RRC ID 61270
著者 Kawabata S, Oka M, Shiozawa K, Tsukamoto K, Nakatomi K, Soda H, Fukuda M, Ikegami Y, Sugahara K, Yamada Y, Kamihira S, Doyle LA, Ross DD, Kohno S.
タイトル Breast cancer resistance protein directly confers SN-38 resistance of lung cancer cells.
ジャーナル Biochem Biophys Res Commun
Abstract Breast cancer resistance protein (BCRP), an ABC half-transporter, is overexpressed in cancer cell lines selected with doxorubicin/verapamil, topotecan, or mitoxantrone. BCRP-overexpressing cells show cross-resistance to camptothecin derivatives such as irinotecan, SN-38 (the active metabolite of irinotecan), and topotecan. To test whether BCRP confers SN-38 resistance, we selected two SN-38 resistant sublines from PC-6 human small-cell lung cancer cells by SN-38, and then characterized these cells. Compared to PC-6 cells, the resistant sublines PC-6/SN2-5 and PC-6/SN2-5H were approximately 18- and 34-fold resistant, respectively. The intracellular SN-38 accumulation was reduced in the sublines, and BCRP mRNA was overexpressed in proportion to the degree of SN-38 resistance. These findings suggest that BCRP confers SN-38 resistance in the sublines. To confirm this hypothesis, PC-6/SN2-5 cells were transfected with antisense oligonucleotides complementary to portions of BCRP mRNA. The antisense oligonucleotides significantly suppressed BCRP mRNA expression, and enhanced SN-38 sensitivity in the subline. These data indicate that BCRP is directly involved with SN-38 resistance, by efflux transport of SN-38.
巻・号 280(5)
ページ 1216-23
公開日 2001-2-9
DOI 10.1006/bbrc.2001.4267
PII S0006-291X(01)94267-6
PMID 11162657
MeSH ATP Binding Cassette Transporter, Subfamily G, Member 2 ATP-Binding Cassette Transporters / genetics* Antineoplastic Agents, Phytogenic / metabolism Antineoplastic Agents, Phytogenic / pharmacology* Blotting, Northern Caco-2 Cells Camptothecin / analogs & derivatives Camptothecin / metabolism Camptothecin / pharmacology* DNA, Antisense / genetics DNA, Antisense / physiology Drug Resistance, Neoplasm Gene Expression Regulation, Neoplastic Humans Irinotecan Lung Neoplasms / genetics* Lung Neoplasms / pathology Neoplasm Proteins* RNA, Messenger / drug effects RNA, Messenger / genetics RNA, Messenger / metabolism Transfection Tumor Cells, Cultured / drug effects
IF 2.985
オルトメトリクス指標
オルトメトリクス指標項目
最多言及媒体 Patent(IFI CLAIMS)
各媒体での言及数の合計 1
過去6か月間でのオルトメトリクス指標の変動値 0.0
リソース情報
ヒト・動物細胞 CACO-2(RCB0988) LoVo(RCB1639) MKN1(RCB1003) MKN7(RCB0999) MKN45(RCB1001) MKN74(RCB1002)