期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 60, 期 4, 页码 2125-2129出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202013265
关键词
azaquinone methide; cancer imaging; fluorescence probe; γ -glutamyltranspeptidase
资金
- AMED [JP19gm0710008, 17cm0106202h0002]
- JST/PRESTO [JPMJPR14F8, JPMJPR17H7]
- MEXT/JSPS KAKENHI [JP16H02606, JP26111012, JP19H05632, JP15H05951, JP19H02826, JP19K22242, JP20H05724]
- JSPS Core-to-Core Program [JPJSCCA20170007]
- A. Advanced Research Networks, by Japan Foundation for Applied Enzymology
- Naito Foundation
- Graduate Program for Leaders in Life Innovation (GPLLI)
A novel functionalized fluorescence probe for GGT was developed, enabling prolonged in vivo cancer imaging and compatibility with fixation and immunostaining of cancer tissue.
gamma-Glutamyltranspeptidase (GGT) is overexpressed in several types of cancer. Existing GGT-targeting fluorescence probes can image these cancers, but the fluorescent hydrolysis product leaks from the target cancer cells during prolonged incubation or fixation. Here, we present a functionalized fluorescence probe for GGT, 4-CH2F-HMDiEtR-gGlu, which is designed to generate an azaquinone methide intermediate during activation by GGT; this intermediate reacts with intracellular nucleophiles to generate a fluorescent adduct that is trapped inside the cells, without loss of the target enzyme activity. Application of the probe to patient-derived xenograft (PDX) mice enabled in vivo cancer imaging for a prolonged period and was also compatible with fixation and immunostaining of the cancer tissue.
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