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A highly GSH-sensitive SN-38 prodrug with an "OFF-to-ON" fluorescence switch as a bifunctional anticancer agent
- 김경수;
- Yoo, E (Yoo, Eunsoo);
- Kim, D (Kim, Dongin);
- Whang, CH (Whang, Chang-Hee);
- Jo, S (Jo, Seongbong);
- 외 1명
초록
SN-38 (7-ethyl-10-hydroxy-camptothecin) is an active metabolite of irinotecan (CPT-11) and the most potent camptothecin analogue. In this study, 2,4-dinitrobenzene sulfonyl (DNS) was covalently conjugated as a GSH-sensitive trigger to 10' -OH of SN-38 to yield a GSH-sensitive prodrug, denoted as DNS-SN38, with virtually quenched fluorescence due to donor-excited photo-induced electron transfer (d-PeT). By investigating DNS-SN38's activation properties upon fluorescence restoration and cytotoxic potency against ovarian cancer cell lines (A2780 and m-Cherry + OCSC1-F2), its potential applicability as a useful chemotherapeutic agent was demonstrated.
- 제목
- A highly GSH-sensitive SN-38 prodrug with an "OFF-to-ON" fluorescence switch as a bifunctional anticancer agent
- 저자
- 김경수; Yoo, E (Yoo, Eunsoo); Kim, D (Kim, Dongin); Whang, CH (Whang, Chang-Hee); Jo, S (Jo, Seongbong); Hur, SK (Hur, Seong Kwon)
- 발행일
- 2018-07
- 권
- 54
- 호
- 65
- 페이지
- 9031 ~ 9034