We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Design, synthesis, and in vitro antitumor activity of a transferrin receptor‐targeted peptide–doxorubicin conjugate.
- Authors
Li, Songtao; Zhao, Hongling; Fan, Yanfang; Zhao, Guiqin; Wang, Ruxing; Wen, Fuyu; Wang, Jianping; Wang, Xiaohui; Wang, Yu; Gao, Yang
- Abstract
In this study, a peptide–drug conjugate was designed and synthesized by connecting a transferrin receptor (TfR)‐targeted binding peptide analog BP9a (CAHLHNRS) with doxorubicin (DOX) through N‐succinimidyl‐3‐maleimidopropionate (SMP) as the cross‐linker. Confocal laser scanning microscopy results indicated that free DOX mainly accumulated in the nuclei of both TfR overexpressed HepG2 hepatoma cells and L‐O2 normal liver cells expressing low level of TfR; most of the BP9a‐DOX conjugate displayed cytoplasmic location, and its cellular uptake by HepG2 cells was obviously reduced by TfR blockage test. Nevertheless, the cellular uptake of this conjugate by L‐O2 cells was much less than that of free DOX. Meanwhile, the BP9a‐DOX conjugate exhibited lower in vitro antiproliferative activity against HepG2 cells than free DOX, but its cytotoxic effect on L‐O2 cells was decreased compared with that of free DOX. These results suggest that BP9a could be applied as a potential TfR‐targeted peptide vector for selective drug delivery.
- Subjects
TRANSFERRIN receptors; LIVER cells; DOXORUBICIN; LASER microscopy
- Publication
Chemical Biology & Drug Design, 2020, Vol 95, Issue 1, p58
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.13613