Development of novel assay system for the functionality of organic cation transporters using fluorescent probe substrate

• Project/Area Number: 21790155
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Single-year Grants
• Research Field: Medical pharmacy
• Research Institution: Nagoya City University
• Principal Investigator: OHTA Kinya Nagoya City University, 大学院・薬学研究科, 助教 (90448704)
• Project Period (FY): 2009 – 2010
• Project Status: Completed (Fiscal Year 2010)
• Budget Amount: ¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000); Fiscal Year 2010: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000); Fiscal Year 2009: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
• Keywords: 医療薬剤学 / トランスポーター / 有機カチオン / 蛍光 / スクリーニング / 薬物間相互作用 / 薬物動態

Research Abstract

We successfully demonstrated that DAPI can be efficiently transported by both hMATEs, hMATE1 and hMATE2-K, and hOCT1. By taking advantage of its fluorescent nature, we developed a rapid assay system for the selection of inhibitors, which include potential substrates, of hMATEs and hOCT1.

Research Products

• [Journal Article] Evaluation of 4',6-diamidino-2-phenylindole as a fluorescent probe substrate for rapid assays of the functionality of human multidrug and toxin extrusion proteins. (2010)
  • Author(s): Tomoya Yasujima, Kinya Ohta, Katsuhisa Inoue, Munenori Ishimaru, Hiroaki Yuasa
  • Journal Title: Drug Metab. Dispos. 38 Pages: 715-721
• [Journal Article] Evaluation of 4',6-diamidino-2-phenylindole as a fluorescent probe substrate for rapid assays of the functionality of human multidrug and toxin extrusion proteins. (2010)
  • Author(s): Yasujima T., et al.
  • Journal Title: Drug Metabolism and Disposition 38 Pages: 715-721
  • Peer Reviewed
• [Journal Article] Characterization of human OCT1-mediated transport of DAPI as a fluorescent probe substrate.
  • Author(s): Tomoya Yasujima, Kinya Ohta, Katsuhisa Inoue, Hiroaki Yuasa
  • Journal Title: J. Pharm. Sci. in press.
  • NAID: 130004639870
• [Journal Article] Characterization of human OCT1-mediated transport of DAPI as a fluorescent probe substrate
  • Author(s): Yasujima T., et al.
  • Journal Title: Journal of Pharmaceutical Sciences Volume: (in press)
  • Peer Reviewed
• [Presentation] hOCT1による蛍光性核染色剤DAPIの輸送:迅速機能評価への応用の可能性 (2010)
  • Author(s): 保嶋智也, 他
  • Organizer: 日本薬学会第130年会
  • Place of Presentation: 岡山
  • Year and Date: 2010-03-28
• [Presentation] Rapid screening of inhibitors for human organic cation transporter 1 using DAPI. (2010)
  • Author(s): Tomoya Yasujima, Kinya Ohta, Katsuhisa Inoue, Hiroaki Yuasa
  • Organizer: 第4回次世代を担う若手医療薬科学シンポジウム,要旨集,p.77(P32).
  • Place of Presentation: 東京
• [Presentation] Characterization of the transport of DAPI by hOCT1 for its utilization for rapid uptake assays. (2010)
  • Author(s): Tomoya Yasujima, Kinya Ohta, Katsuhisa Inoue, Hiroaki Yuasa
  • Organizer: Pharmaceutical Sciences World Congress 2010 (4th),AAPS J, 12(S2), Abstract T3402.
  • Place of Presentation: New Orleans, Louisiana, U.S.A.
• [Presentation] ヒトOCT1の蛍光性プローブ基質としてのDAPIの輸送特性の評価. (2010)
  • Author(s): 保嶋智也, 太田欣哉, 井上勝央, 湯浅博昭
  • Organizer: 第25回日本薬物動態学会年会,要旨集,p.267(1-P-17).
  • Place of Presentation: さいたま
• [Presentation] hOCT1による蛍光性核染色剤DAPIの輸送:迅速機能評価への応用の可能性 (2010)
  • Author(s): 保嶋智也, 太田欣哉, 井上勝央, 石丸宗徳, 湯浅博昭
  • Organizer: 日本薬学会第130年会,要旨集,No.4,p.209(28P-am026).
  • Place of Presentation: 岡山
• [Presentation] 蛍光性核染色剤DAPIを用いた有機カチオントランスポーターの迅速機能評価法の確立 (2010)
  • Author(s): 保嶋智也, 他
  • Organizer: 第5回トランスポーター研究会年会
  • Place of Presentation: 東京
• [Presentation] ヒトOCT1の蛍光性プローブ基質としてのDAPIの輸送特性の評価 (2010)
  • Author(s): 保嶋智也, 他
  • Organizer: 第25回日本薬物動態学会年会
  • Place of Presentation: さいたま
• [Presentation] Rapid screening of inhibitors for human organic cation transporter 1 using DAPI (2010)
  • Author(s): 保嶋智也, 他
  • Organizer: 第4回次世代を担う若手医療薬科学シンポジウム
  • Place of Presentation: 東京
• [Presentation] 蛍光性色素DAPIを用いたMATE輸送機能の迅速評価法 (2008)
  • Author(s): 保嶋智也, 太田欣哉, 井上勝央, 湯浅博昭
  • Organizer: 第23回日本薬物動態学会年会,要旨集,p.257(31B11-5).
  • Place of Presentation: 熊本