Target Information

Target General Infomation
Target ID
T72841
Former ID
TTDR00270
Target Name
Steroid hormone receptor ERR1
Gene Name
ESRRA
Synonyms
ERR-alpha; ERRalpha; Estrogen receptor-like 1; Estrogen-relatedreceptor alpha; Estrogen-relatedreceptor, alpha; ESRRA
Target Type
Clinical Trial
Disease Acne vulgaris [ICD9: 706.1; ICD10: L70.0]
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]
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.
BioChemical Class
Nuclear hormone receptor
Target Validation
T72841
UniProt ID
P11474
Sequence
MSSQVVGIEPLYIKAEPASPDSPKGSSETETEPPVALAPGPAPTRCLPGHKEEEDGEGAG
PGEQGGGKLVLSSLPKRLCLVCGDVASGYHYGVASCEACKAFFKRTIQGSIEYSCPASNE
CEITKRRRKACQACRFTKCLRVGMLKEGVRLDRVRGGRQKYKRRPEVDPLPFPGPFPAGP
LAVAGGPRKTAAPVNALVSHLLVVEPEKLYAMPDPAGPDGHLPAVATLCDLFDREIVVTI
SWAKSIPGFSSLSLSDQMSVLQSVWMEVLVLGVAQRSLPLQDELAFAEDLVLDEEGARAA
GLGELGAALLQLVRRLQALRLEREEYVLLKALALANSDSVHIEDAEAVEQLREALHEALL
EYEAGRAGPGGGAERRRAGRLLLTLPLLRQTAGKVLAHFYGVKLEGKVPMHKLFLEMLEA
MMD
Structure
1XB7; 2PJL; 3D24; 3K6P
Drugs and Mode of Action
Drug(s) Rimexolone Drug Info Approved Arthritis [1], [2]
Pregnenolone Drug Info Phase 4 Schizophrenia [3], [4]
D-5519 Drug Info Phase 3 Asthma [5]
Dexamethasone palmitate Drug Info Phase 1/2 Choroidal neovascularisation [6]
Corticosteroid Drug Info Preclinical Gastrointestinal disease [7]
Rofleponide Drug Info Discontinued in Phase 2 Allergic rhinitis [8]
RPR-106541 Drug Info Discontinued in Phase 2 Asthma [9]
AD-121 Drug Info Discontinued in Phase 1/2 Rheumatoid arthritis [10]
GW-250495 Drug Info Discontinued in Phase 1 Asthma [11]
PLD-177 Drug Info Terminated Allergic rhinitis [12]
Steroid hormone conjugates Drug Info Terminated Cachexia [13]
Inhibitor 2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-ol Drug Info [14]
4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [14]
4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [14]
4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [14]
4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [14]
7-bromo-6H-chromeno[4,3-b]quinoline-3,9-diol Drug Info [14]
7-chloro-6H-chromeno[4,3-b]quinoline-3,9-diol Drug Info [14]
7-ethyl-6H-chromeno[4,3-b]quinoline-3,9-diol Drug Info [14]
7-ethynyl-6H-chromeno[4,3-b]quinoline-3,9-diol Drug Info [14]
7-vinyl-6H-chromeno[4,3-b]quinoline-3,9-diol Drug Info [14]
Modulator AD-121 Drug Info [15]
Corticosteroid Drug Info [15]
Corticosteroids Drug Info [15]
D-5519 Drug Info [16]
ERR alpha modulators Drug Info [15]
NCX-1047 Drug Info [15]
PLD-177 Drug Info [15]
Rimexolone Drug Info [15]
Rofleponide Drug Info [17]
Steroid hormone conjugates Drug Info [18]
Agonist biochanin A Drug Info [19]
daidzein Drug Info [19]
Dexamethasone palmitate Drug Info [20]
GW-250495 Drug Info [15]
Pregnenolone Drug Info [21]
RPR-106541 Drug Info [22]
TDT-044 Drug Info [15]
Antagonist chlordane Drug Info [23]
compound 1a Drug Info [24]
toxaphene Drug Info [23]
XCT790 Drug Info [25]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
Reactome PPARA activates gene expression
Transcriptional activation of mitochondrial biogenesis
Nuclear Receptor transcription pathway
WikiPathways Mitochondrial Gene Expression
Regulation of Lipid Metabolism by Peroxisome proliferator-activated receptor alpha (PPARalpha)
Nuclear Receptors
References
REF 1ClinicalTrials.gov (NCT00471419) Phase II Study of AL-2178 (FID 109980) in the Treatment of Dry Eye. U.S. National Institutes of Health.
REF 2(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 3ClinicalTrials.gov (NCT01409096) Study Using Pregnenolone to Treat Bipolar Depression. U.S. National Institutes of Health.
REF 4(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 5ClinicalTrials.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 6Clinical pipeline report, company report or official report of Santen Pharmaceutical.
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025134)
REF 8Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007303)
REF 9Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007341)
REF 10Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015041)
REF 11Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010129)
REF 12Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020887)
REF 13Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015954)
REF 14Bioorg 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 15(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: 622).
REF 16Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007199)
REF 17Direct activation of GABAA receptors by loreclezole, an anticonvulsant drug with selectivity for the beta-subunit. Neuropharmacology. 1996;35(12):1753-60.
REF 18The 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 19Flavone and isoflavone phytoestrogens are agonists of estrogen-related receptors. Mol Cancer Res. 2003 Nov;1(13):981-91.
REF 20Dexamethasone treatment in childhood bacterial meningitis in Malawi: a randomised controlled trial. Lancet. 2002 Jul 20;360(9328):211-8.
REF 21Suppression 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 22Use 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 23Two 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 24Crystal 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 25Regulation 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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