Target General Infomation
Target ID
T89534
Former ID
TTDS00242
Target Name
Estrogen receptor
Gene Name
ESR1
Synonyms
ER; ER-alpha; ERalpha; Estradiol receptor; Estrogen receptor alpha; Oestrogen receptor; Oestrogen receptor alpha; ESR1
Target Type
Successful
Disease Atrophic vaginitis [ICD9: 627.3; ICD10: N95.2]
Atrophy [ICD10: M62.571]
Arthralgia [ICD10: M25.5]
Acne vulgaris [ICD9: 706.1; ICD10: L70.0]
Autoimmune diabetes [ICD10: E08-E13]
Adrenocortical carcinoma [ICD9: 194; ICD10: C74.0]
Advanced prostate cancer [ICD9: 185; ICD10: C61]
Breast cancer; Prostate cancer; Female infertility [ICD9:174, 175, 185, 628; ICD10: C50, C61, N97.0]
Brain cancer [ICD9: 191, 225.0; ICD10: C71, D33]
Breast cancer [ICD9: 174, 175; ICD10: C50]
Contraception [ICD10: Z30]
Carcinoma [ICD9: 230-234; ICD10: D00-D09]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Dysmenorrhea [ICD9: 625.3; ICD10: N94.4-N94.6]
Dyspareunia [ICD10: N94.1]
Estrogen deficiency [ICD10: E28.39]
Eye disorders [ICD10: H00-H59]
Female hypogonadism [ICD9: 253, 256; ICD10: E23, E28]
Female sexual dysfunction [ICD9: 302.7; ICD10: F52]
Female infertility due to anovulation [ICD10: N97.0]
Female infertility [ICD9: 628; ICD10: N97.0]
Gonorrheal vaginitis; Cancer [ICD9:98, 140-229; ICD10: A54, C00-C96]
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78]
Hypogonadism [ICD9: 257.2; ICD10: E23.0, E28.3, E29.1]
Hormone deficiency [ICD10: E00-E90]
Hormone replacement therapy [ICD9: V07.4; ICD10: Z79.890]
Infertility [ICD9: 628; ICD10: N97.0]
Irregularities [ICD10: N92.6]
Leukemia [ICD9: 208.9; ICD10: C90-C95]
Menorrhagia [ICD9: 627; ICD10: N92.0]
Multiple scierosis; Hormone deficiency [ICD9:340; ICD10: G35, E00-E90]
Menopausal disorder; Postmenopausal disorder [ICD9: 627; ICD10: N95]
Multiple scierosis [ICD9: 340; ICD10: G35]
Menopause symptoms [ICD10: N95.0]
Menopause symptoms; Hormone refractory prostate cancer [ICD9:140-229, 185; ICD10: N95.0, C61]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Osteopetrosis [ICD10: Q78.2]
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890]
Oral contraceptives [ICD10: Z30]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Post-menopausal vaginal atrophy [ICD9: 627.3; ICD10: N95.2]
Trematode infection [ICD10: B66.9]
Vagina disease [ICD10: N76.0]
Unspecified [ICD code not available]
Function
Nuclear 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. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA- binding transcription factors, such as AP-1/c-Jun, c-Fos, ATF-2, Sp1 and Sp3, to mediate ERE-independent signaling. Ligand binding induces a conformational change allowing subsequent or combinatorial associationwith multiprotein coactivator complexes through LXXLL motifs of their respective components. Mutual transrepression occurs between the estrogen receptor (ER) and NF- kappa-B in a cell-type specific manner. Decreases NF-kappa-B DNA- binding activity and inhibits NF-kappa-B-mediated transcription from the IL6 promoter and displace RELA/p65 and associated coregulators from the promoter. Recruited tothe NF-kappa-B response element of the CCL2 and IL8 promoters and can displace CREBBP. Present with NF-kappa-B components RELA/p65 and NFKB1/p50 on ERE sequences. Can also act synergistically with NF-kappa-B to activate transcription involving respective recruitment adjacent response elements; the function involves CREBBP. Can activate the transcriptional activity of TFF1. Also mediates membrane-initiated estrogen signaling involving various kinase cascades. Isoform 3 is involved in activation of NOS3 and endothelial nitric oxide production. Isoforms lacking one or several functional domains are thought to modulate transcriptional activity by competitive ligand or DNA binding and/or heterodimerization with the full length receptor. Essential for MTA1-mediated transcriptional regulation ofBRCA1 and BCAS3. Isoform 3 can bind to ERE and inhibit isoform 1.
BioChemical Class
Zinc-finger
Target Validation
T89534
UniProt ID
Sequence
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY
EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF
LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK
ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC
RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR
SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW
AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG
MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD
KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLL
LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV
Structure
1A52; 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; 4MG5; 4MG6; 4MG7; 4MG8; 4MG9; 4MGA; 4MGB; 4MGC; 4MGD; 4O6F; 4PP6; 4PPP; 4PPS; 1A52; 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; 4MG5; 4MG6; 4MG7; 4MG8; 4MG9; 4MGA; 4MGB; 4MGC; 4MGD; 4O6F; 4PP6; 4PPP; 4PPS
Drugs and Mode of Action
Drug(s) ARZOXIFENE Drug Info Approved Breast cancer [521695], [549961]
Bazedoxifene Drug Info Approved Osteopetrosis [524681], [542376], [551871]
Cenestin Drug Info Approved Menopause symptoms [551871]
Chlorotrianisene Drug Info Approved Menopause symptoms; Hormone refractory prostate cancer [542153], [550720], [551871]
Clomifene Drug Info Approved Female infertility [536296], [542607]
Clomiphene Citrate Drug Info Approved Female infertility due to anovulation [551871]
Conjugated estrogens a Drug Info Approved Hormone replacement therapy [551871]
Conjugated estrogens b Drug Info Approved Hormone replacement therapy [551871]
Cyclofenil Drug Info Approved Infertility [551871]
Danazol Drug Info Approved Menorrhagia [536737], [541983]
Dienestrol Drug Info Approved Atrophic vaginitis [538391], [542169], [551871]
Diethylstilbestrol Drug Info Approved Gonorrheal vaginitis; Cancer [539842], [550715], [551871]
Esterified estrogens Drug Info Approved Breast cancer [551871]
Estradiol Drug Info Approved Breast cancer [533433], [534694], [536361], [538620], [551871]
Estradiol Acetate Drug Info Approved Hormone replacement therapy [551871]
Estradiol Cypionate Drug Info Approved Hormone replacement therapy [551871]
Estradiol Valerate Drug Info Approved Hormone replacement therapy [551871]
Estratab Drug Info Approved Osteoporosis [551871]
Estriol Drug Info Approved Multiple scierosis; Hormone deficiency [539864], [550696], [551871]
Estrogen Drug Info Approved Menopause symptoms [551871]
Estrone Drug Info Approved Menopausal disorder; Postmenopausal disorder [538356], [539860]
Estropipate Drug Info Approved Hypogonadism [551871]
Ethinyl Estradiol Drug Info Approved Female hypogonadism [536361], [542077]
Fosfestrol Drug Info Approved Cancer [551871]
Fulvestrant Drug Info Approved Breast cancer [536361], [538622]
Gestrinone Drug Info Approved Breast cancer [551871]
Lasofoxifene Drug Info Approved Osteoporosis [542544], [549974]
Levormeloxifene non-steroidal Drug Info Approved Breast cancer [546694]
Mestranol Drug Info Approved Oral contraceptives [538441], [542092]
Mitotane Drug Info Approved Adrenocortical carcinoma [538481], [541993]
Nomegestrol acetate Drug Info Approved Breast cancer [526905], [533386], [551871]
Ospemifene Drug Info Approved Dyspareunia [532651], [542369]
Premarin/Trimegestone Drug Info Approved Menopause symptoms [551871]
Promestriene Drug Info Approved Acne vulgaris [551871]
Quinestrol Drug Info Approved Breast cancer; Prostate cancer; Female infertility [542103], [550697], [551871]
Raloxifene Drug Info Approved Osteoporosis [551871]
Tamoxifen Drug Info Approved Breast cancer [536863], [538623]
Toremifene Drug Info Approved Breast cancer [467663], [536361]
Raloxifene Drug Info Phase 4 Osteoporosis [523817], [539863]
Acolbifene Drug Info Phase 3 Breast cancer [523658]
NPC-01 Drug Info Phase 3 Dysmenorrhea [523263]
Ospemifene Drug Info Phase 3 Post-menopausal vaginal atrophy [542369], [551684]
Premarin/Pravachol Drug Info Phase 3 Hyperlipidaemia [535747]
Synthetic conjugated estrogen Drug Info Phase 3 Vagina disease [521865]
Trimegestone/ethinyl estradiol Drug Info Phase 3 Contraception [547436]
Afimoxifene Drug Info Phase 2 Breast cancer [521779]
Androgen restored contraceptive Drug Info Phase 2 Contraception [527054]
ARN-810 Drug Info Phase 2 Breast cancer [524250]
Danazol Drug Info Phase 2 Breast cancer [541983], [551871]
Endoxifen Drug Info Phase 2 Breast cancer [525020]
Estetrol Drug Info Phase 2 Autoimmune diabetes [522168]
Estrogen receptor beta-selective phytoestrogenic formulation Drug Info Phase 2 Menopause symptoms [531544]
GTx-758 Drug Info Phase 2 Advanced prostate cancer [523416]
ICARITIN Drug Info Phase 2 Breast cancer [524499]
RAD-1901 Drug Info Phase 2 Breast cancer [522627]
SR 16234 Drug Info Phase 2 Breast cancer [531682]
ATD transdermal gel Drug Info Phase 1 Contraception [548351]
CC-8490 Drug Info Phase 1 Brain cancer [521581]
CHF-4227 Drug Info Phase 1 Osteoporosis [547486]
BN-AA-003-NY Drug Info Preclinical Estrogen deficiency [548258]
BN-AO-014 Drug Info Preclinical Atrophy [548258]
BN-CB-045 Drug Info Preclinical Female sexual dysfunction [548258]
BN-DF-037 Drug Info Preclinical Osteoporosis [548258]
BN-GU-005-DHP Drug Info Preclinical Arthralgia [548258]
BN-OD-026 Drug Info Preclinical Cancer [548258]
BITHIONOL Drug Info Withdrawn from market Trematode infection [539482], [551871]
HEXESTROL Drug Info Withdrawn from market Irregularities [533402], [534328], [539866]
EM-800 Drug Info Discontinued in Phase 3 Estrogen deficiency [546717]
Idoxifene Drug Info Discontinued in Phase 3 Breast cancer [545487]
IoGen Drug Info Discontinued in Phase 3 Pain [546955]
Miproxifene Drug Info Discontinued in Phase 3 Cancer [544738]
Droloxifene Drug Info Discontinued in Phase 2 Breast cancer [544750]
ERA-923 Drug Info Discontinued in Phase 2 Breast cancer [546969]
NP-50301 Drug Info Discontinued in Phase 2 Eye disorders [548161]
Panomifene Drug Info Discontinued in Phase 2 Cancer [545192]
SERM-3339 Drug Info Discontinued in Phase 2 Osteoporosis [547193]
SR-90067 Drug Info Discontinued in Phase 2 Hormone deficiency [546799]
HRT Drug Info Discontinued in Phase 1 Estrogen deficiency [546947]
MX-4509 Drug Info Discontinued in Phase 1 Neurological disease [547955]
ICI-164384 Drug Info Terminated Breast cancer [544737]
LY-117018 Drug Info Terminated Discovery agent [544760]
Tamoxifen methyl iodide Drug Info Terminated Discovery agent [546052]
Zindoxifene Drug Info Terminated Breast cancer [544757]
ZK-119010 Drug Info Terminated Carcinoma [529380]
Inhibitor 1,2-Bis-(4-hydroxy-phenyl)-3H-inden-5-ol Drug Info [527738]
1,8-Dichloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
1-Bromo-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
1-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
1-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
17-METHYL-17-ALPHA-DIHYDROEQUILENIN Drug Info [551374]
2,3-diphenyl-1H-indole Drug Info [527797]
2,4-Dibenzylamino-6-isopentylpyrimidine Drug Info [529687]
2,4-diisobutylamino-6-isopentylpyrimidine Drug Info [529687]
2-(2-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
2-(3-Butoxy-4-hydroxy-phenyl)-benzooxazol-6-ol Drug Info [527232]
2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-6-ol Drug Info [527232]
2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-6-ol Drug Info [527232]
2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol Drug Info [526532]
2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-6-ol Drug Info [526532]
2-(4-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-4-methoxy-quinolin-6-ol Drug Info [527681]
2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-ol Drug Info [527681]
2-(4-Hydroxy-phenyl)-7-isopropyl-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-7-methoxy-benzofuran-5-ol Drug Info [527198]
2-(4-Hydroxy-phenyl)-7-methoxy-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-7-methyl-benzofuran-5-ol Drug Info [527198]
2-(4-Hydroxy-phenyl)-7-phenyl-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-7-propenyl-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-7-propyl-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-benzofuran-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-benzooxazol-6-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
2-(4-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol Drug Info [526532]
2-(5-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Drug Info [527232]
2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-5-ol Drug Info [527232]
2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Drug Info [527232]
2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-5-ol Drug Info [527232]
2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-6-ol Drug Info [527232]
2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE Drug Info [551374]
2-Naphthalen-1-yl-benzooxazol-6-ol Drug Info [527232]
2-phenyl-1,2'-spirobi[1H-indene]-5'-ol Drug Info [526532]
3'-Methoxy-4'Hydroxyclomiphene Drug Info [533383]
3,8-dihydroxy-4-methyl-6H-benzo[c]chromen-6-one Drug Info [527966]
3,8-dihydroxy-7-methyl-6H-benzo[c]chromen-6-one Drug Info [527966]
3-(2-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol Drug Info [527232]
3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-5-ol Drug Info [527232]
3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol Drug Info [527232]
3-(4-Hydroxyphenyl)-7-isobutoxychromen-4-one Drug Info [531066]
3-(4-Hydroxyphenyl)-7-isopropoxychromen-4-one Drug Info [531066]
3-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Drug Info [527232]
3-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Drug Info [527232]
3-CHLORO-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OL Drug Info [551374]
3-chloro-4-(4-hydroxyphenyl)salicylaldoxime Drug Info [529314]
3-ETHYL-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OL Drug Info [551374]
3-hydroxy-8,10-dimethyl-6H-benzo[c]chromen-6-one Drug Info [527966]
3-[1-ethyl-2-(3-hydroxyphenyl)butyl]phenol Drug Info [533407]
4',5,7-trihydroxy-6,8-dimethylisoflavone Drug Info [526493]
4,10-dimethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
4,6,10-trimethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
4,6,6,7-tetramethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
4,6,7,10-tetramethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
4,6,7-trimethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
4,7-dimethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
4-(1,2-Diphenyl-but-1-enyl)-phenol Drug Info [526457]
4-(1-benzyl-7-chloro-1H-indazol-3-yl)phenol Drug Info [527327]
4-(1-butyl-7-chloro-1H-indazol-3-yl)phenol Drug Info [527327]
4-(1-cyclopentyl-7-fluoro-1H-indazol-3-yl)phenol Drug Info [527327]
4-(2-phenyl-1H-benzo[d]imidazol-1-yl)phenol Drug Info [527797]
4-(2-phenyl-1H-indol-3-yl)phenol Drug Info [527797]
4-(3-(4-hydroxyphenyl)-1H-indol-2-yl)phenol Drug Info [527797]
4-(3-phenyl-1H-indol-2-yl)phenol Drug Info [527797]
4-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol Drug Info [527232]
4-(6-HYDROXY-1H-INDAZOL-3-YL)BENZENE-1,3-DIOL Drug Info [551374]
4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Drug Info [527232]
4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol Drug Info [527232]
4-(7-chloro-1-cyclohexyl-1H-indazol-3-yl)phenol Drug Info [527327]
4-(7-chloro-1-cyclopentyl-1H-indazol-3-yl)phenol Drug Info [527327]
4-(7-chloro-1-propyl-1H-indazol-3-yl)phenol Drug Info [527327]
4-(7-methyl-1-propyl-1H-indazol-3-yl)phenol Drug Info [527327]
4-Benzo[d]isoxazol-3-yl-benzene-1,3-diol Drug Info [527232]
4-benzyl-2,6-diisobutylamino-pyrimidine Drug Info [529687]
4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
4-hydroxy-N,N-diphenylbenzenesulfonamide Drug Info [527880]
4-hydroxy-N-isopropyl-N-phenylbenzenesulfonamide Drug Info [527880]
4-hydroxy-N-neopentyl-N-phenylbenzenesulfonamide Drug Info [527880]
4-hydroxy-N-phenyl-N-propylbenzenesulfonamide Drug Info [527880]
4-Naphthalen-2-yl-phenol Drug Info [527584]
4-[1,2-bis(4-hydroxyphenyl)but-1-enyl]phenol Drug Info [526589]
4-[1,2-bis(4-hydroxyphenyl)hex-1-enyl]phenol Drug Info [526589]
4-[1,2-bis(4-hydroxyphenyl)pent-1-enyl]phenol Drug Info [526589]
4-[1,2-bis(4-hydroxyphenyl)vinyl]phenol Drug Info [526589]
4-[1-(4-hydroxyphenyl)-2-phenylbut-1-enyl]phenol Drug Info [526457]
4-[1-(4-hydroxyphenyl)-2-phenylhex-1-enyl]phenol Drug Info [526457]
4-[1-(4-hydroxyphenyl)-2-phenylpent-1-enyl]phenol Drug Info [526457]
4-[1-(4-hydroxyphenyl)-2-phenylprop-1-enyl]phenol Drug Info [526457]
4-[1-(4-hydroxyphenyl)-2-phenylvinyl]phenol Drug Info [526457]
4-[2,2-bis(4-hydroxyphenyl)-1-methylvinyl]phenol Drug Info [526589]
5-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
5-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-6-ol Drug Info [527232]
5-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
5-hydroxy-2-phenylisoindoline-1,3-dione Drug Info [528481]
6-(2,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(2,6-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(2-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(2-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(3,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(3-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(3-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(3-Hydroxy-phenyl)-naphthalen-1-ol Drug Info [527584]
6-(3-Hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-2-methoxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-2-methyl-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-phenyl)-1-methoxy-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-phenyl)-1-methyl-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-phenyl)-1-nitro-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-phenyl)-1-phenyl-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-phenyl)-naphthalen-1-ol Drug Info [527584]
6-(4-Hydroxy-phenyl)-naphthalen-2-ol Drug Info [527681]
6-butyl-2,4-dipropylaminopyrimidine Drug Info [529687]
6-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
6-ethyl-2,4-diisobutylaminopyrimidine Drug Info [529687]
6-ethyl-4,7-dimethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
6-Phenyl-naphthalen-2-ol Drug Info [527584]
7-(3-Hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
7-(4-Hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
7-Allyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
7-Bromo-2-(4-hydroxy-phenyl)-benzofuran-5-ol Drug Info [527198]
7-Bromo-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
7-Butyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
7-Chloro-2-(4-hydroxy-phenyl)-benzofuran-5-ol Drug Info [527198]
7-Cyclopentyloxy-3-(4-hydroxyphenyl)chromen-4-one Drug Info [531066]
7-Ethyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
7-Ethynyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
7-Phenyl-naphthalen-2-ol Drug Info [527584]
8-(2,2-dimethylpropyl)naringenin Drug Info [528557]
8-(2-methylpropyl)naringenin Drug Info [528557]
8-(3-methylbutyl)naringenin Drug Info [528557]
8-benzylnaringenin Drug Info [528557]
8-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
8-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
8-methylnaringenin Drug Info [528557]
8-n-heptylnaringenin Drug Info [528557]
8-n-nonylnaringenin Drug Info [528557]
8-n-pentylnaringenin Drug Info [528557]
8-n-propylnaringenin Drug Info [528557]
8-n-undecylnaringenin Drug Info [528557]
ANDROSTENEDIOL Drug Info [529061]
ARZOXIFENE Drug Info [528827]
ATD transdermal gel Drug Info [543898]
BITHIONOL Drug Info [531262]
BROUSSONIN A Drug Info [530935]
Carboron Cluster with phenol Drug Info [526873]
Compound 15 Drug Info [551393]
Compound 16 Drug Info [551393]
Compound 19 Drug Info [551393]
Compound 4-D Drug Info [551393]
COUMESTROL Drug Info [527550]
CP-394531 Drug Info [526345]
CP-409069 Drug Info [526345]
DIADZEIN Drug Info [526493]
Dicarba-closo-dodecaborane derivative Drug Info [525663]
DIHYDRORALOXIFENE Drug Info [525493]
Doxorubicin-Formaldehyde Conjugate Drug Info [526966]
EFFUSOL Drug Info [527966]
ERA-923 Drug Info [528422]
Estrogen platinum(II) hybrid derivative Drug Info [527267]
Geldanamycin-estradiol hybrid Drug Info [525501]
GSK-5182 Drug Info [527895]
HEXESTROL Drug Info [551316]
ICI-164384 Drug Info [530807]
JNJ-17148066 Drug Info [530079]
JNJ-19398990 Drug Info [530079]
JNJ-26529126 Drug Info [530079]
JNJ-26529152 Drug Info [530079]
LTERHKILHRLLQEGSPSD Drug Info [528885]
LY-117018 Drug Info [531906]
MPrP Drug Info [529813]
MX-4509 Drug Info [550024]
N,N,N-Triisobutyl-pyrimidine-2,4,6-triamine Drug Info [529687]
N-allyl-4-hydroxy-N-phenylbenzenesulfonamide Drug Info [527880]
N-benzyl-4-hydroxy-N-phenylbenzenesulfonamide Drug Info [527880]
N-butyl-4-hydroxy-N-phenylbenzenesulfonamide Drug Info [527880]
N-cyclohexyl-4-hydroxy-N-phenylbenzenesulfonamide Drug Info [527880]
N-ethyl-4-hydroxy-N-phenylbenzenesulfonamide Drug Info [527880]
NAFOXIDINE Drug Info [534677]
Pipendoxifene Drug Info [526057]
SNG-163 Drug Info [543898]
SNG-8033 Drug Info [543898]
SOPHORAFLAVANONE B Drug Info [528557]
Tamoxifen butyl bromide Drug Info [531028]
Tamoxifen ethyl bromide Drug Info [531028]
Tamoxifen isopropyl bromide Drug Info [531028]
Tamoxifen methyl iodide Drug Info [531028]
WAY-169916 Drug Info [527327]
ZK-119010 Drug Info [531064]
ZK-164015 Drug Info [527179]
[1,1':2',1'']Terphenyl-4'-carbaldehyde oxime Drug Info [526711]
Modulator Acolbifene Drug Info [527443]
Afimoxifene Drug Info [543898]
ARN-810 Drug Info [533211]
Bazedoxifene Drug Info [530223], [551871]
BN-AA-003-NY Drug Info [548259]
BN-AO-014 Drug Info [548259]
BN-CB-045 Drug Info [548259]
BN-DF-037 Drug Info [548259]
BN-GU-005-DHP Drug Info [548259]
BN-OD-026 Drug Info [549739]
CC-8490 Drug Info [527343]
CHF-4227 Drug Info [526427]
Clomifene Drug Info [536404]
Clomiphene Citrate Drug Info [556264]
Conjugated estrogens a Drug Info [536361]
Conjugated estrogens b Drug Info [533439], [536361]
Cyclofenil Drug Info [528133], [551871]
Droloxifene Drug Info [533830]
Endoxifen Drug Info [543898]
Esterified estrogens Drug Info [531167], [551871]
Estetrol Drug Info [550049]
Estradiol Acetate Drug Info [556264]
Estradiol Cypionate Drug Info [556264]
Estradiol Valerate Drug Info [556264]
Estriol E3 Drug Info [531226]
Estrogen receptor beta-selective phytoestrogenic formulation Drug Info [527132]
Estropipate Drug Info [550912], [551871]
Fosfestrol Drug Info [527592], [530110]
Gestrinone Drug Info [536361]
GTx-758 Drug Info [532859]
ICARITIN Drug Info
Idoxifene Drug Info [534760]
IoGen Drug Info [543898]
Lasofoxifene Drug Info [549974]
Levormeloxifene non-steroidal Drug Info [526082], [551871]
Miproxifene Drug Info [525689]
Nomegestrol acetate Drug Info [526905], [533386], [551871]
NP-50301 Drug Info [529539]
NPC-01 Drug Info [523263]
Org-37663 Drug Info
Ospemifene Drug Info [551684]
Panomifene Drug Info [534524]
Premarin/Pravachol Drug Info [535747]
Premarin/Trimegestone Drug Info [544138], [551871]
Promestriene Drug Info [532496], [551871]
Quinestrol Drug Info [536324]
RAD-1901 Drug Info [533286]
Raloxifene Drug Info [543898]
RG6046 Drug Info [551871]
Selective estrogen receptor degraders Drug Info [543898]
SERM-3339 Drug Info [550861]
SERMs Drug Info [543898]
SR 16234 Drug Info [550429]
STX Drug Info [543898]
Synthetic conjugated estrogen Drug Info [526949], [551871]
Toremifene Drug Info [537376]
Trimegestone/ethinyl estradiol Drug Info [527538]
TSERaM Drug Info [543898]
Zindoxifene Drug Info [544032]
Agonist Androgen restored contraceptive Drug Info [543898]
Cenestin Drug Info [526290], [551871]
Dienestrol Drug Info [536915]
Diethylstilbestrol Drug Info [537525]
Estradiol Drug Info [537310]
Estratab Drug Info [534591], [551871]
Estriol Drug Info [537310]
Estrogen Drug Info [535417]
Estrone Drug Info [537310]
Ethinyl Estradiol Drug Info [537099], [537310]
HRT Drug Info [551907]
Mestranol Drug Info [536671]
propylpyrazoletriol Drug Info [525879]
R,R-THC Drug Info [534824]
SR-90067 Drug Info [551906]
Binder Chlorotrianisene Drug Info [537673]
Mitotane Drug Info [536081], [536207]
Antagonist Danazol Drug Info [537674]
EM-800 Drug Info [538072]
Fulvestrant Drug Info [537373]
GW7604 Drug Info [535101]
methyl-piperidino-pyrazole Drug Info [535376]
SNG-8006 Drug Info [543898]
Tamoxifen Drug Info [535410], [536925]
Trans-hydroxytamoxifen Drug Info [535376]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
DRM DRM Info
Pathways
KEGG Pathway Estrogen signaling pathway
Prolactin signaling pathway
Thyroid hormone signaling pathway
Endocrine and other factor-regulated calcium reabsorption
Proteoglycans in cancer
NetPath Pathway FSH Signaling Pathway
EGFR1 Signaling Pathway
RANKL Signaling Pathway
Pathway Interaction Database Regulation of nuclear SMAD2/3 signaling
Signaling events mediated by HDAC Class II
Plasma membrane estrogen receptor signaling
LKB1 signaling events
Regulation of Telomerase
ATF-2 transcription factor network
AP-1 transcription factor network
FOXM1 transcription factor network
Validated nuclear estrogen receptor alpha network
Signaling mediated by p38-alpha and p38-beta
FOXA1 transcription factor network
Reactome Nuclear signaling by ERBB4
Nuclear Receptor transcription pathway
WikiPathways Estrogen signaling pathway
Nuclear Receptors Meta-Pathway
Estrogen Receptor Pathway
Signaling by ERBB4
JAK/STAT
Integrated Pancreatic Cancer Pathway
Leptin signaling pathway
miR-targeted genes in muscle cell - TarBase
Integrated Breast Cancer Pathway
Nuclear Receptors
References
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Ref 525689Estrogen agonistic/antagonistic effects of miproxifene phosphate (TAT-59)Shibata J1, Toko T, Saito H, Lykkesfeldt AE, Fujioka A, Sato K, Hashimoto A, Wierzba K, Yamada Y.Author information1Hanno Research Center, Taiho Pharmaceutical Co., Ltd., 1-27 Misugidai, Hanno-City, Saitama, 357-8527, Japan.Erratum inCancer Chemother Pharmacol 2000;46(2):172. AbstractPURPOSE: We evaluated miproxifene phosphate (TAT-59) to elucidate its efficacy in antiestrogen therapy for breast cancer patients and to assess its tissue-selective estrogenic/antiestrogenic activity.METHODS: Using DP-TAT-59, a major and active metabolite of TAT-59, an in vitro cell growth inhibition test was performed. Antitumor activity was determined using TAT-59 against human tumor xenografts of the MCF-7 and the Br-10 cell lines andMCF-7-derived tamoxifen-resistant cell lines, R-27 and FST-1. The antitumor activity of DP-TAT-59 and DM-DP-TAT-59, major metabolites of TAT-59 found in human blood following a TAT-59 dose, was also examined after intravenous administration to experimental animals. The residual estrogenic activity of TAT-59, evaluated in terms of bone and lipid metabolism in ovariectomized rats, was then comparedwith that of tamoxifen.RESULTS: DP-TAT-59 significantly inhibited the proliferation of estrogen receptor-positive MCF-7 and T-47D tumor cells in the presence of 1 nM estradiol. TAT-59, given to mice bearing MCF-7 or Br-10 xenografts, at the dose level of 5 mg/kg, exerted a significant growth inhibitory effect that was stronger than that of tamoxifen. Moreover, R-27 and FST-1 tumors, which show a resistance to tamoxifen, responded strongly to TAT-59, suggesting that TAT-59 might be effective against tumors resistant to tamoxifen. The metabolites of TAT-59, DP-TAT-59 and DM-DP-TAT-59, showed similar antitumor activity. Both TAT-59 and tamoxifen suppressed the decrease in bone density and reduced the blood cholesterol levels in ovariectomized rats, suggesting that the estrogenic activity of TAT-59 is comparable to that of tamoxifen.CONCLUSIONS: On the basis of the above results, one may expect TAT-59 to become an effective drug in patients with tumors less sensitive to tamoxifen, while its estrogenic activity as determined by bone and lipid metabolism is similar to that of tamoxifen.PMID: 10663628 [PubMed - indexed for MEDLINE] ShareMeSH Terms, SubstancesMeSH TermsAnimalsAntineoplastic Agents, Hormonal/pharmacologyBreast Neoplasms/pathology*Cell Division/drug effectsDrug Screening Assays, AntitumorEstradiol/pharmacologyEstrogen Antagonists/pharmacology*FemaleHumansLipid MetabolismMiceMice, Inbred BALB CRatsRats, Sprague-DawleyReceptors, Estrogen/physiologyTamoxifen/analogs & derivatives*Tamoxifen/pharmacologyTransplantation, HeterologousTumor Cells, Cultured/drug effectsSubstancesAntineoplastic Agents, HormonalEstrogen AntagonistsReceptors, EstrogenTamoxifenTAT 59EstradiolLinkOut - more resourcesOther Literature SourcesAccess more work from the authors - ResearchGateMedicalBreast Cancer - MedlinePlus Health InformationMiscellaneousESTRADIOL - Hazardous Substances Data BankTAMOXIFEN - Hazardous Substances Data BankPubMed Commons home Cancer Chemother Pharmacol. 2000;45(2):133-41.
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