m6A-centered Drug Response Information
General Information of the Drug (ID: M6ADRUG0039)
Name |
Tamoxifen
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Synonyms |
tamoxifen; 10540-29-1; trans-Tamoxifen; Crisafeno; Soltamox; Tamoxifene; Diemon; Tamoxifenum; Tamoxifeno; Tamizam; Istubol; Tamoxen; Citofen; Oncomox; Valodex; Retaxim; Tamoxifene [INN-French]; Tamoxifenum [INN-Latin]; Tamoxifeno [INN-Spanish]; Tamoxifen (Z); Tamoxifen and its salts; Tamoxifen [INN:BAN]; ICI-46474; ICI 47699; TRANS FORM OF TAMOXIFEN; CCRIS 3275; UNII-094ZI81Y45; HSDB 6782; CHEMBL83; EINECS 234-118-0; 1-p-beta-Dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene; Citofen; Nourytam; Novaldex; Tamone; Tamoxifeno;Tamoxifenum; Tomaxithen; Gen-Tamoxifen; Istubal (TN); Nolvadex (TN); Nolvadex-D; Novo-Tamoxifen; Pms-Tamoxifen; Tamoplex (TN); Tamoxifen (INN); Tamoxifen (TN); Trans-Tamoxifen; Valodex (TN); TAMOXIFEN (TAMOXIFEN CITRATE (54965-24-1)); Trans-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine; (Z)-1-(p-Dimethylaminoethoxyphenyl)-1,2-diphenyl-1-butene; (Z)-2-(4-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N-dimethylethanamine; (Z)-2-(4-(1,2-diphenylbut-1-enyl)phenoxy)-N,N-dimethylethanamine; (Z)-2-(para-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N-dimethylamine (IUPAC); (Z)-2-[4-(1,2)-DIPHENYL-1-BUTENYL)-PHENOXY]-N,N-DIMETHYLETHANAMINE; (Z)-2-[p-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine; 1-p-beta-Dimethylamino-ethoxyphenyl-trans-1,2-diphenylbut-1-ene; 1-para-beta-Dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene; 2-[4-[(Z)-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethylethanamine; 2-{4-[(1Z)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine; Tamoxifen (Hormonal therapy); [3H]tamoxifen
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Status | Approved | [1] | |||
Structure |
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Formula |
C26H29NO
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InChI |
InChI=1S/C26H29NO/c1-4-25(21-11-7-5-8-12-21)26(22-13-9-6-10-14-22)23-15-17-24(18-16-23)28-20-19-27(2)3/h5-18H,4,19-20H2,1-3H3/b26-25-
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InChIKey |
NKANXQFJJICGDU-QPLCGJKRSA-N
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PubChem CID | |||||
TTD Drug ID | |||||
DrugBank ID |
Full List of m6A Targets Related to This Drug
Adenylate kinase 4, mitochondrial (AK4)
In total 1 item(s) under this target gene | ||||
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [2] | |||
Response Summary | Adenylate kinase 4 modulates the resistance of breast cancer cells to tamoxifen through an m6A-based epitranscriptomic mechanism. Genetic depletion of METTL3 in TamR MCF-7 cells led to a diminished Adenylate kinase 4, mitochondrial (AK4) protein level and attenuated resistance to tamoxifen. | |||
Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
Target Regulator | Methyltransferase-like 3 (METTL3) | WRITER | ||
Target Regulation | Up regulation | |||
Cell Process | Mitochondrial apoptosis | |||
In-vitro Model | MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 |
MCF7-TamR | Invasive breast carcinoma | Homo sapiens | CVCL_EG55 | |
Mitogen-activated protein kinase 1 (MAPK/ERK2/MAPK1)
In total 1 item(s) under this target gene | ||||
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [3] | |||
Response Summary | In breast cancer, modest stable overexpression of A2B1 in MCF-7 cells (MCF-7-A2B1 cells) resulted in tamoxifen and fulvestrant - resistance whereas knockdown of A2B1 in LCC9 and LY2 cells restored tamoxifen and fulvestrant, endocrine-sensitivity. MCF-7-A2B1 cells have increased ER-alpha and reduced miR-222-3p that targets ER-alpha. MCF-7-A2B1 have activated AKT and Mitogen-activated protein kinase 1 (MAPK/ERK2/MAPK1) that depend on A2B1 expression and are growth inhibited by inhibitors of these pathways. | |||
Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
Target Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | READER | ||
Target Regulation | Up regulation | |||
Pathway Response | MAPK signaling pathway | hsa04010 | ||
PI3K-Akt signaling pathway | hsa04151 | |||
Cell Process | Cell migration and invasion | |||
In-vitro Model | HCC1806 | Breast squamous cell carcinoma | Homo sapiens | CVCL_1258 |
MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 | |
MDA-MB-231 | Breast adenocarcinoma | Homo sapiens | CVCL_0062 | |
MDA-MB-468 | Breast adenocarcinoma | Homo sapiens | CVCL_0419 | |
T-47D | Invasive breast carcinoma | Homo sapiens | CVCL_0553 | |
Myc proto-oncogene protein (MYC)
In total 1 item(s) under this target gene | ||||
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [4] | |||
Response Summary | LCAT3 upregulation is attributable to m6A modification mediated by METTL3, leading to LCAT3 stabilization. Treated cells with tamoxifen to induce MYC activity. Highlights the therapeutic potential of RBPs by uncovering a critical role for YTHDF2 in counteracting the global increase of mRNA synthesis in Myc proto-oncogene protein (MYC)-driven breast cancers. | |||
Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
Target Regulator | YTH domain-containing family protein 2 (YTHDF2) | READER | ||
Pathway Response | MAPK signaling pathway | hsa04010 | ||
Cell Process | Epithelial-to-mesenchymal transition | |||
Cell apoptosis | ||||
In-vitro Model | HEK293T | Normal | Homo sapiens | CVCL_0063 |
MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 | |
MDA-MB-231 | Breast adenocarcinoma | Homo sapiens | CVCL_0062 | |
MBA-MD-231 (Human breast cancer cell) | ||||
MYC-ER HMEC (Human mammary epithelial cells expressing a MYC estrogen receptor fusion) | ||||
SK-BR-3 | Breast adenocarcinoma | Homo sapiens | CVCL_0033 | |
In-vivo Model | To induce recombination at 8 weeks of age both CAG-CreERT;Ythdf2fl/fl and Ythdf2fl/fl littermates were injected with 75mg/kg body weight tamoxifen dissolved in corn oil daily for 5 days. | |||
RAC-alpha serine/threonine-protein kinase (AKT1)
In total 1 item(s) under this target gene | ||||
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [3] | |||
Response Summary | In breast cancer, modest stable overexpression of A2B1 in MCF-7 cells (MCF-7-A2B1 cells) resulted in tamoxifen and fulvestrant - resistance whereas knockdown of A2B1 in LCC9 and LY2 cells restored tamoxifen and fulvestrant, endocrine-sensitivity. MCF-7-A2B1 cells have increased ER-alpha and reduced miR-222-3p that targets ER-alpha. MCF-7-A2B1 have activated RAC-alpha serine/threonine-protein kinase (AKT1) and MAPK that depend on A2B1 expression and are growth inhibited by inhibitors of these pathways. | |||
Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
Target Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | READER | ||
Target Regulation | Up regulation | |||
Pathway Response | MAPK signaling pathway | hsa04010 | ||
PI3K-Akt signaling pathway | hsa04151 | |||
Cell Process | Cell migration and invasion | |||
In-vitro Model | HCC1806 | Breast squamous cell carcinoma | Homo sapiens | CVCL_1258 |
MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 | |
MDA-MB-231 | Breast adenocarcinoma | Homo sapiens | CVCL_0062 | |
MDA-MB-468 | Breast adenocarcinoma | Homo sapiens | CVCL_0419 | |
T-47D | Invasive breast carcinoma | Homo sapiens | CVCL_0553 | |
Ribonuclease 3 (DROSHA)
In total 1 item(s) under this target gene | ||||
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [5] | |||
Response Summary | HNRNPA2B1 is a reader of the N(6)-methyladenosine mark in primary-miRNAs and promotes Ribonuclease 3 (DROSHA) processing to precursor-miRNAs. HNRNPA2B1 downregulated miR-29a-3p, miR-29b-3p, and miR-222 and upregulated miR-1266-5p, miR-1268a, miR-671-3p. Transient overexpression of HNRNPA2/B1 reduced breast cancer cellMCF-7 sensitivity to 4-hydroxytamoxifen and fulvestrant, suggesting a role for HNRNPA2/B1 in endocrine-resistance. | |||
Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
Target Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | READER | ||
Target Regulation | Up regulation | |||
Pathway Response | TGF-beta signaling pathway | hsa04350 | ||
Cell Process | Endocrine-resistance | |||
In-vitro Model | MCF7/LCC9 | Invasive breast carcinoma | Homo sapiens | CVCL_DP52 |
MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 | |
microRNA 222 (MIR222)
In total 1 item(s) under this target gene | ||||
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [5] | |||
Response Summary | HNRNPA2B1 is a reader of the N(6)-methyladenosine mark in primary-miRNAs and promotes DROSHA processing to precursor-miRNAs. HNRNPA2B1 downregulated miR-29a-3p, miR-29b-3p, and microRNA 222 (MIR222) and upregulated miR-1266-5p, miR-1268a, miR-671-3p. Transient overexpression of HNRNPA2/B1 reduced breast cancer cellMCF-7 sensitivity to 4-hydroxytamoxifen and fulvestrant, suggesting a role for HNRNPA2/B1 in endocrine-resistance. | |||
Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
Target Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | READER | ||
Target Regulation | Down regulation | |||
Pathway Response | TGF-beta signaling pathway | hsa04350 | ||
Cell Process | Endocrine-resistance | |||
In-vitro Model | MCF7/LCC9 | Invasive breast carcinoma | Homo sapiens | CVCL_DP52 |
MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 | |
hsa-miR-1266-5p
In total 1 item(s) under this target gene | ||||
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [5] | |||
Response Summary | HNRNPA2B1 is a reader of the N(6)-methyladenosine mark in primary-miRNAs and promotes DROSHA processing to precursor-miRNAs. HNRNPA2B1 downregulated miR-29a-3p, miR-29b-3p, and miR-222 and upregulated hsa-miR-1266-5p, miR-1268a, miR-671-3p. Transient overexpression of HNRNPA2/B1 reduced breast cancer cellMCF-7 sensitivity to 4-hydroxytamoxifen and fulvestrant, suggesting a role for HNRNPA2/B1 in endocrine-resistance. | |||
Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
Target Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | READER | ||
Target Regulation | Up regulation | |||
Pathway Response | TGF-beta signaling pathway | hsa04350 | ||
Cell Process | Endocrine-resistance | |||
In-vitro Model | MCF7/LCC9 | Invasive breast carcinoma | Homo sapiens | CVCL_DP52 |
MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 | |
hsa-miR-1268a
In total 1 item(s) under this target gene | ||||
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [5] | |||
Response Summary | HNRNPA2B1 is a reader of the N(6)-methyladenosine mark in primary-miRNAs and promotes DROSHA processing to precursor-miRNAs. HNRNPA2B1 downregulated miR-29a-3p, miR-29b-3p, and miR-222 and upregulated miR-1266-5p, hsa-miR-1268a, miR-671-3p. Transient overexpression of HNRNPA2/B1 reduced breast cancer cellMCF-7 sensitivity to 4-hydroxytamoxifen and fulvestrant, suggesting a role for HNRNPA2/B1 in endocrine-resistance. | |||
Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
Target Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | READER | ||
Target Regulation | Up regulation | |||
Pathway Response | TGF-beta signaling pathway | hsa04350 | ||
Cell Process | Endocrine-resistance | |||
In-vitro Model | MCF7/LCC9 | Invasive breast carcinoma | Homo sapiens | CVCL_DP52 |
MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 | |
hsa-miR-29a-3p
In total 1 item(s) under this target gene | ||||
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [5] | |||
Response Summary | HNRNPA2B1 is a reader of the N(6)-methyladenosine mark in primary-miRNAs and promotes DROSHA processing to precursor-miRNAs. HNRNPA2B1 downregulated hsa-miR-29a-3p, miR-29b-3p, and miR-222 and upregulated miR-1266-5p, miR-1268a, miR-671-3p. Transient overexpression of HNRNPA2/B1 reduced breast cancer cellMCF-7 sensitivity to 4-hydroxytamoxifen and fulvestrant, suggesting a role for HNRNPA2/B1 in endocrine-resistance. | |||
Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
Target Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | READER | ||
Target Regulation | Down regulation | |||
Pathway Response | TGF-beta signaling pathway | hsa04350 | ||
Cell Process | Endocrine-resistance | |||
In-vitro Model | MCF7/LCC9 | Invasive breast carcinoma | Homo sapiens | CVCL_DP52 |
MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 | |
hsa-miR-29b-3p
In total 1 item(s) under this target gene | ||||
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [5] | |||
Response Summary | HNRNPA2B1 is a reader of the N(6)-methyladenosine mark in primary-miRNAs and promotes DROSHA processing to precursor-miRNAs. HNRNPA2B1 downregulated miR-29a-3p, hsa-miR-29b-3p, and miR-222 and upregulated miR-1266-5p, miR-1268a, miR-671-3p. Transient overexpression of HNRNPA2/B1 reduced breast cancer cellMCF-7 sensitivity to 4-hydroxytamoxifen and fulvestrant, suggesting a role for HNRNPA2/B1 in endocrine-resistance. | |||
Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
Target Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | READER | ||
Target Regulation | Down regulation | |||
Pathway Response | TGF-beta signaling pathway | hsa04350 | ||
Cell Process | Endocrine-resistance | |||
In-vitro Model | MCF7/LCC9 | Invasive breast carcinoma | Homo sapiens | CVCL_DP52 |
MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 | |
hsa-miR-671-3p
In total 1 item(s) under this target gene | ||||
Experiment 1 Reporting the m6A-centered Drug Response by This Target Gene | [5] | |||
Response Summary | HNRNPA2B1 is a reader of the N(6)-methyladenosine mark in primary-miRNAs and promotes DROSHA processing to precursor-miRNAs. HNRNPA2B1 downregulated miR-29a-3p, miR-29b-3p, and miR-222 and upregulated miR-1266-5p, miR-1268a, hsa-miR-671-3p. Transient overexpression of HNRNPA2/B1 reduced breast cancer cellMCF-7 sensitivity to 4-hydroxytamoxifen and fulvestrant, suggesting a role for HNRNPA2/B1 in endocrine-resistance. | |||
Responsed Disease | Breast cancer | ICD-11: 2C60 | ||
Target Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | READER | ||
Target Regulation | Up regulation | |||
Pathway Response | TGF-beta signaling pathway | hsa04350 | ||
Cell Process | Endocrine-resistance | |||
In-vitro Model | MCF7/LCC9 | Invasive breast carcinoma | Homo sapiens | CVCL_DP52 |
MCF-7 | Invasive breast carcinoma | Homo sapiens | CVCL_0031 | |
References