Target Information
Target General Infomation | |||||
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Target ID |
T61722
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Former ID |
TTDC00237
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Target Name |
Putative G-protein coupled receptor 44
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Gene Name |
PTGDR2
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Synonyms |
CD294; Chemoattractant receptor-homologous molecule expressed on Th2 cells; PTGDR2
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Target Type |
Clinical Trial
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Disease | Asthma; Chronic obstructive pulmonary disease [ICD9: 490-492, 493, 494-496; ICD10: J40-J44, J47, J45] | ||||
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] | |||||
Allergic asthma [ICD9: 493, 995.3; ICD10: J45, T78.4] | |||||
Respiratory disease [ICD10: J00-J99] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Function |
Receptor for prostaglandin D2 (PGD2). Coupled to the G(i)-protein. Receptor activation may result in pertussis toxin- sensitive decreases in cAMP levels and Ca(2+) mobilization. PI3K signaling is also implicated in mediating PTGDR2 effects. PGD2 induced receptor internalization. CRTH2 internalization can be regulated by diverse kinases such as, PKC, PKA, ADRBK1/GRK2, GPRK5/GRK5 and GRK6. Receptoractivation is responsible, at least in part, in immune regulation and allergic/inflammation responses.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T61722
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UniProt ID | |||||
Sequence |
MSANATLKPLCPILEQMSRLQSHSNTSIRYIDHAAVLLHGLASLLGLVENGVILFVVGCR
MRQTVVTTWVLHLALSDLLASASLPFFTYFLAVGHSWELGTTFCKLHSSIFFLNMFASGF LLSAISLDRCLQVVRPVWAQNHRTVAAAHKVCLVLWALAVLNTVPYFVFRDTISRLDGRI MCYYNVLLLNPGPDRDATCNSRQVALAVSKFLLAFLVPLAIIASSHAAVSLRLQHRGRRR PGRFVRLVAAVVAAFALCWGPYHVFSLLEARAHANPGLRPLVWRGLPFVTSLAFFNSVAN PVLYVLTCPDMLRKLRRSLRTVLESVLVDDSELGGAGSSRRRRTSSTARSASPLALCSRP EEPRGPARLLGWLLGSCAASPQTGPLNRALSSTSS |
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Drugs and Mode of Action | |||||
Drug(s) | LAROPIPRANT | Drug Info | Phase 4 | Discovery agent | [523049], [540312] |
Setipiprant | Drug Info | Phase 3 | Asthma | [523711] | |
ADC-3680 | Drug Info | Phase 2 | Allergic rhinitis | [523652] | |
AMG 853 | Drug Info | Phase 2 | Asthma | [522862] | |
ARRY-502 | Drug Info | Phase 2 | Allergic asthma | [523846] | |
AZD1981 | Drug Info | Phase 2 | Asthma; Chronic obstructive pulmonary disease | [522453], [542660] | |
OC-000459 | Drug Info | Phase 2 | Allergy | [522929] | |
QAV-680 | Drug Info | Phase 2 | Allergic rhinitis | [523004] | |
AM-211 | Drug Info | Phase 1 | Asthma | [548899] | |
AM-461 | Drug Info | Phase 1 | Respiratory disease | [549002] | |
AP-761 | Drug Info | Phase 1 | Asthma | [548763] | |
MK-7246 | Drug Info | Phase 1 | Respiratory disease | [548999] | |
PGF2alpha | Drug Info | Clinical trial | Solid tumours | [532003] | |
AZD5985 | Drug Info | Discontinued in Phase 1 | Asthma; Chronic obstructive pulmonary disease | [548831] | |
AZD8075 | Drug Info | Discontinued in Phase 1 | Asthma; Chronic obstructive pulmonary disease | [548825] | |
RG-7185 | Drug Info | Discontinued in Phase 1 | Asthma | [549165] | |
Agonist | 13,14-dihydro-15-keto-PGD2 | Drug Info | [527831] | ||
13,14-dihydro-15-keto-PGF2alpha | Drug Info | [526477] | |||
15(R)-15-methyl-PGD2 | Drug Info | [527831] | |||
15(S)-15-methyl-PGD2 | Drug Info | [526477] | |||
15-deoxy-Delta12,14-PGD2 | Drug Info | [526611] | |||
15-deoxy-Delta12,14-PGJ2 | Drug Info | [526611] | |||
CAY 10471 | Drug Info | [527436] | |||
Delta12-PGJ2 | Drug Info | [526477] | |||
L-888,291 | Drug Info | [527465] | |||
PGD2 | Drug Info | [527831] | |||
PGD3 | Drug Info | [526611] | |||
PGF2alpha | Drug Info | [526611] | |||
PGJ2 | Drug Info | [526477] | |||
U46619 | Drug Info | [526477] | |||
[3H]PGD2 | Drug Info | [527971] | |||
Inhibitor | 2-(2,4-diphenylthiazol-5-yl)acetic acid | Drug Info | [530594] | ||
2-(2-acetyl-4-bromophenoxy)acetic acid | Drug Info | [528566] | |||
2-(2-allyl-4-chlorophenoxy)acetic acid | Drug Info | [528862] | |||
2-(2-benzhydryl-4-phenylthiazol-5-yl)acetic acid | Drug Info | [530588] | |||
2-(2-benzoyl-4-bromophenoxy)acetic acid | Drug Info | [528566] | |||
2-(2-cyclohexyl-4-fluorophenoxy)acetic acid | Drug Info | [528862] | |||
2-(2-cyclohexyl-4-methoxyphenoxy)acetic acid | Drug Info | [528862] | |||
2-(2-cyclohexyl-4-methylphenoxy)acetic acid | Drug Info | [528862] | |||
2-(2-cyclohexylphenoxy)acetic acid | Drug Info | [528862] | |||
2-(2-formylphenoxy)acetic acid | Drug Info | [528566] | |||
2-(4-bromo-2-(hydroxymethyl)phenoxy)acetic acid | Drug Info | [528566] | |||
2-(4-bromo-2-cyclohexylphenoxy)acetic acid | Drug Info | [528862] | |||
2-(4-bromo-2-formylphenoxy)acetic acid | Drug Info | [528566] | |||
2-(4-bromo-2-tert-butylphenoxy)acetic acid | Drug Info | [528566] | |||
2-(4-chloro-2-cycloheptylphenoxy)acetic acid | Drug Info | [530255] | |||
2-(4-chloro-2-cyclohexylphenoxy)acetic acid | Drug Info | [528862] | |||
2-(4-chloro-2-cyclopentylphenoxy)acetic acid | Drug Info | [528862] | |||
2-(4-cyano-2-cyclohexylphenoxy)acetic acid | Drug Info | [528862] | |||
3-(4-chloro-2-cyclohexylphenoxy)propanoic acid | Drug Info | [528862] | |||
4-(4-chloro-2-cyclohexylphenoxy)butanoic acid | Drug Info | [528862] | |||
IW-1221 | Drug Info | [543776] | |||
L-888607 | Drug Info | [527768] | |||
LAROPIPRANT | Drug Info | [528672] | |||
Methyl 2-(4-chloro-2-cyclohexylphenoxy)acetate | Drug Info | [528862] | |||
Antagonist | ADC-3680 | Drug Info | [532493] | ||
ADC-9971 | Drug Info | [543776] | |||
AM-156 | Drug Info | [543776] | |||
AM-211 | Drug Info | [531433] | |||
AM-461 | Drug Info | [531698] | |||
AP-761 | Drug Info | [548764] | |||
AZD1981 | Drug Info | [550288] | |||
AZD5985 | Drug Info | [550288] | |||
AZD8075 | Drug Info | [550288] | |||
CRTH2 antagonists | Drug Info | [543776] | |||
CRTh2 receptor antagonists | Drug Info | [543776] | |||
CRTh2 receptor antagonists | Drug Info | [543776] | |||
OC-000459 | Drug Info | [532216] | |||
QAV-680 | Drug Info | [532474] | |||
RG-7185 | Drug Info | [549166] | |||
Setipiprant | Drug Info | [532856] | |||
TM-30089 | Drug Info | [543776] | |||
[3H]ramatroban | Drug Info | [527831] | |||
Modulator | AMG 853 | Drug Info | |||
ARRY-502 | Drug Info | [550275] | |||
MK-7246 | Drug Info | [531277] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
References | |||||
Ref 522453 | ClinicalTrials.gov (NCT00766415) 14729-D9831C00002- 1 Month Biopsy Study. 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 522929 | ClinicalTrials.gov (NCT01056783) Proof of Concept Study of OC000459 in Eosinophilic Esophagitis. U.S. National Institutes of Health. | ||||
Ref 523004 | ClinicalTrials.gov (NCT01103037) Efficacy, Safety and Pharmacokinetics of QAV680 Versus Placebo in Patients With Asthma. U.S. National Institutes of Health. | ||||
Ref 523049 | ClinicalTrials.gov (NCT01126073) Niacin/Laropiprant and Endothelial Function. U.S. National Institutes of Health. | ||||
Ref 523652 | ClinicalTrials.gov (NCT01448954) A Study to Evaluate Safety, Tolerability and Pharmacokinetics of ADC3680B in Subjects With Partly Controlled Atopic Asthma. U.S. National Institutes of Health. | ||||
Ref 523711 | ClinicalTrials.gov (NCT01484119) Efficacy, Safety, and Tolerability Study of ACT-129968 in Patients With Seasonal Allergic Rhinitis. U.S. National Institutes of Health. | ||||
Ref 523846 | ClinicalTrials.gov (NCT01561690) A Study of ARRY-502 in Patients With Persistent Asthma. U.S. National Institutes of Health. | ||||
Ref 532003 | Stereocontrolled organocatalytic synthesis of prostaglandin PGF2alpha in seven steps. Nature. 2012 Sep 13;489(7415):278-81. | ||||
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 542660 | (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: 7680). | ||||
Ref 548763 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028464) | ||||
Ref 548825 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029210) | ||||
Ref 548831 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029299) | ||||
Ref 548899 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030063) | ||||
Ref 548999 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031315) | ||||
Ref 526477 | Molecular pharmacology of the human prostaglandin D2 receptor, CRTH2. Br J Pharmacol. 2002 Dec;137(8):1163-72. | ||||
Ref 526611 | Expression and molecular pharmacology of the mouse CRTH2 receptor. J Pharmacol Exp Ther. 2003 Aug;306(2):463-70. Epub 2003 Apr 29. | ||||
Ref 527436 | Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem. 2005 Feb 24;48(4):897-900. | ||||
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 527768 | J Med Chem. 2005 Oct 6;48(20):6174-7.Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2. | ||||
Ref 527831 | CRTH2-specific binding characteristics of [3H]ramatroban and its effects on PGD2-, 15-deoxy-Delta12, 14-PGJ2- and indomethacin-induced agonist responses. Eur J Pharmacol. 2005 Nov 7;524(1-3):30-7. Epub 2005 Oct 27. | ||||
Ref 527971 | On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2. Mol Pharmacol. 2006 Apr;69(4):1441-53. Epub 2006 Jan 17. | ||||
Ref 528566 | J Med Chem. 2006 Nov 16;49(23):6638-41.Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits. | ||||
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 528862 | Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. Epub 2007 May 13.2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists. | ||||
Ref 530255 | Bioorg Med Chem Lett. 2009 Aug 15;19(16):4794-8. Epub 2009 Jun 14.7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists. | ||||
Ref 530588 | Bioorg Med Chem Lett. 2010 Feb 1;20(3):1181-5. Epub 2009 Dec 6.Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 2. | ||||
Ref 530594 | Bioorg Med Chem Lett. 2010 Feb 1;20(3):1177-80. Epub 2009 Dec 4.Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1. | ||||
Ref 531277 | Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. Bioorg Med Chem Lett. 2011 Jan 1;21(1):288-93. | ||||
Ref 531433 | Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation. J Pharmacol Exp Ther. 2011 Jul;338(1):290-301. | ||||
Ref 531698 | A novel DP2 receptor antagonist (AM-461): a patent evaluation of WO2011085033. Expert Opin Ther Pat. 2011 Dec;21(12):1931-6. | ||||
Ref 532216 | Anti-eosinophil activity and clinical efficacy of the CRTH2 antagonist OC000459 in eosinophilic esophagitis. Allergy. 2013 Mar;68(3):375-85. | ||||
Ref 532474 | Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases. Bioorg Med Chem. 2013 Nov 1;21(21):6582-91. | ||||
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 532856 | Setipiprant, a selective CRTH2 antagonist, reduces allergen-induced airway responses in allergic asthmatics. Clin Exp Allergy. 2014 Aug;44(8):1044-52. | ||||
Ref 543776 | (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: 339). | ||||
Ref 548764 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028464) | ||||
Ref 549166 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033115) |
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