m6A-centered Drug Response Information
General Information of the Drug (ID: M6ADRUG0028)
| Name |
Fulvestrant
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| Synonyms |
Faslodex; AstraZeneca brand of fulvestrant; Fulvestrant [USAN]; Ici 182780; ZD 182780; ZM 182780; Faslodex (TN); ZD-182780; ZD-9238; ZM-182780; Faslodex(ICI 182,780); Faslodex, ICI 182780, Fulvestrant; Fulvestrant (JAN/USAN/INN); (7R,13S,17S)-13-methyl-7-(9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol; (7R,8R,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol; (7R,8S,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl) nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol; (7alpha,17beta)-7-{9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl}estra-1,3,5(10)-triene-3,17-diol; 7-(9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl)estra-1,3,5(10)-triene-3,17-diol; 7alpha-(9-((4,4,5,5,5,-Pentafluoropentyl)sulfinyl)nonyl)estra-1,3,5(10)-triene-3,17beta-diol; 7alpha-(9-((4,4,5,5,5-Pentafluoropentyl)sulfinyl)nonyl)estra-1,3,5(10)-triene-3,17beta-diol; 7alpha-[9[(4,4,5,5,5-Pentafluropentyl)sulfinyl]nonyl]-estra-1,3,5(10)-triene-3, 17 beta diol; ICI
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| Status | Approved | [1] | |||
| Structure |
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| Formula |
C32H47F5O3S
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| InChI |
InChI=1S/C32H47F5O3S/c1-30-17-15-26-25-12-11-24(38)21-23(25)20-22(29(26)27(30)13-14-28(30)39)10-7-5-3-2-4-6-8-18-41(40)19-9-16-31(33,34)32(35,36)37/h11-12,21-22,26-29,38-39H,2-10,13-20H2,1H3/t22-,26-,27+,28+,29-,30+,41/m1/s1
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| InChIKey |
VWUXBMIQPBEWFH-WCCTWKNTSA-N
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| TTD Drug ID | |||||
| DrugBank ID | |||||
Full List of m6A Targets Related to This Drug
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 | [2] | |||
| 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 | |
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 | [2] | |||
| 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 | [3] | |||
| 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 | [3] | |||
| 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 | [3] | |||
| 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 | [3] | |||
| 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 | [3] | |||
| 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 | [3] | |||
| 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 | [3] | |||
| 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 | |
Full List of Crosstalk(s) between m6A Modification and Epigenetic Regulation Related to This Drug
| In total 15 item(s) under this drug | ||
| Crosstalk ID: M6ACROT05129 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | hsa-miR-29a-3p | |
| Epigenetic Regulator | Prostate cancer associated transcript 6 (PCAT6) | |
| Regulated Target | Heterogeneous nuclear ribonucleoprotein A2/B1 (HNRNPA2B1) | |
| Crosstalk relationship | ncRNA → m6A | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05130 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | hsa-miR-29b-3p | |
| Epigenetic Regulator | Prostate cancer associated transcript 6 (PCAT6) | |
| Regulated Target | Heterogeneous nuclear ribonucleoprotein A2/B1 (HNRNPA2B1) | |
| Crosstalk relationship | ncRNA → m6A | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05131 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | microRNA 222 (MIR222) | |
| Epigenetic Regulator | Prostate cancer associated transcript 6 (PCAT6) | |
| Regulated Target | Heterogeneous nuclear ribonucleoprotein A2/B1 (HNRNPA2B1) | |
| Crosstalk relationship | ncRNA → m6A | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05132 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | hsa-miR-1266-5p | |
| Epigenetic Regulator | Prostate cancer associated transcript 6 (PCAT6) | |
| Regulated Target | Heterogeneous nuclear ribonucleoprotein A2/B1 (HNRNPA2B1) | |
| Crosstalk relationship | ncRNA → m6A | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05133 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | hsa-miR-1268a | |
| Epigenetic Regulator | Prostate cancer associated transcript 6 (PCAT6) | |
| Regulated Target | Heterogeneous nuclear ribonucleoprotein A2/B1 (HNRNPA2B1) | |
| Crosstalk relationship | ncRNA → m6A | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05134 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | hsa-miR-671-3p | |
| Epigenetic Regulator | Prostate cancer associated transcript 6 (PCAT6) | |
| Regulated Target | Heterogeneous nuclear ribonucleoprotein A2/B1 (HNRNPA2B1) | |
| Crosstalk relationship | ncRNA → m6A | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05142 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | Ribonuclease 3 (DROSHA) | |
| Epigenetic Regulator | Prostate cancer associated transcript 6 (PCAT6) | |
| Regulated Target | Heterogeneous nuclear ribonucleoprotein A2/B1 (HNRNPA2B1) | |
| Crosstalk relationship | ncRNA → m6A | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05145 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | RAC-alpha serine/threonine-protein kinase (AKT1) | |
| Epigenetic Regulator | Prostate cancer associated transcript 6 (PCAT6) | |
| Regulated Target | Heterogeneous nuclear ribonucleoprotein A2/B1 (HNRNPA2B1) | |
| Crosstalk relationship | ncRNA → m6A | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05146 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | Mitogen-activated protein kinase 1 (MAPK/ERK2/MAPK1) | |
| Epigenetic Regulator | Prostate cancer associated transcript 6 (PCAT6) | |
| Regulated Target | Heterogeneous nuclear ribonucleoprotein A2/B1 (HNRNPA2B1) | |
| Crosstalk relationship | ncRNA → m6A | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05389 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | hsa-miR-29a-3p | |
| Epigenetic Regulator | hsa-miR-29a-3p | |
| Crosstalk relationship | m6A → ncRNA | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05390 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | hsa-miR-29b-3p | |
| Epigenetic Regulator | hsa-miR-29b-3p | |
| Crosstalk relationship | m6A → ncRNA | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05391 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | microRNA 222 (MIR222) | |
| Epigenetic Regulator | MicroRNA 222 (MIR222) | |
| Crosstalk relationship | m6A → ncRNA | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05392 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | hsa-miR-1266-5p | |
| Epigenetic Regulator | hsa-miR-1266-5p | |
| Crosstalk relationship | m6A → ncRNA | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05393 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | hsa-miR-1268a | |
| Epigenetic Regulator | hsa-miR-1268a | |
| Crosstalk relationship | m6A → ncRNA | |
| Disease | Breast cancer | |
| Crosstalk ID: M6ACROT05394 | ||
| m6A Regulator | Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) | |
| m6A Target | hsa-miR-671-3p | |
| Epigenetic Regulator | hsa-miR-671-3p | |
| Crosstalk relationship | m6A → ncRNA | |
| Disease | Breast cancer | |
References