121st General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Event Hall
Time 4월 19일 (목요일) 11:00~12:30
Code MEDI.P-666
Subject Nitroreductase-Sensitive Fluorescent Probes Based on Reduced Fluorescein, Rhodol and Rhodamine for Imaging of Hypoxia
Authors Tae-Hwan Lim, Dong-Jo Chang*
Department of Pharmacy, Suncheon National University, Korea
Abstract Hypoxia is a prominent feature of many solid tumors and is one of the major contributing factors to changes in cellular metabolism, low extracellular pH, glucose deficiency and increased extracellular lactate concentration. In addition, hypoxia has been reported to induce the resistance to chemotherapy and radiotherapy in various classes of cancer. Thus, imaging of hypoxia can be very critical for effective chemotherapy and radiotherapy. Hypoxic tumor is also recognized to induce a bioreductive stress by the overexpression of reductive enzymes such as nitroreductase, azoreductase and DT-diaphrose. Nitroreductase (NTR) catalyzes the reduction of nitro group to hydroxylamine which is additionally changed to an amine in the presence of NADPH as a cofactor. Xanthene fluorophores including fluorescein, rhodamine and their hybrid structure, rhodol, are the most commonly used fluorophores and their asymmetric derivatives have been used for the development of activity-based fluorescent probes in many areas including biology and medicines. Diverse classes of activity-based fluorescent probes based on fluorescein, rhodol and rhodamine have been developed to detect various phenonmena in live cells. Our group already reported a few NTR-responsive fluorescent probes based on fluorescein and rhodol fluorophore. In this study, we synthesized the NTR-responsive fluorescent probes based on the reduced fluorescein, rhodol and rhodamine scaffolds and evaluated their photochemical properties as activity-based fluorescent probes for detection of NTR which is a highly expressed in hypoxic cells.
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