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  • 02월 19일 10시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제121회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Nitroreductase-Sensitive Fluorescent Probes Based on Reduced Fluorescein, Rhodol and Rhodamine for Imaging of Hypoxia

2018년 2월 13일 16시 24분 12초
MEDI.P-666 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
4월 19일 (목요일) 11:00~12:30
Medicinal Chemistry
저자 및
Tae-Hwan Lim, Dong-Jo Chang*
Department of Pharmacy, Suncheon National University, Korea
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.