Rapid screening of antineoplastic candidates for the human organic anion transporter OATP1B3 substrates using fluorescent probes

Yamaguchi, Hiroaki; Kobayashi, Minako; Okada, Masahiro; Takeuchi, Toshiko; Unno, Michiaki; Abe, Takaaki; Goto, Junichi; Hishinuma, Takanori; Mano, Nariyasu

Rapid screening of antineoplastic candidates for the human organic anion transporter OATP1B3 substrates using fluorescent probes

Yamaguchi, Hiroaki; Kobayashi, Minako; Okada, Masahiro et al.

Cancer Letters, 2008, 260(1-2), 163-169

Permalink : https://hdl.handle.net/2115/43859

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アクセス権	open access
URI	https://hdl.handle.net/2115/43859
タイトル	Rapid screening of antineoplastic candidates for the human organic anion transporter OATP1B3 substrates using fluorescent probes
著者	Yamaguchi, Hiroaki ; Kobayashi, Minako ; Okada, Masahiro ; Takeuchi, Toshiko ; Unno, Michiaki ; Abe, Takaaki ; Goto, Junichi ; Hishinuma, Takanori ; Mano, Nariyasu
著者名 Yamaguchi, Hiroaki
著者名 Kobayashi, Minako
著者名 Okada, Masahiro
著者名 Takeuchi, Toshiko
著者名 Unno, Michiaki
著者名 Abe, Takaaki
著者名 Goto, Junichi
著者名 Hishinuma, Takanori
著者名 Mano, Nariyasu
言語	英語
キーワード	Antineoplastic drugs
	Fluorescent substrate
	Imaging
	OATP1B3
	Rapid screening
発行日	2008-02-18
出版者	Elsevier
収録物名	Cancer Letters
巻(号)	260(1-2)
ページ	163-169
抄録	A rapid screening system has been established to extract novel candidates that exhibit potent inhibition of the transport of fluorescent substrate by organic anion transporting polypeptide (OATP) 1B3. OATP1B3 is abundantly expressed in solid digestive organ cancers. Thus, the identification of new substrates leads to novel strategies for effective cancer chemotherapy with minimal adverse effects. We used an automated image acquisition and analysis system (IN Cell Analyzer 1000) to visualize the transport and subsequent accumulation of the fluorescent substrate chenodeoxycholyl-(Nε-NBD)-lysine (CDCA-NBD). Antineoplastic screening demonstrated that five candidates agents, docetaxel, actinomycin D, mitoxantrone, paclitaxel, and SN-38, exhibited potent inhibitory effects on OATP1B3-mediated transport of CDCA-NBD. To clarify if these antineoplastic drugs are substrates for OATP1B3, we performed transport assays in OATP1B3-expressing cells. We determined that SN-38 is a novel substrate for OATP1B3. In conclusion, our results demonstrate that the screening system established in this study is a useful method for the rapid extraction of candidate therapeutic agents from the large numbers of compounds.
資源タイプ	学術雑誌論文
出版タイプ	Accepted Manuscript
PISSN	0304-3835
関連情報	PMID 18082941
関連情報 (isVersionOf)	出版社版DOI https://doi.org/10.1016/j.canlet.2007.10.040