Related Experiment Video
Updated: Dec 7, 2025
Using In Vitro Live-cell Imaging to Explore Chemotherapeutics Delivered by Lipid-based Nanoparticles
Published on: November 1, 2017
Novel TSPO-targeted Doxorubicin Prodrug for Colorectal Carcinoma Cells
Jemianne B Jia1,2, Xiaoxi Ling3, Minzhi Xing1,4
1Interventional Oncology Translational Laboratory, University of Pittsburgh School of Medicine, Pittsburgh, PA, U.S.A.
Background/Aim:
18 kDa Translocator protein (TSPO) is a mitochondrial protein up-regulated in colorectal carcinoma (CRC). Our purpose was to develop a TSPO-targeted doxorubicin prodrug (Dox-TSPO) which can be loaded onto drug-eluting beads for transarterial chemoembolization. Furthermore, we evaluated its loading and release kinetics and effects on cell viability.
Materials And Methods:
N-Fmoc-DOX-14-O-hemiglutarate was coupled with a TSPO ligand, 6-TSPOmbb732, using classical N,N,N',N'-tetramethyl-O-(1H-benzotriazol-1-yl)uranium hexafluorophosphate coupling to produce Dox-TSPO. Loading and elution studies were performed using DC beads™. Cell viability studies were performed using CellTiter-Glo® Luminescent Cell Viability Assay.
Results:
Dox-TSPO was successfully synthesized and readily loaded onto and eluted from DC beads™, albeit at a slower rate than free doxorubicin. CRC cell lines expressing TSPO were 2- to 4- fold more sensitive to Dox-TSPO compared to free doxorubicin at 72 h.
Conclusion:
Dox-TSPO is a promising candidate for targeted and directed cancer treatment of CRC liver metastases.
