Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00250

Target Information
NameEstrogen receptor beta    
Type of targetSuccessful target    
SynonymsBeta-1    
ER-beta    
Erbeta    
Oestrogen receptor beta    
DiseaseBreast cancer
[ICD9: 174, 175   ICD10: C50]
[1][2]
Cardiovascular disease, unspecified
[ICD9: 390-459   ICD10: I00-I99]
[2]
ER beta-positive prostate tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[3]
Neurodegenerative diseases
[ICD9: 330-337   ICD10: G30-G32]
[2]
Vascular injury response[4]
Drug(s)Conjugated EstrogensApprovedVasomotor symptoms[5][6]
BioChemical ClassZinc-finger    
UniProt IDQ92731
PDB Structure1L2J; 1NDE; 1QKM; 1U3Q; 1U3R; 1U3S; 1U9E; 1X76; 1X78; 1X7B; 1X7J; 1YY4; 1YYE; 1ZAF; 2FSZ; 2GIU; 2I0G; 2JJ3; 2NV7; 2QTU; 2YJD; 2YLY; 2Z4B; 3OLL; 3OLS; 3OMO; 3OMP; 3OMQ; 4J24; 4J26.    
FunctionNuclear hormone receptor. binds estrogens with an affinity similar to that of esr1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability.    
SequenceMDIKNSPSSLNSPSSYNCSQSILPLEHGSIYIPSSYVDSHHEYPAMTFYSPAVMNYSIPS NVTNLEGGPGRQTTSPNVLWPTPGHLSPLVVHRQLSHLYAEPQKSPWCEARSLEHTLPVN RETLKRKVSGNRCASPVTGPGSKRDAHFCAVCSDYASGYHYGVWSCEGCKAFFKRSIQGH NDYICPATNQCTIDKNRRKSCQACRLRKCYEVGMVKCGSRRERCGYRLVRRQRSADEQLH CAGKAKRSGGHAPRVRELLLDALSPEQLVLTLLEAEPPHVLISRPSAPFTEASMMMSLTK LADKELVHMISWAKKIPGFVELSLFDQVRLLESCWMEVLMMGLMWRSIDHPGKLIFAPDL VLDRDEGKCVEGILEIFDMLLATTSRFRELKLQHKEYLCVKAMILLNSSMYPLVTATQDA DSSRKLAHLLNAVTDALVWVIAKSGISSQQQSMRLANLLMLLSHVRHASNKGMEHLLNMK CKNVVPVYDLLLEMLNAHVLRGCKSSITGSECSPAEDSKSKEGSQNPQSQ
Related US Patent6,355,670
6,403,611
6,613,796
6,630,508
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor1-CHLORO-6- (4-HYDROXYPHENYL)-2-NAPHTHOL[7]
2- (3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol[8]
2- (3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-6-ol[8]
2- (4-HYDROXY-PHENYL)BENZOFURAN-5-OL[7]
2- (4-Hydroxy-phenyl)-quinolin-6-ol[9]
2- (4-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol[8]
2-phenyl-1,2'-spirobi[1H-indene]-5'-ol[8]
2-phenyl-1,2'-spirobi[1H-indene]-5-ol[8]
3'-Methoxy-4'Hydroxyclomiphene[10]
3- (4-Hydroxy-phenyl)-4H-chromen-7-ol[11]
4- (4-HYDROXYPHENYL)-1-NAPHTHALDEHYDE OXIME[7]
4-HYDROXYTAMOXIFEN[12]
ANDROSTENEDIOL[13]
ARZOXIFENE[14]
Acetate Ion[15]
BITHIONOL[16]
BROUSSONIN A[17]
COUMESTROL[11]
CP-394531[18]
CP-409069[18]
DIADZEIN[19]
DIHYDRORALOXIFENE[20]
Doxorubicin-Formaldehyde Conjugate[21]
EFFUSOL[22]
Estrogen platinum (II) hybrid derivative[23]
Estrogen platinum (II) hybrid derivative[23]
Estrogen platinum (II) hybrid derivative[23]
Estrogen platinum (II) hybrid derivative[23]
Estrogen platinum (II) hybrid derivative[23]
Estrogen platinum (II) hybrid derivative[23]
Estrogen platinum (II) hybrid derivative[23]
Estrogen platinum (II) hybrid derivative[23]
GNF-PF-3037[16]
Genistein[15]
HEXESTROL[24]
ICI-164384[25]
LY-117018[26]
MORIN[16]
NAFOXIDINE[27]
NARINGENIN[28]
ONAPRISTONE[29]
Para-Mercury-Benzenesulfonic Acid[15]
Pipendoxifene[30]
SOPHORAFLAVANONE B[28]
THIOGENISTEIN[31]
TUPICHINOL C[17]
WAY-169916[32]
ZK-119010[33]
ZK-164015[34]
geldanamycin-estradiol hybrid[35]
geldanamycin-estradiol hybrid[35]
AgonistEstrogen[4]
Estrogen receptor B agonist[36]
AntagonistConjugated Estrogens[5][6]
EM-800[37]
Premarin[5][6]
Trans-hydroxytamoxifen[38]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Estrogen receptor beta in breast cancer. Endocr Relat Cancer. 2002 Mar;9(1):1-13. To Reference
Ref 2Non-genomic steroid effects: estrogen action revisited. Ann Endocrinol (Paris). 2000 Dec;61(6):517-523. To Reference
Ref 3Oestrogen receptor beta is required for androgen-stimulated proliferation of LNCaP prostate cancer cells. J Mol Endocrinol. 2004 Jun;32(3):777-91. To Reference
Ref 4Estrogen inhibits the vascular injury response in estrogen receptor beta-deficient female mice. Proc Natl Acad Sci U S A. 1999 Dec 21;96(26):15133-6. To Reference
Ref 5Differential biochemical and cellular actions of Premarin estrogens: distinct pharmacology of bazedoxifene-conjugated estrogens combination. Mol Endocrinol. 2009 Jan;23(1):74-85. Epub 2008 Nov 26. To Reference
Ref 6Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 7Berman 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 8Bioorg Med Chem Lett. 2003 Feb 10;13(3):479-83.2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs). To Reference
Ref 9Bioorg Med Chem Lett. 2005 Oct 15;15(20):4520-5.ERbeta ligands. Part 4: Synthesis and structure-activity relationships of a series of 2-phenylquinoline derivatives. To Reference
Ref 10J Med Chem. 1989 Jan;32(1):192-7.Phenolic metabolites of clomiphene: [(E,Z)-2-[4-(1,2-diphenyl-2-chlorovinyl)phenoxy]ethyl]diethylamine. Preparation, electrophilicity, and effects in MCF 7 breast cancer cells. To Reference
Ref 11J 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 12Bioorg Med Chem. 2008 Nov 1;16(21):9554-73. Epub 2008 Sep 16.Synthesis, biological evaluation, structural-activity relationship, and docking study for a series of benzoxepin-derived estrogen receptor modulators. To Reference
Ref 13Bioorg 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 14J 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 15Overington 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 16Bioorg 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 17Bioorg Med Chem Lett. 2010 Jun 15;20(12):3764-7. Epub 2010 Apr 19.New estrogenic compounds isolated from Broussonetia kazinoki. To Reference
Ref 18J Med Chem. 2002 Jun 6;45(12):2417-24.Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists. To Reference
Ref 19J 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 20Bioorg Med Chem Lett. 1999 Apr 19;9(8):1137-40.Synthesis and biological activity of trans-2,3-dihydroraloxifene. To Reference
Ref 21J Med Chem. 2004 Feb 26;47(5):1193-206.Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells. To Reference
Ref 22Bioorg 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 23Bioorg Med Chem Lett. 2004 Dec 6;14(23):5919-24.Biological evaluation of novel estrogen-platinum(II) hybrid molecules on uterine and ovarian cancers-molecular modeling studies. To Reference
Ref 24Bioorg. Med. Chem. Lett. 6(9):1047-1050 (1996) To Reference
Ref 25J Med Chem. 1991 May;34(5):1624-30.Synthesis and biological activity of new halo-steroidal antiestrogens. To Reference
Ref 26J 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 27J 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 28J 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 29J 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 30J Med Chem. 2001 May 24;44(11):1654-7.Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. To Reference
Ref 31J Med Chem. 2006 Apr 20;49(8):2440-55.Synthesis and characterization of 3-arylquinazolinone and 3-arylquinazolinethione derivatives as selective estrogen receptor beta modulators. To Reference
Ref 32J 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 33J 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 34Bioorg Med Chem Lett. 2004 Sep 20;14(18):4659-63.Synthesis and biological evaluation of stilbene-based pure estrogen antagonists. To Reference
Ref 35Bioorg Med Chem Lett. 1999 May 3;9(9):1233-8.Synthesis and evaluation of geldanamycin-estradiol hybrids. To Reference
Ref 36Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22. To Reference
Ref 37EM-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 38Antagonists selective for estrogen receptor alpha. Endocrinology. 2002 Mar;143(3):941-7. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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