General Information of Drug Off-Target (DOT) (ID: OTKLU61J)

DOT Name Estrogen receptor (ESR1)
Synonyms ER; ER-alpha; Estradiol receptor; Nuclear receptor subfamily 3 group A member 1
Gene Name ESR1
Related Disease
Estrogen resistance syndrome ( )
UniProt ID
ESR1_HUMAN
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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PDB ID
1A52 ; 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 ; 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 ; 4PXM ; 4Q13 ; 4Q50 ; 4TUZ ; 4TV1 ; 4XI3 ; 4ZN7 ; 4ZN9 ; 4ZNH ; 4ZNS ; 4ZNT ; 4ZNU ; 4ZNV ; 4ZNW ; 5AAU ; 5AAV ; 5ACC ; 5AK2 ; 5DI7 ; 5DID ; 5DIE ; 5DIG ; 5DK9 ; 5DKB ; 5DKE ; 5DKG ; 5DKS ; 5DL4 ; 5DLR ; 5DMC ; 5DMF ; 5DP0 ; 5DRJ ; 5DRM ; 5DTV ; 5DU5 ; 5DUE ; 5DUG ; 5DUH ; 5DVS ; 5DVV ; 5DWE ; 5DWG ; 5DWI ; 5DWJ ; 5DX3 ; 5DXB ; 5DXE ; 5DXG ; 5DXK ; 5DXM ; 5DXP ; 5DXQ ; 5DXR ; 5DY8 ; 5DYB ; 5DYD ; 5DZ0 ; 5DZ1 ; 5DZ3 ; 5DZH ; 5DZI ; 5E0W ; 5E0X ; 5E14 ; 5E15 ; 5E19 ; 5E1C ; 5EGV ; 5EHJ ; 5EI1 ; 5EIT ; 5FQP ; 5FQR ; 5FQS ; 5FQT ; 5FQV ; 5GS4 ; 5GTR ; 5HYR ; 5JMM ; 5KCC ; 5KCD ; 5KCE ; 5KCF ; 5KCT ; 5KCU ; 5KCW ; 5KD9 ; 5KR9 ; 5KRA ; 5KRC ; 5KRF ; 5KRH ; 5KRI ; 5KRJ ; 5KRK ; 5KRL ; 5KRM ; 5KRO ; 5N10 ; 5T0X ; 5T1Z ; 5T92 ; 5T97 ; 5TLD ; 5TLF ; 5TLG ; 5TLL ; 5TLM ; 5TLO ; 5TLP ; 5TLT ; 5TLU ; 5TLV ; 5TLX ; 5TLY ; 5TM1 ; 5TM2 ; 5TM3 ; 5TM4 ; 5TM5 ; 5TM6 ; 5TM7 ; 5TM8 ; 5TM9 ; 5TML ; 5TMM ; 5TMO ; 5TMQ ; 5TMR ; 5TMS ; 5TMT ; 5TMU ; 5TMV ; 5TMW ; 5TMZ ; 5TN1 ; 5TN3 ; 5TN4 ; 5TN5 ; 5TN6 ; 5TN7 ; 5TN8 ; 5TN9 ; 5TNB ; 5U2B ; 5U2D ; 5UFW ; 5UFX ; 5W9C ; 5W9D ; 5WGD ; 5WGQ ; 6B0F ; 6C42 ; 6CBZ ; 6CHW ; 6CHZ ; 6CZN ; 6D0F ; 6DF6 ; 6DFN ; 6HHP ; 6HKB ; 6HKF ; 6HMU ; 6IAR ; 6OWC ; 6PET ; 6PFM ; 6PIT ; 6PSJ ; 6SBO ; 6SQ0 ; 6SUO ; 6TJM ; 6TL3 ; 6V87 ; 6V8T ; 6VGH ; 6VJD ; 6VPF ; 6WOK ; 6ZOQ ; 6ZOR ; 6ZOS ; 7B9M ; 7B9R ; 7B9T ; 7BA3 ; 7BA5 ; 7BA6 ; 7BA7 ; 7BA8 ; 7BA9 ; 7BAA ; 7BAB ; 7JHD ; 7KBS ; 7MSA ; 7N9O ; 7NDO ; 7NEL ; 7NFB ; 7NFW ; 7NIZ ; 7OPW ; 7OQ7 ; 7OQ8 ; 7PWT ; 7PWZ ; 7QVJ ; 7QVL ; 7R62 ; 7RKE ; 7RNM ; 7RRX ; 7RRY ; 7RRZ ; 7RS0 ; 7RS1 ; 7RS2 ; 7RS3 ; 7RS4 ; 7RS7 ; 7RS8 ; 7RS9 ; 7SFO ; 7T2X ; 7TE7 ; 7UJ7 ; 7UJ8 ; 7UJC ; 7UJF ; 7UJM ; 7UJO ; 7UJW ; 7UJY ; 7WNV ; 7Y8F ; 7Y8G ; 7YMK ; 8AFN ; 8AI0 ; 8ALR ; 8ALT ; 8ALV ; 8ALW ; 8AM7 ; 8ANF ; 8AOY ; 8APS ; 8AQ1 ; 8AQC ; 8AQE ; 8AQZ ; 8AR4 ; 8AR5 ; 8ARG ; 8ARO ; 8ARQ ; 8ARR ; 8ARW ; 8ARX ; 8ARY ; 8ARZ ; 8AS1 ; 8AT9 ; 8ATP ; 8AU2 ; 8AUS ; 8AUY ; 8AV3 ; 8AV4 ; 8AV7 ; 8AV8 ; 8AWG ; 8AXE ; 8AXU ; 8B39 ; 8BWJ ; 8BWX ; 8BWZ ; 8BX0 ; 8BX3 ; 8BX4 ; 8BXI ; 8BXM ; 8BXN ; 8BXO ; 8BXQ ; 8BXS ; 8BY9 ; 8BYB ; 8BYC ; 8BYD ; 8BYE ; 8BYF ; 8BYO ; 8BYY ; 8BYZ ; 8BZ0 ; 8BZA ; 8BZB ; 8BZW ; 8C04 ; 8C0K ; 8C4F ; 8C4G ; 8DU6 ; 8DU8 ; 8DU9 ; 8DUB ; 8DUC ; 8DUD ; 8DUG ; 8DUH ; 8DUI ; 8DUK ; 8DUS ; 8DV5 ; 8DV7 ; 8DV8 ; 8DVB ; 8EV1 ; 8EV2
Pfam ID
PF12743 ; PF00104 ; PF02159 ; PF00105
Sequence
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAY
EFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPF
LQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAK
ETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQAC
RLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKR
SKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINW
AKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEG
MVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLD
KITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLL
LEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV
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. Essential for MTA1-mediated transcriptional regulation of BRCA1 and BCAS3. Maintains neuronal survival in response to ischemic reperfusion injury when in the presence of circulating estradiol (17-beta-estradiol/E2); [Isoform 3]: 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. Binds to ERE and inhibits isoform 1.
Tissue Specificity Widely expressed . Not expressed in the pituitary gland .; [Isoform 3]: Widely expressed, however not expressed in the pituitary gland.
KEGG Pathway
Endocrine resistance (hsa01522 )
Estrogen sig.ling pathway (hsa04915 )
Prolactin sig.ling pathway (hsa04917 )
Thyroid hormone sig.ling pathway (hsa04919 )
Endocrine and other factor-regulated calcium reabsorption (hsa04961 )
Pathways in cancer (hsa05200 )
Proteoglycans in cancer (hsa05205 )
Chemical carcinogenesis - receptor activation (hsa05207 )
Breast cancer (hsa05224 )
Reactome Pathway
PIP3 activates AKT signaling (R-HSA-1257604 )
Constitutive Signaling by Aberrant PI3K in Cancer (R-HSA-2219530 )
Nuclear Receptor transcription pathway (R-HSA-383280 )
SUMOylation of intracellular receptors (R-HSA-4090294 )
Ovarian tumor domain proteases (R-HSA-5689896 )
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling (R-HSA-6811558 )
TFAP2 (AP-2) family regulates transcription of growth factors and their receptors (R-HSA-8866910 )
RUNX1 regulates estrogen receptor mediated transcription (R-HSA-8931987 )
ESR-mediated signaling (R-HSA-8939211 )
RUNX1 regulates transcription of genes involved in WNT signaling (R-HSA-8939256 )
Regulation of RUNX2 expression and activity (R-HSA-8939902 )
Extra-nuclear estrogen signaling (R-HSA-9009391 )
Estrogen-dependent gene expression (R-HSA-9018519 )
Nuclear signaling by ERBB4 (R-HSA-1251985 )

Molecular Interaction Atlas (MIA) of This DOT

1 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Estrogen resistance syndrome DIS2SYXC Supportive Autosomal recessive [1]
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Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 4 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Cisplatin DMRHGI9 Approved Estrogen receptor (ESR1) increases the response to substance of Cisplatin. [80]
Methamphetamine DMPM4SK Approved Estrogen receptor (ESR1) increases the response to substance of Methamphetamine. [81]
Medroxyprogesterone DMBGWPH Approved Estrogen receptor (ESR1) increases the Breast cancer ADR of Medroxyprogesterone. [82]
Conjugated estrogens DMLT0E1 Approved Estrogen receptor (ESR1) increases the Bone density increased ADR of Conjugated estrogens. [82]
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6 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the methylation of Estrogen receptor (ESR1). [2]
Ciclosporin DMAZJFX Approved Ciclosporin increases the methylation of Estrogen receptor (ESR1). [3]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide decreases the methylation of Estrogen receptor (ESR1). [10]
Gefitinib DM15F0X Approved Gefitinib decreases the phosphorylation of Estrogen receptor (ESR1). [35]
Dinoprostone DMTYOPD Approved Dinoprostone increases the phosphorylation of Estrogen receptor (ESR1). [37]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene decreases the methylation of Estrogen receptor (ESR1). [69]
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⏷ Show the Full List of 6 Drug(s)
86 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Tretinoin DM49DUI Approved Tretinoin increases the expression of Estrogen receptor (ESR1). [4]
Doxorubicin DMVP5YE Approved Doxorubicin increases the expression of Estrogen receptor (ESR1). [5]
Estradiol DMUNTE3 Approved Estradiol decreases the expression of Estrogen receptor (ESR1). [6]
Ivermectin DMDBX5F Approved Ivermectin increases the expression of Estrogen receptor (ESR1). [7]
Arsenic DMTL2Y1 Approved Arsenic decreases the expression of Estrogen receptor (ESR1). [8]
Quercetin DM3NC4M Approved Quercetin decreases the expression of Estrogen receptor (ESR1). [9]
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide increases the expression of Estrogen receptor (ESR1). [11]
Calcitriol DM8ZVJ7 Approved Calcitriol increases the expression of Estrogen receptor (ESR1). [12]
Vorinostat DMWMPD4 Approved Vorinostat decreases the expression of Estrogen receptor (ESR1). [13]
Testosterone DM7HUNW Approved Testosterone decreases the expression of Estrogen receptor (ESR1). [14]
Triclosan DMZUR4N Approved Triclosan decreases the expression of Estrogen receptor (ESR1). [15]
Carbamazepine DMZOLBI Approved Carbamazepine decreases the expression of Estrogen receptor (ESR1). [16]
Decitabine DMQL8XJ Approved Decitabine decreases the expression of Estrogen receptor (ESR1). [17]
Marinol DM70IK5 Approved Marinol increases the expression of Estrogen receptor (ESR1). [18]
Progesterone DMUY35B Approved Progesterone decreases the expression of Estrogen receptor (ESR1). [19]
Fulvestrant DM0YZC6 Approved Fulvestrant decreases the expression of Estrogen receptor (ESR1). [21]
Dexamethasone DMMWZET Approved Dexamethasone decreases the expression of Estrogen receptor (ESR1). [22]
Hydroquinone DM6AVR4 Approved Hydroquinone decreases the expression of Estrogen receptor (ESR1). [23]
Diethylstilbestrol DMN3UXQ Approved Diethylstilbestrol increases the expression of Estrogen receptor (ESR1). [24]
Ethanol DMDRQZU Approved Ethanol increases the expression of Estrogen receptor (ESR1). [25]
Paclitaxel DMLB81S Approved Paclitaxel increases the expression of Estrogen receptor (ESR1). [26]
Diclofenac DMPIHLS Approved Diclofenac affects the activity of Estrogen receptor (ESR1). [27]
Nicotine DMWX5CO Approved Nicotine decreases the expression of Estrogen receptor (ESR1). [28]
Malathion DMXZ84M Approved Malathion decreases the activity of Estrogen receptor (ESR1). [29]
Permethrin DMZ0Q1G Approved Permethrin decreases the expression of Estrogen receptor (ESR1). [30]
Ethinyl estradiol DMODJ40 Approved Ethinyl estradiol increases the expression of Estrogen receptor (ESR1). [31]
Azacitidine DMTA5OE Approved Azacitidine increases the expression of Estrogen receptor (ESR1). [32]
Daunorubicin DMQUSBT Approved Daunorubicin decreases the activity of Estrogen receptor (ESR1). [33]
Liothyronine DM6IR3P Approved Liothyronine decreases the expression of Estrogen receptor (ESR1). [34]
Lindane DMB8CNL Approved Lindane decreases the expression of Estrogen receptor (ESR1). [21]
Ritonavir DMU764S Approved Ritonavir decreases the expression of Estrogen receptor (ESR1). [36]
Estrone DM5T6US Approved Estrone increases the expression of Estrogen receptor (ESR1). [31]
Melatonin DMKWFBT Approved Melatonin decreases the expression of Estrogen receptor (ESR1). [38]
Adenosine DMM2NSK Approved Adenosine increases the expression of Estrogen receptor (ESR1). [39]
Mestranol DMG3F94 Approved Mestranol increases the activity of Estrogen receptor (ESR1). [40]
Estriol DMOEM2I Approved Estriol increases the expression of Estrogen receptor (ESR1). [41]
Mitotane DMU1GX0 Approved Mitotane increases the activity of Estrogen receptor (ESR1). [42]
Nifedipine DMSVOZT Approved Nifedipine increases the activity of Estrogen receptor (ESR1). [33]
Lapatinib DM3BH1Y Approved Lapatinib decreases the activity of Estrogen receptor (ESR1). [43]
Prasterone DM67VKL Approved Prasterone increases the expression of Estrogen receptor (ESR1). [44]
Flutamide DMK0O7U Approved Flutamide increases the expression of Estrogen receptor (ESR1). [45]
Lidocaine DML4ZOT Approved Lidocaine increases the expression of Estrogen receptor (ESR1). [11]
Tibolone DM78XFG Approved Tibolone increases the activity of Estrogen receptor (ESR1). [46]
Chloramphenicol DMFXEWT Approved Chloramphenicol increases the expression of Estrogen receptor (ESR1). [11]
Felodipine DMOSW35 Approved Felodipine increases the activity of Estrogen receptor (ESR1). [33]
Hydralazine DMU8JGH Approved Hydralazine increases the expression of Estrogen receptor (ESR1). [47]
Procaine DM4LSNE Approved Procaine increases the expression of Estrogen receptor (ESR1). [11]
Idarubicin DMM0XGL Approved Idarubicin decreases the activity of Estrogen receptor (ESR1). [33]
ARZOXIFENE DMOKCVI Approved ARZOXIFENE decreases the activity of Estrogen receptor (ESR1). [48]
Nisoldipine DM7ISKJ Approved Nisoldipine decreases the activity of Estrogen receptor (ESR1). [33]
Goserelin DMAT8CG Approved Goserelin decreases the expression of Estrogen receptor (ESR1). [49]
Dienestrol DMBSXI0 Approved Dienestrol decreases the activity of Estrogen receptor (ESR1). [50]
Methyltestosterone DMWLFGO Approved Methyltestosterone increases the expression of Estrogen receptor (ESR1). [51]
Proflavine DMF1X5P Approved Proflavine increases the activity of Estrogen receptor (ESR1). [52]
Liraglutide DM3FXPS Approved Liraglutide increases the expression of Estrogen receptor (ESR1). [53]
Ospemifene DMC4GEI Approved Ospemifene decreases the expression of Estrogen receptor (ESR1). [54]
Dihydrotestosterone DM3S8XC Phase 4 Dihydrotestosterone increases the expression of Estrogen receptor (ESR1). [44]
Isoflavone DM7U58J Phase 4 Isoflavone increases the activity of Estrogen receptor (ESR1). [55]
Benidipine DMWNP6B Phase 4 Benidipine decreases the activity of Estrogen receptor (ESR1). [33]
Lacidipine DMQP5I3 Phase 4 Lacidipine increases the activity of Estrogen receptor (ESR1). [33]
Resveratrol DM3RWXL Phase 3 Resveratrol decreases the expression of Estrogen receptor (ESR1). [56]
Tamibarotene DM3G74J Phase 3 Tamibarotene increases the activity of Estrogen receptor (ESR1). [33]
Curcumin DMQPH29 Phase 3 Curcumin decreases the expression of Estrogen receptor (ESR1). [57]
I3C DMIGFOR Phase 3 I3C decreases the expression of Estrogen receptor (ESR1). [58]
EXISULIND DMBY56U Phase 3 EXISULIND decreases the expression of Estrogen receptor (ESR1). [59]
Manidipine DMJPGUA Phase 3 Manidipine decreases the activity of Estrogen receptor (ESR1). [33]
Cilnidipine DM1975O Phase 3 Cilnidipine decreases the activity of Estrogen receptor (ESR1). [33]
ABC294640 DMCKPG4 Phase 3 ABC294640 decreases the activity of Estrogen receptor (ESR1). [61]
Genistein DM0JETC Phase 2/3 Genistein decreases the expression of Estrogen receptor (ESR1). [9]
Phenol DM1QSM3 Phase 2/3 Phenol increases the expression of Estrogen receptor (ESR1). [11]
DNCB DMDTVYC Phase 2 DNCB affects the expression of Estrogen receptor (ESR1). [62]
Afimoxifene DMFORDT Phase 2 Afimoxifene decreases the activity of Estrogen receptor (ESR1). [63]
phorbol 12-myristate 13-acetate DMJWD62 Phase 2 phorbol 12-myristate 13-acetate decreases the expression of Estrogen receptor (ESR1). [64]
(Z)-endoxifen DMGDOS2 Phase 2 (Z)-endoxifen decreases the expression of Estrogen receptor (ESR1). [66]
Icaritin DMGHQ37 Phase 2 Icaritin increases the activity of Estrogen receptor (ESR1). [67]
ERB-041 DMCEPUA Phase 2 ERB-041 increases the activity of Estrogen receptor (ESR1). [42]
G1 DMTV42K Phase 1/2 G1 increases the expression of Estrogen receptor (ESR1). [44]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Estrogen receptor (ESR1). [70]
GSK525762 DMPAWBN Phase 1 GSK525762 decreases the expression of Estrogen receptor (ESR1). [71]
PMID28460551-Compound-2 DM4DOUB Patented PMID28460551-Compound-2 increases the expression of Estrogen receptor (ESR1). [72]
Phenolphthalein DM5SICT Withdrawn from market Phenolphthalein increases the activity of Estrogen receptor (ESR1). [50]
FORMESTANE DMWIDJK Withdrawn from market FORMESTANE increases the expression of Estrogen receptor (ESR1). [76]
Geldanamycin DMS7TC5 Discontinued in Phase 2 Geldanamycin decreases the expression of Estrogen receptor (ESR1). [77]
MX-4509 DMC4RK7 Discontinued in Phase 1 MX-4509 increases the expression of Estrogen receptor (ESR1). [51]
MG-132 DMKA2YS Preclinical MG-132 decreases the expression of Estrogen receptor (ESR1). [78]
Dioscin DM5H2W9 Preclinical Dioscin increases the expression of Estrogen receptor (ESR1). [79]
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⏷ Show the Full List of 86 Drug(s)
8 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT
Drug Name Drug ID Highest Status Interaction REF
Menadione DMSJDTY Approved Menadione affects the binding of Estrogen receptor (ESR1). [20]
Hexachlorophene DMLKSE0 Approved Hexachlorophene affects the binding of Estrogen receptor (ESR1). [20]
Guaiacol DMN4E7T Phase 3 Guaiacol affects the binding of Estrogen receptor (ESR1). [60]
BAICALEIN DM4C7E6 Phase 2 BAICALEIN affects the binding of Estrogen receptor (ESR1). [65]
Pyrethroids DM1794O Phase 2 Pyrethroids affects the binding of Estrogen receptor (ESR1). [68]
Eugenol DM7US1H Patented Eugenol affects the binding of Estrogen receptor (ESR1). [73]
Flavonoid derivative 1 DMCQP0B Patented Flavonoid derivative 1 affects the binding of Estrogen receptor (ESR1). [74]
HEXESTROL DM9AGWQ Withdrawn from market HEXESTROL affects the binding of Estrogen receptor (ESR1). [75]
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⏷ Show the Full List of 8 Drug(s)

References

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7 Selective Inhibition of SIN3 Corepressor with Avermectins as a Novel Therapeutic Strategy in Triple-Negative Breast Cancer. Mol Cancer Ther. 2015 Aug;14(8):1824-36. doi: 10.1158/1535-7163.MCT-14-0980-T. Epub 2015 Jun 15.
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10 [Arsenic trioxide restores ER expression in ER-negative human breast cancer cells and its treatment efficacy in combination with tamoxifen in xenografts in nude mice]. Zhonghua Zhong Liu Za Zhi. 2012 Sep;34(9):645-51. doi: 10.3760/cma.j.issn.0253-3766.2012.09.002.
11 Sensitivity of human dental pulp cells to eighteen chemical agents used for endodontic treatments in dentistry. Odontology. 2013 Jan;101(1):43-51.
12 Large-scale in silico and microarray-based identification of direct 1,25-dihydroxyvitamin D3 target genes. Mol Endocrinol. 2005 Nov;19(11):2685-95.
13 Histone deacetylase inhibitor SAHA induces ERalpha degradation in breast cancer MCF-7 cells by CHIP-mediated ubiquitin pathway and inhibits survival signaling. Biochem Pharmacol. 2008 May 1;75(9):1697-705. doi: 10.1016/j.bcp.2007.10.035. Epub 2007 Nov 9.
14 Expression of estrogen-, progesterone-, and androgen-responsive genes in MCF-7 and MDA-MB-231 cells treated with o,p'-DDT, p,p'-DDT, or endosulfan. J Biochem Mol Toxicol. 2021 Jun;35(6):1-8. doi: 10.1002/jbt.22773. Epub 2021 Mar 16.
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17 Trichostatin A and 5 Aza-2' deoxycytidine decrease estrogen receptor mRNA stability in ER positive MCF7 cells through modulation of HuR. Breast Cancer Res Treat. 2008 Sep;111(1):15-25. doi: 10.1007/s10549-007-9751-0. Epub 2007 Sep 21.
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