Target Information
Target General Information | Top | |||||
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Target ID |
T89534
(Former ID: TTDS00242)
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Target Name |
Estrogen receptor (ESR)
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Synonyms |
Nuclear receptor subfamily 3 group A member 1; NR3A1; Estradiol receptor; ESR; ER-alpha; ER
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Gene Name |
ESR1
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 15 Target-related Diseases | + | ||||
1 | Acne vulgaris [ICD-11: ED80] | |||||
2 | Acquired prion disease [ICD-11: 8E01] | |||||
3 | Adrenal cancer [ICD-11: 2D11] | |||||
4 | Breast cancer [ICD-11: 2C60-2C6Y] | |||||
5 | Contraceptive management [ICD-11: QA21] | |||||
6 | Dyspareunia [ICD-11: GA12] | |||||
7 | Female infertility [ICD-11: GA31] | |||||
8 | Low bone mass disorder [ICD-11: FB83] | |||||
9 | Male infertility [ICD-11: GB04] | |||||
10 | Menopausal disorder [ICD-11: GA30] | |||||
11 | Menstrual cycle bleeding disorder [ICD-11: GA20] | |||||
12 | Pituitary gland disorder [ICD-11: 5A60-5A61] | |||||
13 | Skeletal anomaly [ICD-11: LD24] | |||||
14 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
15 | Vaginitis [ICD-11: GA02] | |||||
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 association with 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 to the 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 of BRCA1 and BCAS3. Isoform 3 can bind to ERE and inhibit isoform 1.
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BioChemical Class |
Nuclear hormone receptor
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UniProt ID | ||||||
Sequence |
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY
EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLL LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
ADReCS ID | BADD_A00673 ; BADD_A02072 ; BADD_A05322 ; BADD_A08333 | |||||
HIT2.0 ID | T01QLH |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 36 Approved Drugs | + | ||||
1 | ARZOXIFENE | Drug Info | Approved | Breast cancer | [2], [3] | |
2 | Bazedoxifene | Drug Info | Approved | Osteopetrosis | [4], [5], [6] | |
3 | Cenestin | Drug Info | Approved | Menopause symptom | [5] | |
4 | Clomifene | Drug Info | Approved | Female infertility | [7], [8] | |
5 | Clomiphene Citrate | Drug Info | Approved | Female infertility | [5] | |
6 | Conjugated estrogens a | Drug Info | Approved | Hormone replacement therapy | [5] | |
7 | Conjugated estrogens b | Drug Info | Approved | Hormone replacement therapy | [5] | |
8 | Cyclofenil | Drug Info | Approved | Infertility | [5] | |
9 | Danazol | Drug Info | Approved | Menorrhagia | [9], [10] | |
10 | Dienestrol | Drug Info | Approved | Atrophic vaginitis | [5], [11], [12] | |
11 | Diethylstilbestrol | Drug Info | Approved | Gonorrheal vaginitis | [5], [13], [14] | |
12 | Esterified estrogens | Drug Info | Approved | Breast cancer | [5] | |
13 | Estradiol | Drug Info | Approved | Breast cancer | [5], [15], [16], [17], [18] | |
14 | Estradiol Acetate | Drug Info | Approved | Hormone replacement therapy | [5] | |
15 | Estradiol Cypionate | Drug Info | Approved | Hormone replacement therapy | [5] | |
16 | Estradiol Valerate | Drug Info | Approved | Hormone replacement therapy | [5] | |
17 | Estriol | Drug Info | Approved | Hormone deficiency | [19], [20], [5] | |
18 | Estrogen | Drug Info | Approved | Menopause symptom | [5] | |
19 | Estrone | Drug Info | Approved | Menopausal and postmenopausal disorder | [21], [22] | |
20 | Estropipate | Drug Info | Approved | Hypogonadism | [5] | |
21 | Ethinyl Estradiol | Drug Info | Approved | Female hypogonadism | [23], [16] | |
22 | Fosfestrol | Drug Info | Approved | Solid tumour/cancer | [5] | |
23 | Fulvestrant | Drug Info | Approved | Breast cancer | [24], [16] | |
24 | Gestrinone | Drug Info | Approved | Breast cancer | [5] | |
25 | Lasofoxifene | Drug Info | Approved | Osteoporosis | [25], [26] | |
26 | Levormeloxifene | Drug Info | Approved | Breast cancer | [27] | |
27 | Mestranol | Drug Info | Approved | Contraception | [28], [29] | |
28 | Mitotane | Drug Info | Approved | Adrenocortical carcinoma | [30], [31] | |
29 | Nomegestrol acetate | Drug Info | Approved | Breast cancer | [32], [33], [5] | |
30 | Ospemifene | Drug Info | Approved | Dyspareunia | [34], [35] | |
31 | Premarin/Trimegestone | Drug Info | Approved | Menopause symptom | [5] | |
32 | Promestriene | Drug Info | Approved | Acne vulgaris | [5] | |
33 | Quinestrol | Drug Info | Approved | Breast cancer | [36], [37], [5] | |
34 | Raloxifene | Drug Info | Approved | Osteoporosis | [5] | |
35 | Tamoxifen | Drug Info | Approved | Breast cancer | [38], [39] | |
36 | Toremifene | Drug Info | Approved | Breast cancer | [40], [16] | |
Clinical Trial Drug(s) | [+] 28 Clinical Trial Drugs | + | ||||
1 | Acolbifene | Drug Info | Phase 3 | Breast cancer | [41] | |
2 | NPC-01 | Drug Info | Phase 3 | Dysmenorrhea | [42] | |
3 | Premarin/Pravachol | Drug Info | Phase 3 | Hyperlipidaemia | [43] | |
4 | RAD-1901 | Drug Info | Phase 3 | Breast cancer | [44] | |
5 | Synthetic conjugated estrogen | Drug Info | Phase 3 | Vaginal disease | [45] | |
6 | Trimegestone/ethinyl estradiol | Drug Info | Phase 3 | Contraception | [46] | |
7 | TZTX-001 | Drug Info | Phase 3 | Endometriosis | [47] | |
8 | Afimoxifene | Drug Info | Phase 2 | Breast cancer | [48] | |
9 | ARN-810 | Drug Info | Phase 2 | Breast cancer | [49] | |
10 | AZD9833 | Drug Info | Phase 2 | ER-positive breast cancer | [50] | |
11 | Endoxifen | Drug Info | Phase 2 | Breast cancer | [51], [52] | |
12 | Estetrol | Drug Info | Phase 2 | Autoimmune diabetes | [53] | |
13 | GTx-758 | Drug Info | Phase 2 | Prostate cancer | [54] | |
14 | ICARITIN | Drug Info | Phase 2 | Breast cancer | [55] | |
15 | SR 16234 | Drug Info | Phase 2 | Breast cancer | [56] | |
16 | H3B-6545 | Drug Info | Phase 1/2 | Breast cancer | [57] | |
17 | OP-1250 | Drug Info | Phase 1/2 | Breast cancer | [58] | |
18 | ZN-c5 | Drug Info | Phase 1/2 | Breast cancer | [59] | |
19 | ATD transdermal gel | Drug Info | Phase 1 | Contraception | [60] | |
20 | AZD9496 | Drug Info | Phase 1 | Breast cancer | [52] | |
21 | CC-8490 | Drug Info | Phase 1 | Brain cancer | [61] | |
22 | CHF-4227 | Drug Info | Phase 1 | Osteoporosis | [62] | |
23 | D-0502 | Drug Info | Phase 1 | Breast cancer | [63] | |
24 | G1T-48 | Drug Info | Phase 1 | Breast cancer | [64] | |
25 | LY3484356 | Drug Info | Phase 1 | Breast cancer | [65] | |
26 | SCO-120 | Drug Info | Phase 1 | Breast cancer | [66] | |
27 | TTC-352 | Drug Info | Phase 1 | Breast cancer | [52] | |
28 | TTC-352 | Drug Info | Phase 1 | Metastatic melanoma | [67] | |
Discontinued Drug(s) | [+] 19 Discontinued Drugs | + | ||||
1 | BITHIONOL | Drug Info | Withdrawn from market | Trematode infection | [68], [5] | |
2 | Chlorotrianisene | Drug Info | Withdrawn from market | Menopause symptom | [69] | |
3 | HEXESTROL | Drug Info | Withdrawn from market | Irregularities | [70], [71], [72] | |
4 | EM-800 | Drug Info | Discontinued in Phase 3 | Estrogen deficiency | [73] | |
5 | Idoxifene | Drug Info | Discontinued in Phase 3 | Breast cancer | [74] | |
6 | IoGen | Drug Info | Discontinued in Phase 3 | Pain | [75] | |
7 | Miproxifene | Drug Info | Discontinued in Phase 3 | Solid tumour/cancer | [76] | |
8 | Droloxifene | Drug Info | Discontinued in Phase 2 | Breast cancer | [77] | |
9 | ERA-923 | Drug Info | Discontinued in Phase 2 | Breast cancer | [78] | |
10 | NP-50301 | Drug Info | Discontinued in Phase 2 | Eye disorder | [79] | |
11 | Panomifene | Drug Info | Discontinued in Phase 2 | Solid tumour/cancer | [80] | |
12 | SERM-3339 | Drug Info | Discontinued in Phase 2 | Osteoporosis | [81] | |
13 | SR-90067 | Drug Info | Discontinued in Phase 2 | Hormone deficiency | [82] | |
14 | HE2100 | Drug Info | Discontinued in Phase 1 | Thrombocytopenia | [83] | |
15 | HRT | Drug Info | Discontinued in Phase 1 | Estrogen deficiency | [84] | |
16 | MX-4509 | Drug Info | Discontinued in Phase 1 | Neurological disorder | [85] | |
17 | ICI-164384 | Drug Info | Terminated | Breast cancer | [87] | |
18 | Zindoxifene | Drug Info | Terminated | Breast cancer | [88] | |
19 | ZK-119010 | Drug Info | Terminated | Carcinoma | [89] | |
Preclinical Drug(s) | [+] 6 Preclinical Drugs | + | ||||
1 | BN-AA-003-NY | Drug Info | Preclinical | Estrogen deficiency | [86] | |
2 | BN-AO-014 | Drug Info | Preclinical | Atrophy | [86] | |
3 | BN-CB-045 | Drug Info | Preclinical | Female sexual arousal dysfunction | [86] | |
4 | BN-DF-037 | Drug Info | Preclinical | Osteoporosis | [86] | |
5 | BN-GU-005-DHP | Drug Info | Preclinical | Arthralgia | [86] | |
6 | BN-OD-026 | Drug Info | Preclinical | Solid tumour/cancer | [86] | |
Mode of Action | [+] 6 Modes of Action | + | ||||
Inhibitor | [+] 193 Inhibitor drugs | + | ||||
1 | ARZOXIFENE | Drug Info | [90] | |||
2 | ATD transdermal gel | Drug Info | [116] | |||
3 | BITHIONOL | Drug Info | [139] | |||
4 | HEXESTROL | Drug Info | [141] | |||
5 | ERA-923 | Drug Info | [146], [147] | |||
6 | HE2100 | Drug Info | [152] | |||
7 | MX-4509 | Drug Info | [154] | |||
8 | ICI-164384 | Drug Info | [157] | |||
9 | LY-117018 | Drug Info | [158] | |||
10 | Tamoxifen methyl iodide | Drug Info | [159] | |||
11 | ZK-119010 | Drug Info | [161] | |||
12 | 1,2-Bis-(4-hydroxy-phenyl)-3H-inden-5-ol | Drug Info | [162] | |||
13 | 1,8-Dichloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
14 | 1-Bromo-6-(4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
15 | 1-CHLORO-6-(4-HYDROXYPHENYL)-2-NAPHTHOL | Drug Info | [163] | |||
16 | 1-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
17 | 17-METHYL-17-ALPHA-DIHYDROEQUILENIN | Drug Info | [164] | |||
18 | 2,3-diphenyl-1H-indole | Drug Info | [165] | |||
19 | 2,4-Dibenzylamino-6-isopentylpyrimidine | Drug Info | [166] | |||
20 | 2,4-diisobutylamino-6-isopentylpyrimidine | Drug Info | [166] | |||
21 | 2-(2-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [167] | |||
22 | 2-(3-Butoxy-4-hydroxy-phenyl)-benzooxazol-6-ol | Drug Info | [167] | |||
23 | 2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [167] | |||
24 | 2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-6-ol | Drug Info | [167] | |||
25 | 2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [167] | |||
26 | 2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-6-ol | Drug Info | [167] | |||
27 | 2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol | Drug Info | [168] | |||
28 | 2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-6-ol | Drug Info | [168] | |||
29 | 2-(4-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol | Drug Info | [167] | |||
30 | 2-(4-Hydroxy-phenyl)-4-methoxy-quinolin-6-ol | Drug Info | [169] | |||
31 | 2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-ol | Drug Info | [169] | |||
32 | 2-(4-Hydroxy-phenyl)-7-isopropyl-benzooxazol-5-ol | Drug Info | [167] | |||
33 | 2-(4-Hydroxy-phenyl)-7-methoxy-benzofuran-5-ol | Drug Info | [170] | |||
34 | 2-(4-Hydroxy-phenyl)-7-methoxy-benzooxazol-5-ol | Drug Info | [167] | |||
35 | 2-(4-Hydroxy-phenyl)-7-methyl-benzofuran-5-ol | Drug Info | [170] | |||
36 | 2-(4-Hydroxy-phenyl)-7-phenyl-benzooxazol-5-ol | Drug Info | [167] | |||
37 | 2-(4-Hydroxy-phenyl)-7-propenyl-benzooxazol-5-ol | Drug Info | [167] | |||
38 | 2-(4-Hydroxy-phenyl)-7-propyl-benzooxazol-5-ol | Drug Info | [167] | |||
39 | 2-(4-Hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol | Drug Info | [167] | |||
40 | 2-(4-Hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [167] | |||
41 | 2-(4-Hydroxy-phenyl)-benzooxazol-6-ol | Drug Info | [167] | |||
42 | 2-(4-Hydroxy-phenyl)-quinolin-6-ol | Drug Info | [169] | |||
43 | 2-(4-HYDROXY-PHENYL)BENZOFURAN-5-OL | Drug Info | [167] | |||
44 | 2-(4-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol | Drug Info | [168] | |||
45 | 2-(5-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol | Drug Info | [167] | |||
46 | 2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-5-ol | Drug Info | [167] | |||
47 | 2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol | Drug Info | [167] | |||
48 | 2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-5-ol | Drug Info | [167] | |||
49 | 2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-6-ol | Drug Info | [167] | |||
50 | 2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE | Drug Info | [164] | |||
51 | 2-Naphthalen-1-yl-benzooxazol-6-ol | Drug Info | [167] | |||
52 | 2-phenyl-1,2'-spirobi[1H-indene]-5'-ol | Drug Info | [168] | |||
53 | 3'-Methoxy-4'Hydroxyclomiphene | Drug Info | [171] | |||
54 | 3,8-dihydroxy-4-methyl-6H-benzo[c]chromen-6-one | Drug Info | [172] | |||
55 | 3,8-dihydroxy-7-methyl-6H-benzo[c]chromen-6-one | Drug Info | [172] | |||
56 | 3-(2-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol | Drug Info | [167] | |||
57 | 3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-5-ol | Drug Info | [167] | |||
58 | 3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol | Drug Info | [167] | |||
59 | 3-(4-Hydroxyphenyl)-7-isobutoxychromen-4-one | Drug Info | [173] | |||
60 | 3-(4-Hydroxyphenyl)-7-isopropoxychromen-4-one | Drug Info | [173] | |||
61 | 3-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol | Drug Info | [167] | |||
62 | 3-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol | Drug Info | [167] | |||
63 | 3-CHLORO-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OL | Drug Info | [164] | |||
64 | 3-chloro-4-(4-hydroxyphenyl)salicylaldoxime | Drug Info | [174] | |||
65 | 3-ETHYL-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OL | Drug Info | [164] | |||
66 | 3-hydroxy-8,10-dimethyl-6H-benzo[c]chromen-6-one | Drug Info | [172] | |||
67 | 3-[1-ethyl-2-(3-hydroxyphenyl)butyl]phenol | Drug Info | [175] | |||
68 | 4',5,7-trihydroxy-6,8-dimethylisoflavone | Drug Info | [176] | |||
69 | 4,10-dimethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [172] | |||
70 | 4,6,10-trimethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [172] | |||
71 | 4,6,6,7-tetramethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [172] | |||
72 | 4,6,7,10-tetramethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [172] | |||
73 | 4,6,7-trimethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [172] | |||
74 | 4,7-dimethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [172] | |||
75 | 4-(1,2-Diphenyl-but-1-enyl)-phenol | Drug Info | [177] | |||
76 | 4-(1-benzyl-7-chloro-1H-indazol-3-yl)phenol | Drug Info | [178] | |||
77 | 4-(1-butyl-7-chloro-1H-indazol-3-yl)phenol | Drug Info | [178] | |||
78 | 4-(1-cyclopentyl-7-fluoro-1H-indazol-3-yl)phenol | Drug Info | [178] | |||
79 | 4-(2-phenyl-1H-benzo[d]imidazol-1-yl)phenol | Drug Info | [165] | |||
80 | 4-(2-phenyl-1H-indol-3-yl)phenol | Drug Info | [165] | |||
81 | 4-(3-(4-hydroxyphenyl)-1H-indol-2-yl)phenol | Drug Info | [165] | |||
82 | 4-(3-phenyl-1H-indol-2-yl)phenol | Drug Info | [165] | |||
83 | 4-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol | Drug Info | [167] | |||
84 | 4-(6-HYDROXY-1H-INDAZOL-3-YL)BENZENE-1,3-DIOL | Drug Info | [164] | |||
85 | 4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol | Drug Info | [167] | |||
86 | 4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol | Drug Info | [167] | |||
87 | 4-(7-chloro-1-cyclohexyl-1H-indazol-3-yl)phenol | Drug Info | [178] | |||
88 | 4-(7-chloro-1-cyclopentyl-1H-indazol-3-yl)phenol | Drug Info | [178] | |||
89 | 4-(7-chloro-1-propyl-1H-indazol-3-yl)phenol | Drug Info | [178] | |||
90 | 4-(7-methyl-1-propyl-1H-indazol-3-yl)phenol | Drug Info | [178] | |||
91 | 4-Benzo[d]isoxazol-3-yl-benzene-1,3-diol | Drug Info | [167] | |||
92 | 4-benzyl-2,6-diisobutylamino-pyrimidine | Drug Info | [166] | |||
93 | 4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [169] | |||
94 | 4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [169] | |||
95 | 4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [169] | |||
96 | 4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [169] | |||
97 | 4-hydroxy-N,N-diphenylbenzenesulfonamide | Drug Info | [179] | |||
98 | 4-hydroxy-N-isopropyl-N-phenylbenzenesulfonamide | Drug Info | [179] | |||
99 | 4-hydroxy-N-neopentyl-N-phenylbenzenesulfonamide | Drug Info | [179] | |||
100 | 4-hydroxy-N-phenyl-N-propylbenzenesulfonamide | Drug Info | [179] | |||
101 | 4-Naphthalen-2-yl-phenol | Drug Info | [163] | |||
102 | 4-[1,2-bis(4-hydroxyphenyl)but-1-enyl]phenol | Drug Info | [180] | |||
103 | 4-[1,2-bis(4-hydroxyphenyl)hex-1-enyl]phenol | Drug Info | [180] | |||
104 | 4-[1,2-bis(4-hydroxyphenyl)pent-1-enyl]phenol | Drug Info | [180] | |||
105 | 4-[1,2-bis(4-hydroxyphenyl)vinyl]phenol | Drug Info | [180] | |||
106 | 4-[1-(4-hydroxyphenyl)-2-phenylbut-1-enyl]phenol | Drug Info | [177] | |||
107 | 4-[1-(4-hydroxyphenyl)-2-phenylhex-1-enyl]phenol | Drug Info | [177] | |||
108 | 4-[1-(4-hydroxyphenyl)-2-phenylpent-1-enyl]phenol | Drug Info | [177] | |||
109 | 4-[1-(4-hydroxyphenyl)-2-phenylprop-1-enyl]phenol | Drug Info | [177] | |||
110 | 4-[1-(4-hydroxyphenyl)-2-phenylvinyl]phenol | Drug Info | [177] | |||
111 | 4-[2,2-bis(4-hydroxyphenyl)-1-methylvinyl]phenol | Drug Info | [180] | |||
112 | 5-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [169] | |||
113 | 5-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-6-ol | Drug Info | [167] | |||
114 | 5-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [169] | |||
115 | 5-hydroxy-2-phenylisoindoline-1,3-dione | Drug Info | [181] | |||
116 | 6-(2,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
117 | 6-(2,6-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
118 | 6-(2-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
119 | 6-(2-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
120 | 6-(3,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
121 | 6-(3-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
122 | 6-(3-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
123 | 6-(3-Hydroxy-phenyl)-naphthalen-1-ol | Drug Info | [163] | |||
124 | 6-(3-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
125 | 6-(4-Hydroxy-2-methoxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
126 | 6-(4-Hydroxy-2-methyl-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
127 | 6-(4-Hydroxy-phenyl)-1-methoxy-naphthalen-2-ol | Drug Info | [163] | |||
128 | 6-(4-Hydroxy-phenyl)-1-methyl-naphthalen-2-ol | Drug Info | [163] | |||
129 | 6-(4-Hydroxy-phenyl)-1-nitro-naphthalen-2-ol | Drug Info | [163] | |||
130 | 6-(4-Hydroxy-phenyl)-1-phenyl-naphthalen-2-ol | Drug Info | [163] | |||
131 | 6-(4-Hydroxy-phenyl)-naphthalen-1-ol | Drug Info | [163] | |||
132 | 6-(4-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [169] | |||
133 | 6-butyl-2,4-dipropylaminopyrimidine | Drug Info | [166] | |||
134 | 6-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [167] | |||
135 | 6-ethyl-2,4-diisobutylaminopyrimidine | Drug Info | [166] | |||
136 | 6-ethyl-4,7-dimethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [172] | |||
137 | 6-Phenyl-naphthalen-2-ol | Drug Info | [163] | |||
138 | 7-(3-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
139 | 7-(4-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
140 | 7-Allyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [167] | |||
141 | 7-Bromo-2-(4-hydroxy-phenyl)-benzofuran-5-ol | Drug Info | [170] | |||
142 | 7-Butyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [167] | |||
143 | 7-Chloro-2-(4-hydroxy-phenyl)-benzofuran-5-ol | Drug Info | [170] | |||
144 | 7-Cyclopentyloxy-3-(4-hydroxyphenyl)chromen-4-one | Drug Info | [173] | |||
145 | 7-Ethyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [167] | |||
146 | 7-Ethynyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [167] | |||
147 | 7-Phenyl-naphthalen-2-ol | Drug Info | [163] | |||
148 | 8-(2,2-dimethylpropyl)naringenin | Drug Info | [182] | |||
149 | 8-(2-methylpropyl)naringenin | Drug Info | [182] | |||
150 | 8-(3-methylbutyl)naringenin | Drug Info | [182] | |||
151 | 8-benzylnaringenin | Drug Info | [182] | |||
152 | 8-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
153 | 8-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [163] | |||
154 | 8-methylnaringenin | Drug Info | [182] | |||
155 | 8-n-heptylnaringenin | Drug Info | [182] | |||
156 | 8-n-nonylnaringenin | Drug Info | [182] | |||
157 | 8-n-pentylnaringenin | Drug Info | [182] | |||
158 | 8-n-propylnaringenin | Drug Info | [182] | |||
159 | 8-n-undecylnaringenin | Drug Info | [182] | |||
160 | BROUSSONIN A | Drug Info | [183] | |||
161 | Carboron Cluster with phenol | Drug Info | [184] | |||
162 | COUMESTROL | Drug Info | [185] | |||
163 | CP-394531 | Drug Info | [186] | |||
164 | CP-409069 | Drug Info | [186] | |||
165 | daidzein | Drug Info | [176] | |||
166 | DIHYDRORALOXIFENE | Drug Info | [187] | |||
167 | Doxorubicin-Formaldehyde Conjugate | Drug Info | [188] | |||
168 | EFFUSOL | Drug Info | [172] | |||
169 | Geldanamycin-estradiol hybrid | Drug Info | [190] | |||
170 | GSK-5182 | Drug Info | [191] | |||
171 | JNJ-17148066 | Drug Info | [193] | |||
172 | JNJ-19398990 | Drug Info | [193] | |||
173 | JNJ-26529126 | Drug Info | [193] | |||
174 | JNJ-26529152 | Drug Info | [193] | |||
175 | LTERHKILHRLLQEGSPSD | Drug Info | [194] | |||
176 | MPrP | Drug Info | [196] | |||
177 | N,N,N-Triisobutyl-pyrimidine-2,4,6-triamine | Drug Info | [166] | |||
178 | N-allyl-4-hydroxy-N-phenylbenzenesulfonamide | Drug Info | [179] | |||
179 | N-benzyl-4-hydroxy-N-phenylbenzenesulfonamide | Drug Info | [179] | |||
180 | N-butyl-4-hydroxy-N-phenylbenzenesulfonamide | Drug Info | [179] | |||
181 | N-cyclohexyl-4-hydroxy-N-phenylbenzenesulfonamide | Drug Info | [179] | |||
182 | N-ethyl-4-hydroxy-N-phenylbenzenesulfonamide | Drug Info | [179] | |||
183 | Nafoxidine | Drug Info | [197] | |||
184 | SNG-163 | Drug Info | [116] | |||
185 | SNG-8033 | Drug Info | [116] | |||
186 | SOPHORAFLAVANONE B | Drug Info | [182] | |||
187 | Tamoxifen butyl bromide | Drug Info | [159] | |||
188 | Tamoxifen ethyl bromide | Drug Info | [159] | |||
189 | Tamoxifen isopropyl bromide | Drug Info | [159] | |||
190 | WAY-169916 | Drug Info | [178] | |||
191 | WAY200070 | Drug Info | [167] | |||
192 | ZK-164015 | Drug Info | [201] | |||
193 | [1,1':2',1'']Terphenyl-4'-carbaldehyde oxime | Drug Info | [202] | |||
Modulator | [+] 58 Modulator drugs | + | ||||
1 | Bazedoxifene | Drug Info | [5], [91] | |||
2 | Clomifene | Drug Info | [94] | |||
3 | Clomiphene Citrate | Drug Info | [95] | |||
4 | Conjugated estrogens a | Drug Info | [16] | |||
5 | Conjugated estrogens b | Drug Info | [96], [16] | |||
6 | Cyclofenil | Drug Info | [97], [5] | |||
7 | Esterified estrogens | Drug Info | [101], [5] | |||
8 | Estradiol Acetate | Drug Info | [95] | |||
9 | Estradiol Cypionate | Drug Info | [95] | |||
10 | Estradiol Valerate | Drug Info | [95] | |||
11 | Estropipate | Drug Info | [104], [5] | |||
12 | Fosfestrol | Drug Info | [106], [107] | |||
13 | Gestrinone | Drug Info | [16] | |||
14 | Lasofoxifene | Drug Info | [26] | |||
15 | Levormeloxifene | Drug Info | [108], [5] | |||
16 | Nomegestrol acetate | Drug Info | [5], [32], [33] | |||
17 | Ospemifene | Drug Info | [112] | |||
18 | Premarin/Trimegestone | Drug Info | [113], [5] | |||
19 | Promestriene | Drug Info | [114], [5] | |||
20 | Quinestrol | Drug Info | [115] | |||
21 | Raloxifene | Drug Info | [116] | |||
22 | Toremifene | Drug Info | [119] | |||
23 | Acolbifene | Drug Info | [120] | |||
24 | NPC-01 | Drug Info | [42] | |||
25 | Premarin/Pravachol | Drug Info | [43] | |||
26 | RAD-1901 | Drug Info | [121] | |||
27 | Synthetic conjugated estrogen | Drug Info | [122], [5] | |||
28 | Trimegestone/ethinyl estradiol | Drug Info | [123] | |||
29 | TZTX-001 | Drug Info | [124] | |||
30 | Afimoxifene | Drug Info | [116] | |||
31 | ARN-810 | Drug Info | [125] | |||
32 | Endoxifen | Drug Info | [116] | |||
33 | Estetrol | Drug Info | [127] | |||
34 | GTx-758 | Drug Info | [128] | |||
35 | ICARITIN | Drug Info | [129] | |||
36 | SR 16234 | Drug Info | [130] | |||
37 | CC-8490 | Drug Info | [133] | |||
38 | CHF-4227 | Drug Info | [134] | |||
39 | Idoxifene | Drug Info | [143] | |||
40 | IoGen | Drug Info | [116] | |||
41 | Miproxifene | Drug Info | [144] | |||
42 | Droloxifene | Drug Info | [145] | |||
43 | NP-50301 | Drug Info | [148] | |||
44 | Panomifene | Drug Info | [149] | |||
45 | SERM-3339 | Drug Info | [150] | |||
46 | BN-AA-003-NY | Drug Info | [155] | |||
47 | BN-AO-014 | Drug Info | [155] | |||
48 | BN-CB-045 | Drug Info | [155] | |||
49 | BN-DF-037 | Drug Info | [155] | |||
50 | BN-GU-005-DHP | Drug Info | [155] | |||
51 | BN-OD-026 | Drug Info | [156] | |||
52 | Zindoxifene | Drug Info | [160] | |||
53 | Estriol E3 | Drug Info | [189] | |||
54 | Org-37663 | Drug Info | [198] | |||
55 | RG6046 | Drug Info | [5] | |||
56 | SERMs | Drug Info | [116] | |||
57 | STX | Drug Info | [116] | |||
58 | TSERaM | Drug Info | [116] | |||
Agonist | [+] 15 Agonist drugs | + | ||||
1 | Cenestin | Drug Info | [5], [92], [93] | |||
2 | Dienestrol | Drug Info | [99] | |||
3 | Diethylstilbestrol | Drug Info | [100] | |||
4 | Estradiol | Drug Info | [102] | |||
5 | Estriol | Drug Info | [102] | |||
6 | Estrogen | Drug Info | [103] | |||
7 | Estrone | Drug Info | [102] | |||
8 | Ethinyl Estradiol | Drug Info | [105], [102] | |||
9 | Mestranol | Drug Info | [109] | |||
10 | TTC-352 | Drug Info | [52] | |||
11 | TTC-352 | Drug Info | [138] | |||
12 | SR-90067 | Drug Info | [151] | |||
13 | HRT | Drug Info | [153] | |||
14 | propylpyrazoletriol | Drug Info | [199] | |||
15 | R,R-THC | Drug Info | [200] | |||
Antagonist | [+] 11 Antagonist drugs | + | ||||
1 | Danazol | Drug Info | [98] | |||
2 | Fulvestrant | Drug Info | [1] | |||
3 | Tamoxifen | Drug Info | [117], [118] | |||
4 | H3B-6545 | Drug Info | [52] | |||
5 | OP-1250 | Drug Info | [131] | |||
6 | AZD9496 | Drug Info | [52] | |||
7 | EM-800 | Drug Info | [142] | |||
8 | GW7604 | Drug Info | [192] | |||
9 | methyl-piperidino-pyrazole | Drug Info | [195] | |||
10 | SNG-8006 | Drug Info | [116] | |||
11 | Trans-hydroxytamoxifen | Drug Info | [195] | |||
Binder | [+] 2 Binder drugs | + | ||||
1 | Mitotane | Drug Info | [110], [111] | |||
2 | Chlorotrianisene | Drug Info | [140] | |||
Degrader | [+] 6 Degrader drugs | + | ||||
1 | AZD9833 | Drug Info | [126] | |||
2 | ZN-c5 | Drug Info | [132] | |||
3 | D-0502 | Drug Info | [135] | |||
4 | G1T-48 | Drug Info | [136] | |||
5 | LY3484356 | Drug Info | [65] | |||
6 | SCO-120 | Drug Info | [137] |
Chemical Structure based Activity Landscape of Target | Top |
---|---|
Drug Property Profile of Target | Top | |
---|---|---|
(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
|
||
(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
|
||
(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
|
||
"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
---|---|---|---|---|---|---|
Co-Targets |
Target Poor or Non Binders | Top | |||||
---|---|---|---|---|---|---|
Target Poor or Non Binders |
Target Regulators | Top | |||||
---|---|---|---|---|---|---|
Target-regulating microRNAs | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
---|---|---|---|---|---|---|
Target Expression Profile (TEP) | ||||||
Drug Resistance Mutation (DRM) |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | 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 2 | Clinical pipeline report, company report or official report of Lilly. | |||||
REF 3 | 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 4 | URL: 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 5 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 6 | 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. | |||||
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REF 8 | Emerging drugs for hypogonadism. Expert Opin Emerg Drugs. 2006 Nov;11(4):685-707. | |||||
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REF 10 | Emerging drugs for idiopathic thrombocytopenic purpura in adults. Expert Opin Emerg Drugs. 2008 Jun;13(2):237-54. | |||||
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REF 12 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 006110. | |||||
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REF 14 | Drug information of Diethylstilbestrol, 2008. eduDrugs. | |||||
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REF 16 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
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REF 18 | Estradiol regulates estrogen receptor mRNA stability. J Steroid Biochem Mol Biol. 1998 Aug;66(3):113-20. | |||||
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REF 20 | Drug information of Estriol, 2008. eduDrugs. | |||||
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REF 22 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 085239. | |||||
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REF 24 | URL: 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). | |||||
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REF 26 | Pfizer. Product Development Pipeline. March 31 2009. | |||||
REF 27 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009670) | |||||
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REF 29 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010976. | |||||
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REF 31 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 016885. | |||||
REF 32 | 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 33 | 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 34 | URL: 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 35 | Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651. | |||||
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REF 37 | Drug information of Quinestrol, 2008. eduDrugs. | |||||
REF 38 | URL: 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 39 | 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. | |||||
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REF 41 | ClinicalTrials.gov (NCT01452373) Dehydroepiandrosterone (DHEA) + Acolbifene Against Vasomotor Symptoms (Hot Flushes) in Postmenopausal Women. U.S. National Institutes of Health. | |||||
REF 42 | ClinicalTrials.gov (NCT01246791) Pharmacokinetics of NPC-01 After Single Oral Administration in Healthy Female Volunteers. U.S. National Institutes of Health. | |||||
REF 43 | Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26. | |||||
REF 44 | ClinicalTrials.gov (NCT03778931) Phase 3 Trial of Elacestrant vs. Standard of Care for the Treatment of Patients With ER+/HER2- Advanced Breast Cancer (EMERALD). U.S. National Institutes of Health. | |||||
REF 45 | 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 46 | 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 47 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800038089) | |||||
REF 48 | ClinicalTrials.gov (NCT00272714) Study of Afimoxifene Gel to Treat Cyclic Mastalgia in Premenopausal Women. U.S. National Institutes of Health. | |||||
REF 49 | 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 50 | ClinicalTrials.gov (NCT04214288) A Comparative Study of AZD9833 Versus Fulvestrant in Women With Advanced ER-Positive HER2-Negative Breast Cancer (SERENA-2). U.S. National Institutes of Health. | |||||
REF 51 | 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 52 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 53 | ClinicalTrials.gov (NCT00563472) Feasibility Study Into the Contraceptive Effect of Estetrol. U.S. National Institutes of Health. | |||||
REF 54 | 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 55 | ClinicalTrials.gov (NCT01972672) The Phase II Study of Icaritin in Patients With Advanced Hepatocellular Carcinoma. U.S. National Institutes of Health. | |||||
REF 56 | 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 57 | ClinicalTrials.gov (NCT03250676) Trial of H3B-6545, in Women With Locally Advanced or Metastatic Estrogen Receptor-positive, HER2 Negative Breast Cancer. U.S. National Institutes of Health. | |||||
REF 58 | ClinicalTrials.gov (NCT04505826) A Dose Escalation/Expansion Study of Oral OP-1250 in Subjects With Advanced and/or Metastatic HR+, HER2- Breast Cancer. U.S. National Institutes of Health. | |||||
REF 59 | ClinicalTrials.gov (NCT03560531) A Study of ZN-c5 in Subjects With Breast Cancer. U.S. National Institutes of Health. | |||||
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REF 61 | 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. | |||||
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REF 63 | ClinicalTrials.gov (NCT03471663) A First-in-Human Study of D-0502 Alone and in Combination With Palbociclib in Women With Advanced or Metastatic ER-Positive and HER2-Negative Breast Cancer. U.S. National Institutes of Health. | |||||
REF 64 | ClinicalTrials.gov (NCT03455270) G1T48, an Oral SERD, Alone and in Combination With Palbociclib in ER-Positive, HER2-Negative Advanced Breast Cancer. U.S. National Institutes of Health. | |||||
REF 65 | ClinicalTrials.gov (NCT04647487) A Study of LY3484356 in Women With Breast Cancer Before Having Surgery (EMBER-2). U.S. National Institutes of Health. | |||||
REF 66 | ClinicalTrials.gov (NCT04242953) Study to Determine Safety, Tolerability and Pharmacokinetics, of SCO-120 in Healthy Male and Post-menopausal Female Subjects. U.S. National Institutes of Health. | |||||
REF 67 | ClinicalTrials.gov (NCT03201913) Study of TTC-352 in Patients With Metastatic Breast Cancer Progressing on Endocrine Therapy. U.S. National Institutes of Health. | |||||
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REF 69 | FDA Approved Drug Products from FDA Official Website. 2008. Application Number: (ANDA) 017675. | |||||
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REF 144 | 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. | |||||
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