Target Information
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 | Advanced prostate cancer [ICD9: 185; ICD10: C61] | ||||
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] | |||||
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] | |||||
Carcinoma [ICD9: 230-234; ICD10: D00-D09] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Contraception [ICD10: Z30] | |||||
Dysmenorrhea [ICD9: 625.3; ICD10: N94.4-N94.6] | |||||
Dyspareunia [ICD10: N94.1] | |||||
Estrogen deficiency [ICD10: E28.39] | |||||
Eye disorders [ICD10: H00-H59] | |||||
Female infertility due to anovulation [ICD10: N97.0] | |||||
Female infertility [ICD9: 628; ICD10: N97.0] | |||||
Female hypogonadism [ICD9: 253, 256; ICD10: E23, E28] | |||||
Female sexual dysfunction [ICD9: 302.7; ICD10: F52] | |||||
Gonorrheal vaginitis; Cancer [ICD9:98, 140-229; ICD10: A54, C00-C96] | |||||
Hormone replacement therapy [ICD9: V07.4; ICD10: Z79.890] | |||||
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78] | |||||
Hypogonadism [ICD9: 257.2; ICD10: E23.0, E28.3, E29.1] | |||||
Hormone deficiency [ICD10: E00-E90] | |||||
Irregularities [ICD10: N92.6] | |||||
Infertility [ICD9: 628; ICD10: N97.0] | |||||
Leukemia [ICD9: 208.9; ICD10: C90-C95] | |||||
Menopause symptoms; Hormone refractory prostate cancer [ICD9:140-229, 185; ICD10: N95.0, C61] | |||||
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] | |||||
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89] | |||||
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890] | |||||
Oral contraceptives [ICD10: Z30] | |||||
Osteopetrosis [ICD10: Q78.2] | |||||
Post-menopausal vaginal atrophy [ICD9: 627.3; ICD10: N95.2] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
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) | |||||
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 | |||||
Ref 467663 | (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: 4325). | ||||
Ref 521581 | ClinicalTrials.gov (NCT00074646) Phase I Trial of CC-8490 for the Treatment of Subjects With Recurrent/Refractory High-Grade Gliomas. U.S. National Institutes of Health. | ||||
Ref 521695 | ClinicalTrials.gov (NCT00190697) A Study of LY353381 (Arzoxifene) for Patients Who Benefitted From This Drug in Other Oncology Trials and Wished to Continue Treatment. U.S. National Institutes of Health. | ||||
Ref 521779 | ClinicalTrials.gov (NCT00272714) Study of Afimoxifene Gel to Treat Cyclic Mastalgia in Premenopausal Women. U.S. National Institutes of Health. | ||||
Ref 521865 | ClinicalTrials.gov (NCT00361569) A Clinical Trial to Evaluate the Safety and Efficacy of DR-2041(Synthetic Conjugated Estrogens, A) for Treatment of Vulvovaginal Atrophy. U.S. National Institutes of Health. | ||||
Ref 522168 | ClinicalTrials.gov (NCT00563472) Feasibility Study Into the Contraceptive Effect of Estetrol. U.S. National Institutes of Health. | ||||
Ref 522627 | ClinicalTrials.gov (NCT00875420) A Study to Evaluate the Effects of RAD1901 in the Treatment of Vasomotor Symptoms in Postmenopausal Women. U.S. National Institutes of Health. | ||||
Ref 523263 | ClinicalTrials.gov (NCT01246791) Pharmacokinetics of NPC-01 After Single Oral Administration in Healthy Female Volunteers. U.S. National Institutes of Health. | ||||
Ref 523416 | ClinicalTrials.gov (NCT01326312) Effect of GTx-758 on Total and Free Testosterone Levels in Men With Prostate Cancer. U.S. National Institutes of Health. | ||||
Ref 523658 | ClinicalTrials.gov (NCT01452373) Dehydroepiandrosterone (DHEA) + Acolbifene Against Vasomotor Symptoms (Hot Flushes) in Postmenopausal Women. U.S. National Institutes of Health. | ||||
Ref 523817 | ClinicalTrials.gov (NCT01544894) Clinical Study of Raloxifene and Strontium Ranelate in Postmenopausal Osteoporosis. U.S. National Institutes of Health. | ||||
Ref 524250 | ClinicalTrials.gov (NCT01823835) A Study of ARN-810 (GDC-0810) in Postmenopausal Women With Locally Advanced or Metastatic Estrogen Receptor Positive Breast Cancer. U.S. National Institutes of Health. | ||||
Ref 524499 | ClinicalTrials.gov (NCT01972672) The Phase II Study of Icaritin in Patients With Advanced Hepatocellular Carcinoma. U.S. National Institutes of Health. | ||||
Ref 524681 | ClinicalTrials.gov (NCT02090400) Switching From Oral Bisphosphonates to Bazedoxifene to Evaluate Effects on Bone Mineral Density in Postmenopausal Women. U.S. National Institutes of Health. | ||||
Ref 525020 | ClinicalTrials.gov (NCT02311933) Tamoxifen Citrate or Z-Endoxifen Hydrochloride in Treating Patients With Locally Advanced or Metastatic, Estrogen Receptor-Positive, HER2-Negative Breast Cancer. U.S.National Institutes of Health. | ||||
Ref 526905 | An overview of nomegestrol acetate selective receptor binding and lack of estrogenic action on hormone-dependent cancer cells. J Steroid Biochem Mol Biol. 2003 Nov;87(2-3):111-22. | ||||
Ref 527054 | Treatment outcome in endodontics-the Toronto Study. Phase II: initial treatment. J Endod. 2004 May;30(5):302-9. | ||||
Ref 529380 | Pharmacological characterization of a novel oestrogen antagonist, ZK 119010, in rats and mice. J Endocrinol. 1991 Sep;130(3):409-14. | ||||
Ref 531544 | Estrogen receptor beta-selective phytoestrogenic formulation prevents physical and neurological changes in a preclinical model of human menopause. Menopause. 2011 Oct;18(10):1131-42. | ||||
Ref 531682 | Randomized double-blind phase 2 trial of 3 doses of TAS-108 in patients with advanced or metastatic postmenopausal breast cancer. Cancer. 2012 Jul 1;118(13):3244-53. | ||||
Ref 533386 | Regulation of rat uterine steroid receptors by nomegestrol acetate, a new 19-nor-progesterone derivative. J Pharmacol Exp Ther. 1989 Feb;248(2):758-61. | ||||
Ref 533402 | Carcinogenicity and metabolic activation of hexestrol. Chem Biol Interact. 1985 Oct;55(1-2):157-76. | ||||
Ref 533433 | Regulation of the estrogen receptor in MCF-7 cells by estradiol. Mol Endocrinol. 1988 Dec;2(12):1157-62. | ||||
Ref 534328 | Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta. Endocrinology. 1997 Mar;138(3):863-70. | ||||
Ref 534694 | Estradiol regulates estrogen receptor mRNA stability. J Steroid Biochem Mol Biol. 1998 Aug;66(3):113-20. | ||||
Ref 535747 | Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 536737 | Emerging drugs for idiopathic thrombocytopenic purpura in adults. Expert Opin Emerg Drugs. 2008 Jun;13(2):237-54. | ||||
Ref 536863 | Rational management of endocrine resistance in breast cancer: a comprehensive review of estrogen receptor biology, treatment options, and future directions. Cancer. 2008 Nov 1;113(9):2385-97. | ||||
Ref 538356 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 085239. | ||||
Ref 538391 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 006110. | ||||
Ref 538441 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010976. | ||||
Ref 538481 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 016885. | ||||
Ref 538620 | (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: 1013). | ||||
Ref 538622 | (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: 1015). | ||||
Ref 538623 | (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: 1016). | ||||
Ref 539482 | (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: 2338). | ||||
Ref 539842 | (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: 2801). | ||||
Ref 539860 | (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: 2818). | ||||
Ref 539863 | (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: 2820). | ||||
Ref 539864 | (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: 2821). | ||||
Ref 539866 | (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: 2823). | ||||
Ref 541983 | (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: 6942). | ||||
Ref 541993 | (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: 6957). | ||||
Ref 542077 | (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: 7071). | ||||
Ref 542092 | (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: 7087). | ||||
Ref 542103 | (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: 7097). | ||||
Ref 542153 | (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: 7146). | ||||
Ref 542169 | (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: 7160). | ||||
Ref 542369 | (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: 7349). | ||||
Ref 542376 | (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: 7355). | ||||
Ref 542544 | (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: 7542). | ||||
Ref 542607 | (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: 7619). | ||||
Ref 544737 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000792) | ||||
Ref 544738 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000796) | ||||
Ref 544750 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000847) | ||||
Ref 544757 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000885) | ||||
Ref 544760 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000893) | ||||
Ref 545192 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002425) | ||||
Ref 545487 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003448) | ||||
Ref 546052 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006065) | ||||
Ref 546694 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009670) | ||||
Ref 546717 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009862) | ||||
Ref 546799 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010354) | ||||
Ref 546947 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011425) | ||||
Ref 546955 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011554) | ||||
Ref 546969 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011640) | ||||
Ref 547193 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013842) | ||||
Ref 547436 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016303) | ||||
Ref 547486 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016760) | ||||
Ref 547955 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020680) | ||||
Ref 548161 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022636) | ||||
Ref 548258 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023897) | ||||
Ref 523263 | ClinicalTrials.gov (NCT01246791) Pharmacokinetics of NPC-01 After Single Oral Administration in Healthy Female Volunteers. U.S. National Institutes of Health. | ||||
Ref 525493 | Bioorg Med Chem Lett. 1999 Apr 19;9(8):1137-40.Synthesis and biological activity of trans-2,3-dihydroraloxifene. | ||||
Ref 525501 | Bioorg Med Chem Lett. 1999 May 3;9(9):1233-8.Synthesis and evaluation of geldanamycin-estradiol hybrids. | ||||
Ref 525663 | Bioorg Med Chem Lett. 1999 Dec 20;9(24):3387-92.Estrogenic antagonists bearing dicarba-closo-dodecaborane as a hydrophobic pharmacophore. | ||||
Ref 525689 | Estrogen 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. | ||||
Ref 525879 | Conformational changes and coactivator recruitment by novel ligands for estrogen receptor-alpha and estrogen receptor-beta: correlations with biological character and distinct differences among SRC coactivator family members. Endocrinology. 2000 Oct;141(10):3534-45. | ||||
Ref 526057 | J Med Chem. 2001 May 24;44(11):1654-7.Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. | ||||
Ref 526082 | Centchroman, a selective estrogen receptor modulator, as a contraceptive and for the management of hormone-related clinical disorders. Med Res Rev. 2001 Jul;21(4):302-47. | ||||
Ref 526290 | Estrogen replacement therapy and cardioprotection: mechanisms and controversies. Braz J Med Biol Res. 2002 Mar;35(3):271-6. | ||||
Ref 526345 | J Med Chem. 2002 Jun 6;45(12):2417-24.Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists. | ||||
Ref 526427 | Pharmacological actions of a novel, potent, tissue-selective benzopyran estrogen. J Pharmacol Exp Ther. 2002 Oct;303(1):196-203. | ||||
Ref 526457 | J Med Chem. 2002 Nov 21;45(24):5358-64.Investigations on estrogen receptor binding. The estrogenic, antiestrogenic, and cytotoxic properties of C2-alkyl-substituted 1,1-bis(4-hydroxyphenyl)-2-phenylethenes. | ||||
Ref 526493 | J Nat Prod. 2002 Dec;65(12):1749-53.Isolation and structure elucidation of an isoflavone and a sesterterpenoic acid from Henriettella fascicularis. | ||||
Ref 526532 | Bioorg Med Chem Lett. 2003 Feb 10;13(3):479-83.2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs). | ||||
Ref 526589 | J Med Chem. 2003 Apr 10;46(8):1484-91.Antiestrogenically active 1,1,2-tris(4-hydroxyphenyl)alkenes without basic side chain: synthesis and biological activity. | ||||
Ref 526711 | J Med Chem. 2003 Sep 11;46(19):4032-42.Novel estrogen receptor ligands based on an anthranylaldoxime structure: role of the phenol-type pseudocycle in the binding process. | ||||
Ref 526873 | Bioorg Med Chem Lett. 2003 Nov 17;13(22):4089-92.Utility of boron clusters for drug design. Relation between estrogen receptor binding affinity and hydrophobicity of phenols bearing various types of carboranyl groups. | ||||
Ref 526905 | An overview of nomegestrol acetate selective receptor binding and lack of estrogenic action on hormone-dependent cancer cells. J Steroid Biochem Mol Biol. 2003 Nov;87(2-3):111-22. | ||||
Ref 526949 | Relief of hot flushes with new plant-derived 10-component synthetic conjugated estrogens. Obstet Gynecol. 2004 Feb;103(2):245-53. | ||||
Ref 526966 | J Med Chem. 2004 Feb 26;47(5):1193-206.Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells. | ||||
Ref 527132 | A structural explanation for ERalpha/ERbeta SERM discrimination. Ernst Schering Res Found Workshop. 2004;(46):33-45. | ||||
Ref 527179 | Bioorg Med Chem Lett. 2004 Sep 20;14(18):4659-63.Synthesis and biological evaluation of stilbene-based pure estrogen antagonists. | ||||
Ref 527198 | Bioorg Med Chem Lett. 2004 Oct 4;14(19):4925-9.7-Substituted 2-phenyl-benzofurans as ER beta selective ligands. | ||||
Ref 527232 | J Med Chem. 2004 Oct 7;47(21):5021-40.Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands. | ||||
Ref 527267 | Bioorg 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. | ||||
Ref 527327 | J 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. | ||||
Ref 527343 | Agents with selective estrogen receptor (ER) modulator activity induce apoptosis in vitro and in vivo in ER-negative glioma cells. Cancer Res. 2004 Dec 15;64(24):9115-23. | ||||
Ref 527443 | Bioactivation of the selective estrogen receptor modulator acolbifene to quinone methides. Chem Res Toxicol. 2005 Feb;18(2):174-82. | ||||
Ref 527538 | Differential effects of estrogens and progestins on the anticoagulant tissue factor pathway inhibitor in the rat. J Steroid Biochem Mol Biol. 2005 Mar;94(4):361-8. | ||||
Ref 527550 | J 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. | ||||
Ref 527584 | J 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. | ||||
Ref 527592 | Assay of the synthetic estrogen fosfestrol in pharmaceutical formulations using capillary electrophoresis. J Pharm Biomed Anal. 2005 Sep 15;39(3-4):559-63. | ||||
Ref 527681 | Bioorg 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. | ||||
Ref 527738 | J Med Chem. 2005 Sep 22;48(19):5989-6003.Differential response of estrogen receptor subtypes to 1,3-diarylindene and 2,3-diarylindene ligands. | ||||
Ref 527797 | Bioorg 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. | ||||
Ref 527880 | Bioorg Med Chem Lett. 2006 Feb 15;16(4):854-8. Epub 2005 Nov 21.Substituted 4-hydroxyphenyl sulfonamides as pathway-selective estrogen receptor ligands. | ||||
Ref 527895 | Bioorg 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. | ||||
Ref 527966 | Bioorg 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. | ||||
Ref 528133 | Fluorine-substituted cyclofenil derivatives as estrogen receptor ligands: synthesis and structure-affinity relationship study of potential positron emission tomography agents for imaging estrogen receptors in breast cancer. J Med Chem. 2006 Apr 20;49(8):2496-511. | ||||
Ref 528422 | Combination therapy for treating breast cancer using antiestrogen, ERA-923, and the mammalian target of rapamycin inhibitor, temsirolimus. Endocr Relat Cancer. 2006 Sep;13(3):863-73. | ||||
Ref 528481 | Bioorg Med Chem Lett. 2007 Jan 1;17(1):118-22. Epub 2006 Oct 1.Estrogen receptor beta ligands: design and synthesis of new 2-phenyl-isoindole-1,3-diones. | ||||
Ref 528557 | J 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 alphaand beta. | ||||
Ref 528827 | J 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. | ||||
Ref 528885 | Bioorg 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. | ||||
Ref 529061 | Bioorg Med Chem Lett. 2007 Nov 15;17(22):6295-8. Epub 2007 Sep 7.Androstene-3,5-dienes as ER-beta selective SERMs. | ||||
Ref 529314 | J Med Chem. 2008 Mar 13;51(5):1344-51. Epub 2008 Feb 13.Monoaryl-substituted salicylaldoximes as ligands for estrogen receptor beta. | ||||
Ref 529687 | J Med Chem. 2008 Oct 23;51(20):6512-30. Epub 2008 Sep 12.Blocking estrogen signaling after the hormone: pyrimidine-core inhibitors of estrogen receptor-coactivator binding. | ||||
Ref 529813 | Bioorg 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. | ||||
Ref 530079 | J 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. | ||||
Ref 530110 | Impact of natural products on developing new anti-cancer agents. Chem Rev. 2009 Jul;109(7):3012-43. | ||||
Ref 530223 | Bazedoxifene, a selective estrogen receptor modulator: effects on the endometrium, ovaries, and breast from a randomized controlled trial in osteoporotic postmenopausal women. Menopause. 2009 Nov-Dec;16(6):1109-15. | ||||
Ref 530807 | J Med Chem. 1991 May;34(5):1624-30.Synthesis and biological activity of new halo-steroidal antiestrogens. | ||||
Ref 530935 | Bioorg Med Chem Lett. 2010 Jun 15;20(12):3764-7. Epub 2010 Apr 19.New estrogenic compounds isolated from Broussonetia kazinoki. | ||||
Ref 531028 | Bioorg Med Chem. 2010 Aug 1;18(15):5593-601. Epub 2010 Jun 20.Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha. | ||||
Ref 531064 | J 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. | ||||
Ref 531066 | J Med Chem. 2010 Aug 26;53(16):6153-63.Effects of 7-O substitutions on estrogenic and anti-estrogenic activities of daidzein analogues in MCF-7 breast cancer cells. | ||||
Ref 531167 | Safety and efficacy of low-dose esterified estrogens and methyltestosterone, alone or combined, for the treatment of hot flashes in menopausal women: a randomized, double-blind, placebo-controlled study. Fertil Steril. 2011 Jan;95(1):366-8. | ||||
Ref 531226 | Estrogen: estrone (E1), estradiol (E2), estriol (E3) and estetrol (E4). Nihon Rinsho. 2010 Jul;68 Suppl 7:448-61. | ||||
Ref 531262 | Bioorg 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). | ||||
Ref 531906 | J Med Chem. 1990 Dec;33(12):3222-9.Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans. | ||||
Ref 532496 | Promestriene, a specific topic estrogen. Review of 40 years of vaginal atrophy treatment: is it safe even in cancer patients. Anticancer Drugs. 2013 Nov;24(10):989-98. | ||||
Ref 532859 | Selective estrogen receptor alpha agonist GTx-758 decreases testosterone with reduced side effects of androgen deprivation therapy in men with advanced prostate cancer. Eur Urol. 2015 Feb;67(2):334-41. | ||||
Ref 533211 | Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. J Med Chem.2015 Jun 25;58(12):4888-904. | ||||
Ref 533286 | RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015 Oct;26(9):948-56. | ||||
Ref 533383 | J 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. | ||||
Ref 533386 | Regulation of rat uterine steroid receptors by nomegestrol acetate, a new 19-nor-progesterone derivative. J Pharmacol Exp Ther. 1989 Feb;248(2):758-61. | ||||
Ref 533407 | J Med Chem. 1986 Sep;29(9):1668-74.Influence of alkyl chain ramification on estradiol receptor binding affinity and intrinsic activity of 1,2-dialkylated 1,2-bis(4- or 3-hydroxyphenyl)ethane estrogens and antiestrogens. | ||||
Ref 533439 | Effect of MK-486 alone on Parkinsonism; studies on the clinical symptoms and catecholamine concentrations in the blood, urine and cerebrospinal fluid. No To Shinkei. 1977 Feb;29(2):205-13. | ||||
Ref 533830 | Droloxifene, a new antiestrogen: its role in metastatic breast cancer. Breast Cancer Res Treat. 1994;31(1):83-94. | ||||
Ref 534524 | Species differences in metabolism of panomifene, an analogue of tamoxifen. Drug Metab Dispos. 1997 Dec;25(12):1370-8. | ||||
Ref 534591 | Low-dose esterified estrogen therapy: effects on bone, plasma estradiol concentrations, endometrium, and lipid levels. Estratab/Osteoporosis Study Group. Arch Intern Med. 1997 Dec 8-22;157(22):2609-15. | ||||
Ref 534677 | J 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. | ||||
Ref 534760 | Idoxifene: a novel selective estrogen receptor modulator prevents bone loss and lowers cholesterol levels in ovariectomized rats and decreases uterine weight in intact rats. Endocrinology. 1998 Dec;139(12):5224-34. | ||||
Ref 534824 | Novel ligands that function as selective estrogens or antiestrogens for estrogen receptor-alpha or estrogen receptor-beta. Endocrinology. 1999 Feb;140(2):800-4. | ||||
Ref 535101 | Molecular mechanism of action at estrogen receptor alpha of a new clinically relevant antiestrogen (GW7604) related to tamoxifen. Endocrinology. 2001 Feb;142(2):838-46. | ||||
Ref 535410 | Chemoprevention for high-risk women: tamoxifen and beyond. Breast J. 2001 Sep-Oct;7(5):311-20. | ||||
Ref 535417 | Estrogen-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. | ||||
Ref 535747 | Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26. | ||||
Ref 536081 | Mitotane for adrenocortical carcinoma treatment. Curr Opin Investig Drugs. 2005 Apr;6(4):386-94. | ||||
Ref 536207 | Mitotane 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. | ||||
Ref 536324 | The 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. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 536404 | The future of the new selective estrogen receptor modulators. Menopause Int. 2007 Mar;13(1):27-34. | ||||
Ref 536671 | Short-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. | ||||
Ref 536915 | Potential 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. | ||||
Ref 536925 | Modulators 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. | ||||
Ref 537099 | 17alpha-Ethinylestradiol hinders nucleotide excision repair in zebrafish liver cells. Aquat Toxicol. 2009 Jan 23. | ||||
Ref 537373 | Beta3-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. | ||||
Ref 537376 | Effect 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. | ||||
Ref 537525 | Effects of Diethylstilbestrol on Programmed Oocyte Death and Induction of Polyovular Follicles in Neonatal Mouse Ovaries. Biol Reprod. 2009 Jun 24. | ||||
Ref 537673 | Inactivation 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. | ||||
Ref 537674 | Danazol 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. | ||||
Ref 538072 | EM-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. | ||||
Ref 543898 | (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: 620). | ||||
Ref 544032 | Phase I/II study of the anti-oestrogen zindoxifene (D16726) in the treatment of advanced breast cancer. A Cancer Research Campaign Phase I/II Clinical Trials Committee study.. Br J Cancer. 1990 March; 61(3): 451-453. | ||||
Ref 544138 | The Haunting of Medical Journals: How Ghostwriting Sold ??RT?? PLoS Med. 2010 September; 7(9): e1000335. | ||||
Ref 548259 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023897) | ||||
Ref 550024 | Review of the effects of 17alpha-estradiol in humans: a less feminizing estrogen with neuroprotective potential. Article first published online: 9 FEB 2009. | ||||
Ref 550861 | CN patent application no. 102406650, Sex steroid precursors alone or in combination with selective estrogen receptor modulator for prevention and treatment of vaginal dryness and sexual dysfunction in postmenop. | ||||
Ref 551316 | Bone targeted drugs 2. synthesis of estrogens with hydroxyapatite affinity, Bioorg. Med. Chem. Lett. 6(9):1047-1050 (1996). | ||||
Ref 551871 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
Ref 551906 | US patent application no. 2010,0278,784, Methods and compositions for treating skin conditions. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.