Esophageal Neoplasms, Carcinoma, Transitional Cell, Colorectal Neoplasms, Endometrial Neoplasms, Carcinoma, Non-Small-Cell Lung, Adenocarcinoma

KRP-EPA-605

KEA-0447, KRP-EPA605

Pending

Kyorin

Urinary Bladder, Overactive

Aganepag isopropyl

AGN-210961

Pending

Allergan Plc

Glaucoma, Open-Angle, Ocular Hypertension, Glaucoma

References


Title

Authors

Source

Cloning of a novel human prostaglandin receptor with characteristics of the pharmacologically defined EP2 subtype

Regan J.W., Bailey T.J., Pepperl D.J., Pierce K.L., Bogardus A.M., Donello J.E., Fairbairn C.E., Kedzie K.M., Woodward D.F., Gil D.W.,

Mol. Pharmacol. 46:213-220(1994)

Cloning, structural characterization, and chromosomal localization of the gene encoding the human prostaglandin E2 receptor EP2 subtype

Smock S.L., Pan L.C., Castleberry T.A., Lu B., Mather R.J., Owen T.A.,

Gene 237:393-402(1999)

The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)

The MGC Project Team,

Genome Res. 14:2121-2127(2004)

Cloning of a novel human prostaglandin receptor with characteristics of the pharmacologically defined EP2 subtype.

Regan J.W., Bailey T.J., Pepperl D.J., Pierce K.L., Bogardus A.M., Donello J.E., Fairbairn C.E., Kedzie K.M., Woodward D.F., Gil D.W.,

Mol. Pharmacol. 46:213-220(1994)

Cloning, structural characterization, and chromosomal localization of the gene encoding the human prostaglandin E2 receptor EP2 subtype.

Smock S.L., Pan L.C., Castleberry T.A., Lu B., Mather R.J., Owen T.A.,

Gene 237:393-402(1999)

The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).

The MGC Project Team,

Genome Res. 14:2121-2127(2004)

Selective inhibition of heterotrimeric Gs signaling. Targeting the receptor-G protein interface using a peptide minigene encoding the Galpha(s) carboxyl terminus.

Feldman D.S., Zamah A.M., Pierce K.L., Miller W.E., Kelly F., Rapacciuolo A., Rockman H.A., Koch W.J., Luttrell L.M.,

J Biol Chem 277:28631-28640(2002)

PGE(2) receptors and synthesis in human gastric mucosa: perturbation in cancer.

Takafuji V.A., Evans A., Lynch K.R., Roche J.K.,

Prostaglandins Leukot Essent Fatty Acids 66:71-81(2002)

Similarities and differences in the coupling of human beta1- and beta2-adrenoceptors to Gs(alpha) splice variants.

Wenzel-Seifert K., Liu H.Y., Seifert R.,

Biochem Pharmacol 64:9-20(2002)

Prostaglandin E2 is a key factor for CCR7 surface expression and migration of monocyte-derived dendritic cells.

Scandella E., Men Y., Gillessen S., Forster R., Groettrup M.,

Blood 100:1354-1361(2002)