期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 53, 期 17, 页码 4469-4474出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201311133
关键词
biotin; cellular imaging; glutathione; SN-38; theranostic
资金
- Creative Research Initiative program of National Research Foundation of Korea [2009-0081566]
- CAP [PBC066]
- Korea Research Council of Fundamental Science and Technology
- Korea Basic Science Institute [D33400]
- National Research Council of Science & Technology (NST), Republic of Korea [D33400] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
A new theranostic strategy is described. It is based on the use of an all in one prodrug, namely the biotinylated piperazine-rhodol conjugate 4a. This conjugate, which incorporates the anticancer drug SN-38, undergoes self-immolative cleavage when exposed to biological thiols. This leads to the tumor-targeted release of the active SN-38 payload along with fluorophore 1a. This release is made selective as the result of the biotin functionality. Fluorophore 1a is 32-fold more fluorescent than prodrug 4a. It permits the delivery and release of the SN-38 payload to be monitored easily invitro and invivo, as inferred from cell studies and exvivo analyses of mice xenografts derived from HeLa cells, respectively. Prodrug 4a also displays anticancer activity in the HeLa cell murine xenograft tumor model. On the basis of these findings we suggest that the present strategy, which combines within a single agent the key functions of targeting, release, imaging, and treatment, may have a role to play in cancer diagnosis and therapy.
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