TY - JOUR
T1 - Estrone and 17β-estradiol reverse breast cancer resistance protein-mediated multidrug resistance
AU - Imai, Yasuo
AU - Tsukahara, Satomi
AU - Ishikawa, Etsuko
AU - Tsuruo, Takashi
AU - Sugimoto, Yoshikazu
PY - 2002
Y1 - 2002
N2 - Breast cancer resistance protein (BCRP), an adenosine triphosphate-binding cassette transporter, confers resistance to a series of anticancer reagents, including mitoxantrone, SN-38 and topotecan. In the present study, we found that estrone and 17β-estradiol potentiated the cytotoxicity of mitoxantrone, SN-38 and topotecan in BCRP-transduced K562 cells (K562/BCRP). These estrogens showed only a marginal effect, or none, in parental K562 cells. Estrone and 17β-estradiol increased the cellular accumulation of topotecan in K562/BCRP cells, but not in K562 cells, suggesting that these estrogens inhibit the BCRP-mediated drug efflux and overcome drug resistance.
AB - Breast cancer resistance protein (BCRP), an adenosine triphosphate-binding cassette transporter, confers resistance to a series of anticancer reagents, including mitoxantrone, SN-38 and topotecan. In the present study, we found that estrone and 17β-estradiol potentiated the cytotoxicity of mitoxantrone, SN-38 and topotecan in BCRP-transduced K562 cells (K562/BCRP). These estrogens showed only a marginal effect, or none, in parental K562 cells. Estrone and 17β-estradiol increased the cellular accumulation of topotecan in K562/BCRP cells, but not in K562 cells, suggesting that these estrogens inhibit the BCRP-mediated drug efflux and overcome drug resistance.
KW - 17β-estradiol
KW - BCRP
KW - Estrone
KW - MDR
KW - Reversal of drug resistance
UR - http://www.scopus.com/inward/record.url?scp=0036011103&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0036011103&partnerID=8YFLogxK
U2 - 10.1111/j.1349-7006.2002.tb02162.x
DO - 10.1111/j.1349-7006.2002.tb02162.x
M3 - Article
C2 - 11927002
AN - SCOPUS:0036011103
VL - 93
SP - 231
EP - 235
JO - Cancer Science
JF - Cancer Science
SN - 1347-9032
IS - 3
ER -
