Target Information
Target General Infomation | |||||
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Target ID |
T75797
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Former ID |
TTDS00169
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Target Name |
Prostaglandin F2-alpha receptor
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Gene Name |
PTGFR
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Synonyms |
FP prostaglandin receptor; FP prostanoid receptor; PGF receptor; PGF2 alpha receptor; Prostanoid FP receptor; PTGFR
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Target Type |
Successful
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Disease | Aborting pregnancy [ICD9: 779.6; ICD10: O04] | ||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Dysmenorrhea [ICD9: 625.3; ICD10: N94.4-N94.6] | |||||
Glaucoma [ICD9: 365; ICD10: H40-H42] | |||||
Open-angle glaucoma; Ocular hypertension [ICD9: 365, 365.04; ICD10: H40-H42, H40.0] | |||||
Ocular disease [ICD10: H00-H59] | |||||
Renal cancer [ICD9: 140-229, 189; ICD10: C64] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T75797
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UniProt ID | |||||
Sequence |
MSMNNSKQLVSPAAALLSNTTCQTENRLSVFFSVIFMTVGILSNSLAIAILMKAYQRFRQ
KSKASFLLLASGLVITDFFGHLINGAIAVFVYASDKEWIRFDQSNVLCSIFGICMVFSGL CPLLLGSVMAIERCIGVTKPIFHSTKITSKHVKMMLSGVCLFAVFIALLPILGHRDYKIQ ASRTWCFYNTEDIKDWEDRFYLLLFSFLGLLALGVSLLCNAITGITLLRVKFKSQQHRQG RSHHLEMVIQLLAIMCVSCICWSPFLVTMANIGINGNHSLETCETTLFALRMATWNQILD PWVYILLRKAVLKNLYKLASQCCGVHVISLHIWELSSIKNSLKVAAISESPVAEKSAST |
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Drugs and Mode of Action | |||||
Drug(s) | Carboprost Tromethamine | Drug Info | Approved | Aborting pregnancy | [538496] |
Latanoprost | Drug Info | Approved | Open-angle glaucoma; Ocular hypertension | [536361], [539258] | |
Tafluprost | Drug Info | Approved | Glaucoma | [530618], [532210], [542476], [551871] | |
Travoprost | Drug Info | Approved | Open-angle glaucoma; Ocular hypertension | [536361], [542110] | |
LAROPIPRANT | Drug Info | Phase 4 | Discovery agent | [523049], [540312] | |
BOL-303259-X | Drug Info | Phase 3 | Renal cancer | [524354] | |
PGF2ALPHA-IE | Drug Info | Phase 3 | Glaucoma | [533334] | |
Latanoprost | Drug Info | Phase 2 | Glaucoma | [551115] | |
ONO-9054 | Drug Info | Phase 2 | Glaucoma | [533184] | |
Latanoprost | Drug Info | Phase 1/2 | Glaucoma | [551493] | |
PDC-41 | Drug Info | Phase 1 | Dysmenorrhea | [523270] | |
bimatoprost (free acid form) | Drug Info | Clinical trial | Alzheimer disease | [539256] | |
PGF2alpha | Drug Info | Clinical trial | Solid tumours | [532003] | |
Agonist | 13,14-dihydro-16-m-chlorophenoxy-w-tetranor-PGF1alpha | Drug Info | [525721] | ||
AL-8810 | Drug Info | [525568] | |||
AL12180 | Drug Info | [528506] | |||
bimatoprost (free acid form) | Drug Info | [525853] | |||
BOL-303259-X | Drug Info | [531388] | |||
carbacyclin | Drug Info | [525673] | |||
cloprostenol | Drug Info | [525673] | |||
fluprostenol | Drug Info | [534478] | |||
I-BOP | Drug Info | [534478] | |||
Latanoprost | Drug Info | [537255] | |||
M&B 28767 | Drug Info | [534478] | |||
PGD2 | Drug Info | [534478] | |||
PGF2alpha | Drug Info | [526505] | |||
Travoprost | Drug Info | [537092] | |||
U46619 | Drug Info | [525673] | |||
[3H](+)-fluprostenol | Drug Info | [543781] | |||
[3H]PGF2alpha | Drug Info | [533982] | |||
Antagonist | AS604872 | Drug Info | [528941] | ||
PDC-31 | Drug Info | [543781] | |||
PDC-41 | Drug Info | [526514] | |||
Modulator | Carboprost Tromethamine | Drug Info | [556264] | ||
H2S-releasing latanoprost | Drug Info | [543781] | |||
NCX-125 | Drug Info | [543781] | |||
ONO-9054 | Drug Info | [533184] | |||
PGF2ALPHA-IE | Drug Info | [533620], [551871] | |||
Tafluprost | Drug Info | [551871] | |||
Inhibitor | LAROPIPRANT | Drug Info | [528672] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
Reactome | Prostanoid ligand receptors | ||||
G alpha (q) signalling events | |||||
WikiPathways | Prostaglandin Synthesis and Regulation | ||||
GPCRs, Class A Rhodopsin-like | |||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
Small Ligand GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
GPCRs, Other | |||||
References | |||||
Ref 523049 | ClinicalTrials.gov (NCT01126073) Niacin/Laropiprant and Endothelial Function. U.S. National Institutes of Health. | ||||
Ref 523270 | ClinicalTrials.gov (NCT01250587) Dose-Finding Study of PDC31 in Patients With Primary Dysmenorrhea. U.S. National Institutes of Health. | ||||
Ref 524354 | ClinicalTrials.gov (NCT01895972) A Study Evaluating the Long-Term Safety of Latanoprostene Bunod Ophthalmic Solution 0.024%, in Japanese Subjects With Open-Angle Glaucoma or Ocular Hypertension. U.S.National Institutes of Health. | ||||
Ref 530618 | Mol Endocrinol. 2010 Feb;24(2):436-46. Epub 2010 Jan 5.Pasireotide and octreotide stimulate distinct patterns of sst2A somatostatin receptor phosphorylation. | ||||
Ref 532003 | Stereocontrolled organocatalytic synthesis of prostaglandin PGF2alpha in seven steps. Nature. 2012 Sep 13;489(7415):278-81. | ||||
Ref 533184 | IOP-Lowering Effect of ONO-9054, A Novel Dual Agonist of Prostanoid EP3 and FP Receptors, in Monkeys. Invest Ophthalmol Vis Sci. 2015 Apr;56(4):2547-52. | ||||
Ref 533334 | The effect of prostaglandin F2 alpha-1-isopropylester (PGF2 alpha-IE) on uveoscleral outflow. Prog Clin Biol Res. 1989;312:429-36. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 538496 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017989. | ||||
Ref 539256 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1959). | ||||
Ref 539258 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1961). | ||||
Ref 540312 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3356). | ||||
Ref 542110 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7102). | ||||
Ref 525568 | AL-8810: a novel prostaglandin F2 alpha analog with selective antagonist effects at the prostaglandin F2 alpha (FP) receptor. J Pharmacol Exp Ther. 1999 Sep;290(3):1278-84. | ||||
Ref 525673 | The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta. 2000 Jan 17;1483(2):285-93. | ||||
Ref 525721 | J Med Chem. 2000 Mar 9;43(5):945-52.Design and synthesis of 13,14-dihydro prostaglandin F(1alpha) analogues as potent and selective ligands for the human FP receptor. | ||||
Ref 525853 | Replacement of the carboxylic acid group of prostaglandin f(2alpha) with a hydroxyl or methoxy substituent provides biologically unique compounds. Br J Pharmacol. 2000 Aug;130(8):1933-43. | ||||
Ref 526505 | Identification by site-directed mutagenesis of amino acids contributing to ligand-binding specificity or signal transduction properties of the human FP prostanoid receptor. Biochem J. 2003 Apr 15;371(Pt 2):443-9. | ||||
Ref 526514 | THG113: a novel selective FP antagonist that delays preterm labor. Semin Perinatol. 2002 Dec;26(6):389-97. | ||||
Ref 528506 | Preclinical pharmacology of AL-12182, a new ocular hypotensive 11-oxa prostaglandin analog. J Ocul Pharmacol Ther. 2006 Oct;22(5):291-309. | ||||
Ref 528672 | J Med Chem. 2007 Feb 22;50(4):794-806.Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). | ||||
Ref 528941 | Arrest of preterm labor in rat and mouse by an oral and selective nonprostanoid antagonist of the prostaglandin F2alpha receptor (FP). Am J Obstet Gynecol. 2007 Jul;197(1):54.e1-9. | ||||
Ref 531388 | Ocular hypotensive activity of BOL-303259-X, a nitric oxide donating prostaglandin F2alpha agonist, in preclinical models. Exp Eye Res. 2011 Sep;93(3):250-5. | ||||
Ref 533184 | IOP-Lowering Effect of ONO-9054, A Novel Dual Agonist of Prostanoid EP3 and FP Receptors, in Monkeys. Invest Ophthalmol Vis Sci. 2015 Apr;56(4):2547-52. | ||||
Ref 533620 | Role of nitric oxide in PGF2 alpha-induced ocular hyperemia. Exp Eye Res. 1994 Oct;59(4):401-7. | ||||
Ref 533982 | Cloning and expression of a cDNA for the human prostanoid FP receptor. J Biol Chem. 1994 Jan 28;269(4):2632-6. | ||||
Ref 534478 | Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1997 Sep;122(2):217-24. | ||||
Ref 537092 | Prostaglandin subtype-selective and non-selective IOP-lowering comparison in monkeys. J Ocul Pharmacol Ther. 2009 Feb;25(1):1-8. | ||||
Ref 537255 | PGF(2alpha) FP Receptor Contributes to Brain Damage Following Transient Focal Brain Ischemia. Neurotox Res. 2009 Jan;15(1):62-70. Epub 2009 Feb 11. | ||||
Ref 543781 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 344). |
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