Target Information
Target General Infomation | |||||
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Target ID |
T72841
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Former ID |
TTDR00270
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Target Name |
Steroid hormone receptor ERR1
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Gene Name |
ESRRA
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Synonyms |
ERR-alpha; ERRalpha; Estrogen receptor-like 1; Estrogen-relatedreceptor alpha; Estrogen-relatedreceptor, alpha; ESRRA
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Target Type |
Clinical Trial
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Disease | Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4] | ||||
Arthritis [ICD9: 710-719; ICD10: M00-M25] | |||||
Asthma [ICD10: J45] | |||||
Acne vulgaris [ICD9: 706.1; ICD10: L70.0] | |||||
Cachexia [ICD9: 799.4; ICD10: R64] | |||||
Choroidal neovascularisation [ICD10: H35] | |||||
Dermatitis [ICD9: 692.9; ICD10: L20-L30] | |||||
Dermatological disease [ICD10: L00-L99] | |||||
Gastrointestinal disease [ICD10: K00-K93] | |||||
Non-insulin dependent diabetes [ICD10: E11.9] | |||||
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06] | |||||
Schizophrenia [ICD9: 295; ICD10: F20] | |||||
Function |
Binds to an ERR-alpha response element (ERRE) containing a single consensus half-site, 5'-TNAAGGTCA-3'. Can bind to the medium-chain acyl coenzyme A dehydrogenase (MCAD) response element NRRE-1 and may act as an important regulator of MCAD promoter. Binds to the C1 region of the lactoferrin gene promoter. Requires dimerization and the coactivator, PGC-1A, for full activity. The ERRalpha/PGC1alpha complex is a regulator of energy metabolism. Induces the expression of PERM1 in the skeletal muscle.
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BioChemical Class |
Nuclear hormone receptor
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Target Validation |
T72841
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UniProt ID | |||||
Sequence |
MSSQVVGIEPLYIKAEPASPDSPKGSSETETEPPVALAPGPAPTRCLPGHKEEEDGEGAG
PGEQGGGKLVLSSLPKRLCLVCGDVASGYHYGVASCEACKAFFKRTIQGSIEYSCPASNE CEITKRRRKACQACRFTKCLRVGMLKEGVRLDRVRGGRQKYKRRPEVDPLPFPGPFPAGP LAVAGGPRKTAAPVNALVSHLLVVEPEKLYAMPDPAGPDGHLPAVATLCDLFDREIVVTI SWAKSIPGFSSLSLSDQMSVLQSVWMEVLVLGVAQRSLPLQDELAFAEDLVLDEEGARAA GLGELGAALLQLVRRLQALRLEREEYVLLKALALANSDSVHIEDAEAVEQLREALHEALL EYEAGRAGPGGGAERRRAGRLLLTLPLLRQTAGKVLAHFYGVKLEGKVPMHKLFLEMLEA MMD |
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Structure |
1XB7; 2PJL; 3D24; 3K6P
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Drugs and Mode of Action | |||||
Drug(s) | Rimexolone | Drug Info | Approved | Arthritis | [522023], [542105] |
Pregnenolone | Drug Info | Phase 4 | Schizophrenia | [523578], [539512] | |
D-5519 | Drug Info | Phase 3 | Asthma | [524960] | |
Dexamethasone palmitate | Drug Info | Phase 1/2 | Choroidal neovascularisation | [551624] | |
Corticosteroid | Drug Info | Preclinical | Gastrointestinal disease | [548383] | |
Rofleponide | Drug Info | Discontinued in Phase 2 | Allergic rhinitis | [546294] | |
RPR-106541 | Drug Info | Discontinued in Phase 2 | Asthma | [546303] | |
AD-121 | Drug Info | Discontinued in Phase 1/2 | Rheumatoid arthritis | [547307] | |
GW-250495 | Drug Info | Discontinued in Phase 1 | Asthma | [546754] | |
PLD-177 | Drug Info | Terminated | Allergic rhinitis | [547980] | |
Steroid hormone conjugates | Drug Info | Terminated | Cachexia | [547402] | |
Inhibitor | 2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-ol | Drug Info | [528822] | ||
4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [528822] | |||
4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [528822] | |||
4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [528822] | |||
4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [528822] | |||
7-bromo-6H-chromeno[4,3-b]quinoline-3,9-diol | Drug Info | [528822] | |||
7-chloro-6H-chromeno[4,3-b]quinoline-3,9-diol | Drug Info | [528822] | |||
7-ethyl-6H-chromeno[4,3-b]quinoline-3,9-diol | Drug Info | [528822] | |||
7-ethynyl-6H-chromeno[4,3-b]quinoline-3,9-diol | Drug Info | [528822] | |||
7-vinyl-6H-chromeno[4,3-b]quinoline-3,9-diol | Drug Info | [528822] | |||
Modulator | AD-121 | Drug Info | [543900] | ||
Corticosteroid | Drug Info | [543900] | |||
Corticosteroids | Drug Info | [543900] | |||
D-5519 | Drug Info | [546275] | |||
ERR alpha modulators | Drug Info | [543900] | |||
NCX-1047 | Drug Info | [543900] | |||
PLD-177 | Drug Info | [543900] | |||
Rimexolone | Drug Info | [543900] | |||
Rofleponide | Drug Info | [534346] | |||
Steroid hormone conjugates | Drug Info | [534809] | |||
Agonist | biochanin A | Drug Info | [526891] | ||
daidzein | Drug Info | [526891] | |||
Dexamethasone palmitate | Drug Info | [526384] | |||
GW-250495 | Drug Info | [543900] | |||
Pregnenolone | Drug Info | [528119] | |||
RPR-106541 | Drug Info | [525541] | |||
TDT-044 | Drug Info | [543900] | |||
Antagonist | chlordane | Drug Info | [525591] | ||
compound 1a | Drug Info | [528883] | |||
toxaphene | Drug Info | [525591] | |||
XCT790 | Drug Info | [535978] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
References | |||||
Ref 522023 | ClinicalTrials.gov (NCT00471419) Phase II Study of AL-2178 (FID 109980) in the Treatment of Dry Eye. U.S. National Institutes of Health. | ||||
Ref 523578 | ClinicalTrials.gov (NCT01409096) Study Using Pregnenolone to Treat Bipolar Depression. U.S. National Institutes of Health. | ||||
Ref 524960 | ClinicalTrials.gov (NCT02270450) S1316, Surgery or Non-Surgical Management in Treating Patients With Intra-Abdominal Cancer and Bowel Obstruction. U.S. National Institutes of Health. | ||||
Ref 539512 | (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: 2376). | ||||
Ref 542105 | (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: 7099). | ||||
Ref 546294 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007303) | ||||
Ref 546303 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007341) | ||||
Ref 546754 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010129) | ||||
Ref 547307 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015041) | ||||
Ref 547402 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015954) | ||||
Ref 547980 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020887) | ||||
Ref 525541 | Use of the steroid derivative RPR 106541 in combination with site-directed mutagenesis for enhanced cytochrome P-450 3A4 structure/function analysis. J Pharmacol Exp Ther. 1999 Aug;290(2):594-602. | ||||
Ref 525591 | Two organochlorine pesticides, toxaphene and chlordane, are antagonists for estrogen-related receptor alpha-1 orphan receptor. Cancer Res. 1999 Sep 15;59(18):4519-24. | ||||
Ref 526384 | Dexamethasone treatment in childhood bacterial meningitis in Malawi: a randomised controlled trial. Lancet. 2002 Jul 20;360(9328):211-8. | ||||
Ref 526891 | Flavone and isoflavone phytoestrogens are agonists of estrogen-related receptors. Mol Cancer Res. 2003 Nov;1(13):981-91. | ||||
Ref 528119 | Suppression of adrenal function by low-dose prednisone: assessment with 24-hour urinary steroid hormone profiles--a review of five cases. Altern Med Rev. 2006 Mar;11(1):40-6. | ||||
Ref 528822 | Bioorg Med Chem Lett. 2007 Jul 15;17(14):4053-6. Epub 2007 May 4.ERbeta ligands. Part 6: 6H-Chromeno[4,3-b]quinolines as a new series of estrogen receptor beta-selective ligands. | ||||
Ref 528883 | Crystal structure of human estrogen-related receptor alpha in complex with a synthetic inverse agonist reveals its novel molecular mechanism. J Biol Chem. 2007 Aug 10;282(32):23231-9. Epub 2007 Jun 6. | ||||
Ref 534346 | Direct activation of GABAA receptors by loreclezole, an anticonvulsant drug with selectivity for the beta-subunit. Neuropharmacology. 1996;35(12):1753-60. | ||||
Ref 534809 | The effect of six months treatment with a 100 mg daily dose of dehydroepiandrosterone (DHEA) on circulating sex steroids, body composition and muscle strength in age-advanced men and women. Clin Endocrinol (Oxf). 1998 Oct;49(4):421-32. | ||||
Ref 535978 | Regulation of PPARgamma coactivator 1alpha (PGC-1alpha) signaling by an estrogen-related receptor alpha (ERRalpha) ligand. Proc Natl Acad Sci U S A. 2004 Jun 15;101(24):8912-7. Epub 2004 Jun 7. |
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