期刊
BIOORGANIC CHEMISTRY
卷 129, 期 -, 页码 -出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2022.106221
关键词
Thiol-Michael addition; Conjugate; Glutathione activation; Drug release; Antitumor
资金
- National Natural Sci- ence Foundation of China
- Science and Tech- nology Program of Gansu Province
- Fundamental Research Funds for the Central Universities
- [22107041]
- [32271307]
- [20JR5RA273]
- [21JR11RA081]
- [lzujbky- 2021-it25]
Glutathione (GSH) level is an important tumor biomarker, and the newly discovered GSH response conjugate TC6 showed good stability and selectivity, and exhibited improved anti-tumor ability in cancer treatment. This finding provides a new direction for the development of anti-tumor drugs.
Glutathione (GSH) level has long been recognized as a valuable tumor biomarker. GSH-mediated activation and release systems have been extensively developed for cancer diagnosis and treatment, but mainly focused on disulfide-based conjugate. We reported here a new thiol-Michael addition based GSH response conjugate TC6, which consists of a unique tricyclic structure containing alpha, beta-unsaturated ketone responsive groups. The conjugate was easily synthesized and showed good selectivity to glutathione with certain stability. The camptothecin delivery experiment of TC6 showed improved anti-tumor ability in cells and tumor-bearing mice. TC6 could be used for the development of antibody or small molecule conjugated drugs.
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