4.7 Article

Thiol-Michael addition based conjugate for glutathione activation and release

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

  1. National Natural Sci- ence Foundation of China
  2. Science and Tech- nology Program of Gansu Province
  3. Fundamental Research Funds for the Central Universities
  4. [22107041]
  5. [32271307]
  6. [20JR5RA273]
  7. [21JR11RA081]
  8. [lzujbky- 2021-it25]

向作者/读者索取更多资源

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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