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Estrogen Down-regulator Fulvestrant Potentiates Antitumor Activity of Fluoropyrimidine in Estrogen-responsive MCF-7 Human Breast Cancer Cells
by
TAKECHI, TEIJI
, NUKATSUKA, MAMORU
, SAITO, HITOSHI
, NOGUCHI, SHINZABURO
in
Animals
/ Antibodies
/ Antineoplastic Agents, Hormonal - pharmacology
/ Breast cancer
/ Breast Neoplasms - metabolism
/ Cancer therapies
/ Cell growth
/ Cell Line, Tumor
/ Cell Proliferation - drug effects
/ Clinical trials
/ Cloning
/ Cyclin-dependent kinases
/ Dose-Response Relationship, Drug
/ Drug Resistance, Neoplasm - drug effects
/ Drug Synergism
/ Endocrine therapy
/ Estrogen Receptor Antagonists - pharmacology
/ Estrogens
/ Estrogens - metabolism
/ Estrogens - pharmacology
/ Female
/ Fulvestrant - pharmacology
/ Humans
/ Kinases
/ Mice
/ Potassium
/ Pyrimidines - pharmacology
/ Toxicity
2019
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Estrogen Down-regulator Fulvestrant Potentiates Antitumor Activity of Fluoropyrimidine in Estrogen-responsive MCF-7 Human Breast Cancer Cells
by
TAKECHI, TEIJI
, NUKATSUKA, MAMORU
, SAITO, HITOSHI
, NOGUCHI, SHINZABURO
in
Animals
/ Antibodies
/ Antineoplastic Agents, Hormonal - pharmacology
/ Breast cancer
/ Breast Neoplasms - metabolism
/ Cancer therapies
/ Cell growth
/ Cell Line, Tumor
/ Cell Proliferation - drug effects
/ Clinical trials
/ Cloning
/ Cyclin-dependent kinases
/ Dose-Response Relationship, Drug
/ Drug Resistance, Neoplasm - drug effects
/ Drug Synergism
/ Endocrine therapy
/ Estrogen Receptor Antagonists - pharmacology
/ Estrogens
/ Estrogens - metabolism
/ Estrogens - pharmacology
/ Female
/ Fulvestrant - pharmacology
/ Humans
/ Kinases
/ Mice
/ Potassium
/ Pyrimidines - pharmacology
/ Toxicity
2019
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Estrogen Down-regulator Fulvestrant Potentiates Antitumor Activity of Fluoropyrimidine in Estrogen-responsive MCF-7 Human Breast Cancer Cells
by
TAKECHI, TEIJI
, NUKATSUKA, MAMORU
, SAITO, HITOSHI
, NOGUCHI, SHINZABURO
in
Animals
/ Antibodies
/ Antineoplastic Agents, Hormonal - pharmacology
/ Breast cancer
/ Breast Neoplasms - metabolism
/ Cancer therapies
/ Cell growth
/ Cell Line, Tumor
/ Cell Proliferation - drug effects
/ Clinical trials
/ Cloning
/ Cyclin-dependent kinases
/ Dose-Response Relationship, Drug
/ Drug Resistance, Neoplasm - drug effects
/ Drug Synergism
/ Endocrine therapy
/ Estrogen Receptor Antagonists - pharmacology
/ Estrogens
/ Estrogens - metabolism
/ Estrogens - pharmacology
/ Female
/ Fulvestrant - pharmacology
/ Humans
/ Kinases
/ Mice
/ Potassium
/ Pyrimidines - pharmacology
/ Toxicity
2019
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Estrogen Down-regulator Fulvestrant Potentiates Antitumor Activity of Fluoropyrimidine in Estrogen-responsive MCF-7 Human Breast Cancer Cells
Journal Article
Estrogen Down-regulator Fulvestrant Potentiates Antitumor Activity of Fluoropyrimidine in Estrogen-responsive MCF-7 Human Breast Cancer Cells
2019
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Overview
Endocrine therapy is clinically administered in hormone-responsive breast cancer. Combinations of fluoropyrimidine S-1 and an aromatase inhibitor or anti-estrogen are considered beneficial in Japan. Herein we assessed new combinations of S-1 and fulvestrant.
Cytotoxicity of fulvestrant and 5-fluorouracil (5-FU) was assessed in hormone-responsive (MCF-7) and non-responsive (MDA-MB-231) breast cancer cell cultures. Fulvestrant and S-1 were evaluated for antitumor activity in mice and their effects on estrogen receptor (ER)-α and progesterone receptor (PgR) levels in MCF-7 xenografts using immunohistochemical methods.
Fulvestrant inhibited growth of MCF-7, but not of MDA-MB-231 xenografts. Combinations of 5-FU and fulvestrant were superior to monotherapy in vitro. In vivo antitumor activity of S-1/fulvestrant combination therapy was significantly (p<0.05) enhanced compared to that of both monotherapies. Fulvestrant partially down-regulated expression of ERα and PgR, but in combination with S-1, it almost completely blocked their expression.
Chemo-endocrine combination therapy using S-1 and fulvestrant is beneficial in estrogen-responsive breast cancer.
Publisher
International Institute of Anticancer Research
Subject
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