Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 63, Issue 17, Pages 9271-9283Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.0c00354
Keywords
-
Categories
Funding
- Natural Science Foundation of China [31830028, 21977058]
- China Postdoctoral Science Foundation [2018 T110533, 2016 M590488, 1601136B]
- Project of Jiangsu Six Peaks of Talent [2016-SWYY-CXTD-008, 2014-SWYY-044]
- Project of Jiangsu 333 high-level talents, Jiangsu Province Innovation Project of Postgraduate Training [KYCX19 2086]
- Applied Research Projects of Nantong City [MS12018079, JC2018125]
- Jiangsu Province Postdoctoral Science Foundation [2018 T110533, 2016 M590488, 1601136B]
Ask authors/readers for more resources
Two novel theranostic agents HJTA and HJTB have been designed and synthesized by covalently linking a beta-carboline derivative, with antitumor activities and pH-responsive fluorescence, with a 2-exomethylenecyclohexanone moiety, which can be activated by the tumor-targeting glutathione (GSH)/glutathione S-transferase pi (GST pi). These agents showed pH- and GSH-dual-responsive fluorescence in tumor cells but not in normal cells. Importantly, HJTA selectively illuminated tumor tissue for up to 7 h and generated precise visualization of orthotopic colonic tumors through the blood circulation system in intraoperative mice. Furthermore, HJTA exhibited potent and selective antiproliferative activities and colonic tumor inhibition in mice. Finally, HJTA induced great cancer cell apoptosis and autophagy by regulating the expression of apoptotic and autophagic proteins. Therefore, this pH/GSH-dual-responsive fluorescent probe with cancer-targeting therapeutic activity provides a novel tool for precise diagnosis and tumor treatment, therefore broadening the impact of multifunctional agents as theranostic precision medicines.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available