HUSCAP logo Hokkaido Univ. logo

Hokkaido University Collection of Scholarly and Academic Papers >
Faculty of Pharmaceutical Sciences >
Peer-reviewed Journal Articles, etc >

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

Files in This Item:
yamaguchi2008.pdf770.96 kBPDFView/Open
Please use this identifier to cite or link to this item:

Title: Rapid screening of antineoplastic candidates for the human organic anion transporter OATP1B3 substrates using fluorescent probes
Authors: Yamaguchi, Hiroaki Browse this author
Kobayashi, Minako Browse this author
Okada, Masahiro Browse this author
Takeuchi, Toshiko Browse this author
Unno, Michiaki Browse this author
Abe, Takaaki Browse this author
Goto, Junichi Browse this author
Hishinuma, Takanori Browse this author
Mano, Nariyasu Browse this author
Keywords: Antineoplastic drugs
Fluorescent substrate
Rapid screening
Issue Date: 18-Feb-2008
Publisher: Elsevier
Journal Title: Cancer Letters
Volume: 260
Issue: 1-2
Start Page: 163
End Page: 169
Publisher DOI: 10.1016/j.canlet.2007.10.040
PMID: 18082941
Abstract: 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.
Type: article (author version)
Appears in Collections:薬学研究院 (Faculty of Pharmaceutical Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 山口 浩明

Export metadata:

OAI-PMH ( junii2 , jpcoar_1.0 )

MathJax is now OFF:


 - Hokkaido University