Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00242

Target Information
NameEstrogen receptor    
Type of targetSuccessful target    
SynonymsER    
ER-alpha    
ERalpha    
Estradiol receptor    
Estrogen receptor alpha    
Oestrogen receptor    
Oestrogen receptor alpha    
DiseaseBrain injury[1]
Breast cancer
[ICD9: 174, 175   ICD10: C50]
[2][3][4][5]
Cardiovascular disease, unspecified
[ICD9: 390-459   ICD10: I00-I99]
[5]
Coronary atherosclerosis
[ICD9: 414.0, 440   ICD10: I70]
[6]
Endocrine independent cancer
[ICD9: 140-229   ICD10: C00-C96]
[2]
Neurodegenerative diseases
[ICD9: 330-337   ICD10: G30-G32]
[5]
Osteoporosis, unspecified
[ICD9: 733.0   ICD10: M80-M81]
[7]
Postmenopausal symptoms
[ICD9: 627.2   ICD10: N95.0]
[6]
Drug(s)ChlorotrianiseneApprovedMenopause[8]
ClomifeneApprovedFemale infertility[9]
Conjugated estrogens aApprovedHormone replacement therapy[10][11][12]
Conjugated estrogens bApprovedHormone replacement therapy[13][14][12]
DanazolApprovedMenorrhagia[15]
DienestrolApprovedAtrophic vaginitis[16]
DiethylstilbestrolApprovedGonorrheal vaginitis[17]
EstradiolApprovedHormone replacement therapy[18]
EstriolApprovedMultiple sclerosis[18]
EstroneApprovedMenopausal and postmenopausal disorders[18]
Ethinyl EstradiolApprovedFemale hypogonadism[19][18]
FosfestrolApprovedAnticancer[20][21][22]
FulvestrantApprovedBreast Cancer[23]
GestrinoneApprovedAntiprogestogenic[24][25][12]
LasofoxifeneApprovedOsteoporosis[26]
MestranolApprovedFirst oral contraceptives[27]
MitotaneApprovedAdrenocortical carcinoma[28][29]
QuinestrolApprovedBreast cancer and prostate cancer[30]
RaloxifeneApprovedOsteoporosis in post-menopausal women[7]
TamoxifenApprovedBreast cancer[31][32]
ToremifeneApprovedBreast Cancer[33]
OspemifenePhase IIIPost-menopausal vaginal atrophy[34]
GTx-758Phase IIFirst-line advanced prostate cancer, second-line advanced prostate cancer
Estrogen and selective estrogen receptor modulatorsPreclinicalParkinsons Disease[35]
BioChemical ClassZinc-finger    
UniProt IDP03372
Q13262
PDB Structure1A52; 1AKF; 1ERE; 1ERR; 1G50; 1GWQ; 1GWR; 1HCP; 1HCQ; 1L2I; 1PCG; 1QKT; 1QKU; 1R5K; 1SJ0; 1UOM; 1X7E; 1X7R; 1XP1; 1XP6; 1XP9; 1XPC; 1XQC; 1YIM; 1YIN; 1ZKY; 2AYR; 2B1V; 2B1Z; 2B23; 2BJ4; 2FAI; 2G44; 2G5O; 2I0J; 2IOG; 2IOK; 2JF9; 2JFA; 2LLO; 2LLQ; 2OCF; 2OUZ; 2P15; 2POG; 2Q6J; 2Q70; 2QA6; 2QA8; 2QAB; 2QE4; 2QGT; 2QGW; 2QH6; 2QR9; 2QSE; 2QXM; 2QXS; 2QZO; 2R6W; 2R6Y; 2YAT; 2YJA; 3CBM; 3CBO; 3CBP; 3DT3; 3ERD; 3ERT; 3HLV; 3HM1; 3L03; 3OS8; 3OS9; 3OSA; 3Q95; 3Q97; 3UU7; 3UUA; 3UUC; 3UUD; 4AA6; 4DMA; 4IU7; 4IUI; 4IV2; 4IV4; 4IVW; 4IVY; 4IW6; 4IW8; 4IWC; 4IWF; 4JC3; 4JDD.    
FunctionNuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues.    
SequenceMTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLL LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV
Related US Patent6,340,774
6,355,670
6,403,611
6,524,805
6,613,796
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor2,3-diphenyl-1H-indole[36]
4-Naphthalen-2-yl-phenol[37]
6-Phenyl-naphthalen-2-ol[37]
7-Phenyl-naphthalen-2-ol[37]
8-benzylnaringenin[38]
8-methylnaringenin[38]
8-n-heptylnaringenin[38]
8-n-nonylnaringenin[38]
8-n-pentylnaringenin[38]
8-n-propylnaringenin[38]
8-n-undecylnaringenin[38]
ANDROSTENEDIOL[39]
ARZOXIFENE[40]
BITHIONOL[41]
BROUSSONIN A[42]
COUMESTROL[43]
CP-394531[44]
CP-409069[44]
DIADZEIN[45]
DIHYDRORALOXIFENE[46]
EFFUSOL[47]
GSK-5182[48]
Genistein[49]
HEXESTROL[50]
ICI-164384[51]
JNJ-17148066[52]
JNJ-19398990[52]
JNJ-26529126[52]
JNJ-26529152[52]
LTERHKILHRLLQEGSPSD[53]
LY-117018[54]
MPrP[55]
NAFOXIDINE[56]
ONAPRISTONE[57]
Pipendoxifene[58]
RALOXIFENE CORE[59]
SOPHORAFLAVANONE B[38]
Tamoxifen butyl bromide[60]
Tamoxifen ethyl bromide[60]
Tamoxifen isopropyl bromide[60]
Tamoxifen methyl iodide[60]
WAY-169916[61]
ZK-119010[62]
ZK-164015[63]
AgonistDienestrol[16]
Diethylstilbestrol[17]
Estradiol[18]
Estriol[18]
Estrogen[6]
Estrone[18]
Ethinyl Estradiol[19][18]
Mestranol[27]
AntagonistDanazol[15]
EM-800[64]
Fulvestrant[23]
GW7604[65]
Tamoxifen[31][32]
Trans-hydroxytamoxifen[66]
ModulatorClomifene[9]
Estrogen and selective estrogen receptor modulators[35]
Lasofoxifene[26]
Ospemifene[34]
Quinestrol[30]
Raloxifene[7]
Toremifene[33]
BinderChlorotrianisene[8]
Mitotane[28][29]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Estrogen receptor alpha, not beta, is a critical link in estradiol-mediated protection against brain injury. Proc Natl Acad Sci U S A. 2001 Feb 13;98(4):1952-7. Epub 2001 Feb 6. To Reference
Ref 2Targeting oestrogen to kill the cancer but not the patient. Br J Cancer. 2004 Mar 8;90(5):944-9. To Reference
Ref 3Tumour necrosis factor and PI3-kinase control oestrogen receptor alpha protein level and its transrepression function. Br J Cancer. 2004 Feb 23;90(4):853-9. To Reference
Ref 4How does the estrogen receptor work? Breast Cancer Res. 2002;4(2):62-4. Epub 2002 Feb 13. To Reference
Ref 5Non-genomic steroid effects: estrogen action revisited. Ann Endocrinol (Paris). 2000 Dec;61(6):517-523. To Reference
Ref 6Estrogen-receptor polymorphisms and effects of estrogen replacement on high-density lipoprotein cholesterol in women with coronary disease. N Engl J Med. 2002 Mar 28;346(13):967-74. To Reference
Ref 7Raloxifene: risks and benefits. Ann N Y Acad Sci. 2001 Dec;949:295-303. To Reference
Ref 8Inactivation of the uterine estrogen receptor binding of estradiol during P-450 catalyzed metabolism of chlorotrianisene (TACE). Speculation that TACE antiestrogenic activity involves covalent binding to the estrogen receptor. FEBS Lett. 1990 Feb 12;261(1):59-62. To Reference
Ref 9The future of the new selective estrogen receptor modulators. Menopause Int. 2007 Mar;13(1):27-34. To Reference
Ref 10DNP 13 To Reference
Ref 1143 To Reference
Ref 12Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. To Reference
Ref 13Prous Integrity database To Reference
Ref 14326277 To Reference
Ref 15Danazol suppression of luteinizing hormone in the rat: evidence for mediation by both androgen and estrogen receptors. Proc Soc Exp Biol Med. 1990 May;194(1):54-7. To Reference
Ref 16Potential use of an estrogen-glucocorticoid receptor chimera as a drug screen for tissue selective estrogenic activity. Bone. 2009 Jan;44(1):102-12. Epub 2008 Oct 11. To Reference
Ref 17Effects of Diethylstilbestrol on Programmed Oocyte Death and Induction of Polyovular Follicles in Neonatal Mouse Ovaries. Biol Reprod. 2009 Jun 24. [Epub ahead of print] To Reference
Ref 18Reprint of Are all estrogens the same? Maturitas. 2008 Sep-Oct;61(1-2):195-201. To Reference
Ref 1917alpha-Ethinylestradiol hinders nucleotide excision repair in zebrafish liver cells. Aquat Toxicol. 2009 Jan 23. [Epub ahead of print] To Reference
Ref 2019422222 To Reference
Ref 21Carter, S. K., Bakowski, M. T., Hellman, K. Chemotherapy of Cancer, Wiley: New York, 1977, p 350 To Reference
Ref 2215953702 To Reference
Ref 23Beta3-tubulin is induced by estradiol in human breast carcinoma cells through an estrogen-receptor dependent pathway. Cell Motil Cytoskeleton. 2009 Jul;66(7):378-88. To Reference
Ref 24ARMC 22 To Reference
Ref 25321 To Reference
Ref 26Pfizer. Product Development Pipeline. March 31 2009. To Reference
Ref 27Short-term effects of environmentally relevant concentrations of EDC mixtures on Mytilus galloprovincialis digestive gland. Aquat Toxicol. 2008 May 30;87(4):272-9. Epub 2008 Mar 10. To Reference
Ref 28Mitotane for adrenocortical carcinoma treatment. Curr Opin Investig Drugs. 2005 Apr;6(4):386-94. To Reference
Ref 29Mitotane has an estrogenic effect on sex hormone-binding globulin and corticosteroid-binding globulin in humans. J Clin Endocrinol Metab. 2006 Jun;91(6):2165-70. Epub 2006 Mar 21. To Reference
Ref 30The antioxidant effect of estrogen and Selective Estrogen Receptor Modulators in the inhibition of osteocyte apoptosis in vitro. Bone. 2007 Mar;40(3):674-84. Epub 2006 Dec 13. To Reference
Ref 31Modulators of vascular sex hormone receptors and their effects in estrogen-deficiency states associated with menopause. Recent Pat Cardiovasc Drug Discov. 2008 Nov;3(3):165-86. To Reference
Ref 32Chemoprevention for high-risk women: tamoxifen and beyond. Breast J. 2001 Sep-Oct;7(5):311-20. To Reference
Ref 33Effect of selective estrogen receptor modulators on cell proliferation and estrogen receptor activities in normal human prostate stromal and epithelial cells. Prostate Cancer Prostatic Dis. 2009 May 26. [Epub ahead of print] To Reference
Ref 342011 Pipeline of Shionogi. To Reference
Ref 35Drugs used to treat Parkinson's disease, present status and future directions. CNS Neurol Disord Drug Targets. 2008 Oct;7(4):321-42. To Reference
Ref 36Bioorg Med Chem Lett. 2005 Dec 15;15(24):5562-6. Epub 2005 Oct 10.Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands. To Reference
Ref 37J Med Chem. 2005 Jun 16;48(12):3953-79.ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity. To Reference
Ref 38J Med Chem. 2006 Dec 14;49(25):7357-65.Subtle side-chain modifications of the hop phytoestrogen 8-prenylnaringenin result in distinct agonist/antagonist activity profiles for estrogen receptors alpha and beta. To Reference
Ref 39Bioorg Med Chem Lett. 2007 Nov 15;17(22):6295-8. Epub 2007 Sep 7.Androstene-3,5-dienes as ER-beta selective SERMs. To Reference
Ref 40J Med Chem. 2007 May 31;50(11):2682-92. Epub 2007 May 10.Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. To Reference
Ref 41Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). To Reference
Ref 42Bioorg Med Chem Lett. 2010 Jun 15;20(12):3764-7. Epub 2010 Apr 19.New estrogenic compounds isolated from Broussonetia kazinoki. To Reference
Ref 43J Med Chem. 2005 May 19;48(10):3463-6.Structure-based virtual screening for plant-based ERbeta-selective ligands as potential preventative therapy against age-related neurodegenerative diseases. To Reference
Ref 44J Med Chem. 2002 Jun 6;45(12):2417-24.Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists. To Reference
Ref 45J Nat Prod. 2002 Dec;65(12):1749-53.Isolation and structure elucidation of an isoflavone and a sesterterpenoic acid from Henriettella fascicularis. To Reference
Ref 46Bioorg Med Chem Lett. 1999 Apr 19;9(8):1137-40.Synthesis and biological activity of trans-2,3-dihydroraloxifene. To Reference
Ref 47Bioorg Med Chem Lett. 2006 Mar 15;16(6):1468-72. Epub 2006 Jan 18.6H-Benzo[c]chromen-6-one derivatives as selective ERbeta agonists. To Reference
Ref 48Bioorg Med Chem Lett. 2006 Feb 15;16(4):821-4. Epub 2005 Nov 22.Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma. To Reference
Ref 49Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 50Bioorg. Med. Chem. Lett. 6(9):1047-1050 (1996) To Reference
Ref 51J Med Chem. 1991 May;34(5):1624-30.Synthesis and biological activity of new halo-steroidal antiestrogens. To Reference
Ref 52J Med Chem. 2009 Dec 10;52(23):7544-69.Identification and structure-activity relationships of chromene-derived selective estrogen receptor modulators for treatment of postmenopausal symptoms. To Reference
Ref 53Bioorg Med Chem Lett. 2007 Aug 1;17(15):4118-22. Epub 2007 May 23.Bicyclo[2.2.2]octanes: close structural mimics of the nuclear receptor-binding motif of steroid receptor coactivators. To Reference
Ref 54J Med Chem. 1990 Dec;33(12):3222-9.Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans. To Reference
Ref 55Bioorg Med Chem Lett. 2009 Jan 1;19(1):108-10. Epub 2008 Nov 6.Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity. To Reference
Ref 56J Med Chem. 1998 Jul 30;41(16):2928-31.Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene. To Reference
Ref 57J Med Chem. 1996 Apr 26;39(9):1778-89.Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether. To Reference
Ref 58J Med Chem. 2001 May 24;44(11):1654-7.Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. To Reference
Ref 59Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 60Bioorg Med Chem. 2010 Aug 1;18(15):5593-601. Epub 2010 Jun 20.Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha. To Reference
Ref 61J Med Chem. 2004 Dec 16;47(26):6435-8.Synthesis and activity of substituted 4-(indazol-3-yl)phenols as pathway-selective estrogen receptor ligands useful in the treatment of rheumatoid arthritis. To Reference
Ref 62J Med Chem. 1991 Jul;34(7):2145-52.2-Phenylindole-linked [2-(aminoalkyl)pyridine]dichloroplatinum(II): complexes with a selective action on estrogen receptor positive mammary tumors. To Reference
Ref 63Bioorg Med Chem Lett. 2004 Sep 20;14(18):4659-63.Synthesis and biological evaluation of stilbene-based pure estrogen antagonists. To Reference
Ref 64EM-800, a novel antiestrogen, acts as a pure antagonist of the transcriptional functions of estrogen receptors alpha and beta. Endocrinology. 1998 Jan;139(1):111-8. To Reference
Ref 65Molecular mechanism of action at estrogen receptor alpha of a new clinically relevant antiestrogen (GW7604) related to tamoxifen. Endocrinology. 2001 Feb;142(2):838-46. To Reference
Ref 66Antagonists selective for estrogen receptor alpha. Endocrinology. 2002 Mar;143(3):941-7. To Reference



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543