Target Information
Target General Infomation | |||||
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Target ID |
T68782
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Former ID |
TTDR00802
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Target Name |
Prostaglandin D2 receptor
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Gene Name |
PTGDR
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Synonyms |
PGD receptor; Prostanoid DP receptor; PTGDR
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Target Type |
Clinical Trial
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Disease | Allergy [ICD9: 995.3; ICD10: T78.4] | ||||
Asthma [ICD10: J45] | |||||
Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4] | |||||
Atopic dermatitis [ICD9: 691.8, 692.9; ICD10: L00-L99] | |||||
Dyslipidaemias [ICD9: 272; ICD10: E78] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Rhinitis [ICD9: 472.0, 477; ICD10: J00, J30, J31.0] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82] | |||||
Thromboembolism [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82] | |||||
Function |
Receptor for prostaglandin D2 (PGD2). The activity of this receptor is mainly mediated by G(s) proteins that stimulate adenylate cyclase, resulting in an elevation of intracellular cAMP. A mobilization of calcium is also observed, but without formation of inositol 1,4,5-trisphosphate (By similarity).
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T68782
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UniProt ID | |||||
Sequence |
MKSPFYRCQNTTSVEKGNSAVMGGVLFSTGLLGNLLALGLLARSGLGWCSRRPLRPLPSV
FYMLVCGLTVTDLLGKCLLSPVVLAAYAQNRSLRVLAPALDNSLCQAFAFFMSFFGLSST LQLLAMALECWLSLGHPFFYRRHITLRLGALVAPVVSAFSLAFCALPFMGFGKFVQYCPG TWCFIQMVHEEGSLSVLGYSVLYSSLMALLVLATVLCNLGAMRNLYAMHRRLQRHPRSCT RDCAEPRADGREASPQPLEELDHLLLLALMTVLFTMCSLPVIYRAYYGAFKDVKEKNRTS EEAEDLRALRFLSVISIVDPWIFIIFRSPVFRIFFHKIFIRPLRYRSRCSNSTNMESSL |
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Drugs and Mode of Action | |||||
Drug(s) | LAROPIPRANT | Drug Info | Phase 4 | Discovery agent | [523049], [540312] |
QAW-039 | Drug Info | Phase 3 | Asthma | [525329] | |
AMG 853 | Drug Info | Phase 2 | Asthma | [522862] | |
MK-1029 | Drug Info | Phase 2 | Asthma | [523952] | |
ONO-4053 | Drug Info | Phase 2 | Allergic rhinitis | [524158] | |
S-555739 | Drug Info | Phase 2 | Allergy | [551683] | |
TS-022 | Drug Info | Phase 2 | Atopic dermatitis | [522686] | |
192C86 | Drug Info | Phase 1 | Thrombosis | [526857] | |
SAR-389644 | Drug Info | Phase 1 | Allergic rhinitis | [548481] | |
PGF2alpha | Drug Info | Clinical trial | Solid tumours | [532003] | |
Laropiprant+niacin | Drug Info | Discontinued in Phase 3 | Dyslipidaemias | [522926] | |
S-5751 | Drug Info | Discontinued in Phase 2 | Rhinitis | [539197], [547015] | |
ONO-4127Na | Drug Info | Discontinued in Phase 1 | Allergic rhinitis | [547738] | |
ZK-118182 | Drug Info | Terminated | Thromboembolism | [539190], [545456] | |
Agonist | 15-deoxy-Delta12,14-PGJ2 | Drug Info | [534620] | ||
butaprost (free acid form) | Drug Info | [525673] | |||
BW 245C | Drug Info | [534478] | |||
carbacyclin | Drug Info | [525673] | |||
cloprostenol | Drug Info | [525673] | |||
Delta12-PGJ2 | Drug Info | [534620] | |||
L-644,698 | Drug Info | [525559] | |||
L-888,291 | Drug Info | [527465] | |||
PGD2 | Drug Info | [525559] | |||
PGF2alpha | Drug Info | [525673] | |||
PGJ2 | Drug Info | [534620] | |||
RS 93520 | Drug Info | [525753] | |||
SQ-27986 | Drug Info | [525753] | |||
TS-022 | Drug Info | [528554] | |||
U46619 | Drug Info | [525673] | |||
ZK110841 | Drug Info | [534620] | |||
[3H]PGD2 | Drug Info | [528126] | |||
Modulator | 192C86 | Drug Info | [544117] | ||
AMG 853 | Drug Info | ||||
TTH 03-001 | Drug Info | [543775] | |||
ZK-118182 | Drug Info | [525716] | |||
Antagonist | AH6809 | Drug Info | [525673] | ||
BWA868C | Drug Info | [534620] | |||
Laropiprant+niacin | Drug Info | [536740] | |||
ONO-4053 | Drug Info | [551636] | |||
ONO-4127Na | Drug Info | [531930] | |||
ONO-AE3-237 | Drug Info | [529248] | |||
Prostaglandin D2 antagonists | Drug Info | [543775] | |||
QAW-039 | Drug Info | [550305] | |||
S-555739 | Drug Info | [551683] | |||
S-5751 | Drug Info | [531635] | |||
SAR-389644 | Drug Info | [550898] | |||
[3H]BWA868C | Drug Info | [525913] | |||
Inhibitor | DIASTEREOMER 2 | Drug Info | [528672] | ||
LAROPIPRANT | Drug Info | [528672] | |||
MK-1029 | Drug Info | [532493] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Pathway Interaction Database | Thromboxane A2 receptor signaling | ||||
PathWhiz Pathway | Intracellular Signalling Through PGD2 receptor and Prostaglandin D2 | ||||
Reactome | Prostanoid ligand receptors | ||||
G alpha (s) signalling events | |||||
WikiPathways | Prostaglandin Synthesis and Regulation | ||||
GPCRs, Class A Rhodopsin-like | |||||
Small Ligand GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 522686 | ClinicalTrials.gov (NCT00914186) Study of TS-022 in Adult Patients With Atopic Dermatitis With Pruritus (POC). U.S. National Institutes of Health. | ||||
Ref 522862 | ClinicalTrials.gov (NCT01018550) AMG 853 Phase 2 Study in Subjects With Inadequately Controlled Asthma. U.S. National Institutes of Health. | ||||
Ref 522926 | ClinicalTrials.gov (NCT01054508) Effect of Tredaptive on Serum Lipoproteins and Inflammatory Markers. U.S. National Institutes of Health. | ||||
Ref 523049 | ClinicalTrials.gov (NCT01126073) Niacin/Laropiprant and Endothelial Function. U.S. National Institutes of Health. | ||||
Ref 523952 | ClinicalTrials.gov (NCT01624974) Study to Evaluate the Effectiveness and Safety of MK-1029 in the Treatment of Persistent Asthma That is Not Controlled With Montelukast (ML) in Adults (MK-1029-011 AM2). U.S. National Institutes of Health. | ||||
Ref 524158 | ClinicalTrials.gov (NCT01748344) Phase II Study Evaluating ONO-4053 and Cetirizine in Subjects With Seasonal Allergic Rhinitis. U.S. National Institutes of Health. | ||||
Ref 525329 | ClinicalTrials.gov (NCT02563067) Study of Efficacy and Safety of QAW039 in Patients With Severe Asthma Inadequately Controlled With Standard of Care Asthma Treatment. | ||||
Ref 526857 | The effect of a prostaglandin DP-receptor partial agonist (192C86) on platelet aggregation and the cardiovascular system in healthy volunteers. Br J Clin Pharmacol. 1992 Oct;34(4):344-51. | ||||
Ref 532003 | Stereocontrolled organocatalytic synthesis of prostaglandin PGF2alpha in seven steps. Nature. 2012 Sep 13;489(7415):278-81. | ||||
Ref 539190 | (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: 1890). | ||||
Ref 539197 | (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: 1898). | ||||
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 545456 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003331) | ||||
Ref 547015 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012090) | ||||
Ref 547738 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018932) | ||||
Ref 525559 | A novel biological role for prostaglandin D2 is suggested by distribution studies of the rat DP prostanoid receptor. Eur J Pharmacol. 1999 Jul 14;377(1):101-15. | ||||
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 525716 | Characterization of prostanoid receptors mediating inhibition of histamine release from anti-IgE-activated rat peritoneal mast cells. Br J Pharmacol. 2000 Feb;129(3):589-97. | ||||
Ref 525753 | Affinities, selectivities, potencies, and intrinsic activities of natural and synthetic prostanoids using endogenous receptors: focus on DP class prostanoids. J Pharmacol Exp Ther. 2000 May;293(2):321-8. | ||||
Ref 525913 | Pharmacology and autoradiography of human DP prostanoid receptors using [(3)H]-BWA868C, a DP receptor-selective antagonist radioligand. Br J Pharmacol. 2000 Nov;131(6):1025-38. | ||||
Ref 527465 | Identification of a potent and selective synthetic agonist at the CRTH2 receptor. Mol Pharmacol. 2005 Jun;67(6):1834-9. Epub 2005 Mar 8. | ||||
Ref 528126 | GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist. Br J Pharmacol. 2006 Jun;148(3):326-39. | ||||
Ref 528554 | Effects of TS-022, a newly developed prostanoid DP1 receptor agonist, on experimental pruritus, cutaneous barrier disruptions and atopic dermatitis in mice. Eur J Pharmacol. 2007 Feb 5;556(1-3):207-14. Epub 2006 Nov 3. | ||||
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 529248 | Prostaglandin D2 inhibits the production of IFN-gamma by invariant NK T cells: consequences in the control of B16 melanoma. J Immunol. 2008 Jan 15;180(2):783-92. | ||||
Ref 531635 | Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36. | ||||
Ref 531930 | Sleep-wake regulation by prostaglandin D2 and adenosine. Brain Nerve. 2012 Jun;64(6):621-8. | ||||
Ref 532493 | Update on the status of DP2 receptor antagonists; from proof of concept through clinical failures to promising new drugs. Expert Opin Investig Drugs. 2014 Jan;23(1):55-66. | ||||
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 534620 | Characterization of the recombinant human prostanoid DP receptor and identification of L-644,698, a novel selective DP agonist. Br J Pharmacol. 1998 Apr;123(7):1317-24. | ||||
Ref 543775 | (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: 338). | ||||
Ref 544117 | Prostanoid receptor antagonists: development strategies and therapeutic applications. Br J Pharmacol. 2009 September; 158(1): 104-145. | ||||
Ref 550305 | Effect Of QAW039, An Oral Prostaglandin D2 Receptor (DP2/CRTh2) Antagonist, Upon Sputum And Bronchial Eosinophilic Inflammation And Clinical Outcomes In Treatment-Resistant Asthma: A Phase 2a Randomized Placebo-Controlled Trial. American Thoracic Society Journals. 2015. | ||||
Ref 550898 | US patent application no. 2008,0300,217, Combination therapy with fumaric acid esters for the treatment of autoimmune and,or inflammatory disorders. |
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