Usefulness of imaging tumor-specific enzyme expression by radiopharmaceuticals with thymidine phosphorylase inhibitory potency

2017 Fiscal Year Final Research Report

• Project/Area Number: 26461802
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Radiation science
• Research Institution: Health Sciences University of Hokkaido
• Principal Investigator: Ohkua Kazue 北海道医療大学, 薬学部, 教授 (60094827)
• Co-Investigator(Kenkyū-buntansha): 久下 裕司 北海道大学, アイソトープ総合センター, 教授 (70321958) ; 河嶋 秀和 京都薬科大学, 薬学部, 准教授 (70359438) ; 趙 松吉 福島県立医科大学, ふくしま国際医療科学センター, 教授 (80374239) ; 秋澤 宏行 昭和薬科大学, 薬学部, 教授 (90311795)
• Project Period (FY): 2014-04-01 – 2018-03-31
• Keywords: 核医学診断 / 腫瘍 / チミジンホスホリラーゼ / 放射線

Outline of Final Research Achievements

Thymidine phosphorylase (TP) is an angiogenic growth factor; it catalyzes the reversible phosphorylation of thymidine to thymine. TP is overexpressed in highly malignant cancers. To identify the cancer malignancy or predict therapeutic effects of anticancer drugs based on the thymidine analog in relation to TP expression levels in tumors, we developed a radio-iodinated uracil derivative with TP inhibitory potency. Here, we elucidated its uptake mechanism into tumor cells and normal tissues based on the organic cation transporter. Our results could help advance reliability and applicability in cancer theranostics.

Free Research Field

放射性医薬品化学