Specific expression of proton-coupled oligopeptide transporter 1 in primary hepatocarcinoma-a novel strategy for tumor-targeted therapy
| Autor: | Zhi Yao, Xi Liu, Xiang Wu, Yanxia Gong, Jie Zhang, Xu Jian, Jia Zhao, Qingyu Zhang, Tao Wang |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
Cancer Research
Cell Immunofluorescence 03 medical and health sciences 0302 clinical medicine expression medicine Oligopeptide Oncogene biology medicine.diagnostic_test Peptide transporter 1 Articles tumor-targeted therapy Cell cycle Molecular biology digestive system diseases primary hepatocarcinoma Blot medicine.anatomical_structure Oncology Cell culture 030220 oncology & carcinogenesis biology.protein 030211 gastroenterology & hepatology proton-coupled oligopeptide transporter 1 |
| Zdroj: | Oncology Letters |
| ISSN: | 1792-1082 1792-1074 |
| DOI: | 10.3892/ol.2017.6724 |
| Popis: | Proton-coupled oligopeptide transporter 1 (PEPT1) is a membrane protein which expressed predominantly in intestine and recognized as the target of dietary nutrients (di/tripeptide) or peptidomimetic drug for delivery. The information on the existence of PEPT1 in carcinomas were limited. Our study aimed to investigate the expression profile and transport activity of PEPT1 both in human hepatocarcinoma tissues and cell lines. Western blotting and an immunofluorescence assay revealed the high level of PEPT1 protein expression in hepatocarcinoma Bel-7402, SMMC-7721, HepG2, HEP3B, SK-HEP-1 cell lines. Quantitative real time PCR showed the mRNA expression of PEPT1 in Bel-7402, SMMC-7721, HepG2, HEP3B, SK-HEP-1 cells. High level PEPT1 expression in hepatocarcinoma patient samples were observed by Immunohistology and showed a significant correlation between protein level and pathological grade. Functional activities were also studied using D-Ala-Lys-AMCA (a substrate of peptide transporter) in above five hepatocarcinoma cell lines. The uptake tests performed by fluorescent microscopy suggested that PEPT1 can transport both D-Ala-Lys-AMCA into the hepatocarcinoma cells and the uptake can be competitively inhibited by three PEPT1 substrates (Gly-sar, Gly-gln and Glyglygly). In conclusion, our findings provided the novel information on the expression and function of PEPT1 in human hepatocarcinoma and expanded the potential values for tumor specific drug delivery. |
| Databáze: | OpenAIRE |
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