Open Access

Specific expression of proton-coupled oligopeptide transporter 1 in primary hepatocarcinoma‑a novel strategy for tumor-targeted therapy

  • Authors:
    • Yanxia Gong
    • Jie Zhang
    • Xiang Wu
    • Tao Wang
    • Jia Zhao
    • Zhi Yao
    • Qingyu Zhang
    • Xi Liu
    • Xu Jian
  • View Affiliations

  • Published online on: August 4, 2017     https://doi.org/10.3892/ol.2017.6724
  • Pages: 4158-4166
  • Copyright: © Gong et al. This is an open access article distributed under the terms of Creative Commons Attribution License.

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Abstract

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.
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October-2017
Volume 14 Issue 4

Print ISSN: 1792-1074
Online ISSN:1792-1082

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Spandidos Publications style
Gong Y, Zhang J, Wu X, Wang T, Zhao J, Yao Z, Zhang Q, Liu X and Jian X: Specific expression of proton-coupled oligopeptide transporter 1 in primary hepatocarcinoma‑a novel strategy for tumor-targeted therapy. Oncol Lett 14: 4158-4166, 2017
APA
Gong, Y., Zhang, J., Wu, X., Wang, T., Zhao, J., Yao, Z. ... Jian, X. (2017). Specific expression of proton-coupled oligopeptide transporter 1 in primary hepatocarcinoma‑a novel strategy for tumor-targeted therapy. Oncology Letters, 14, 4158-4166. https://doi.org/10.3892/ol.2017.6724
MLA
Gong, Y., Zhang, J., Wu, X., Wang, T., Zhao, J., Yao, Z., Zhang, Q., Liu, X., Jian, X."Specific expression of proton-coupled oligopeptide transporter 1 in primary hepatocarcinoma‑a novel strategy for tumor-targeted therapy". Oncology Letters 14.4 (2017): 4158-4166.
Chicago
Gong, Y., Zhang, J., Wu, X., Wang, T., Zhao, J., Yao, Z., Zhang, Q., Liu, X., Jian, X."Specific expression of proton-coupled oligopeptide transporter 1 in primary hepatocarcinoma‑a novel strategy for tumor-targeted therapy". Oncology Letters 14, no. 4 (2017): 4158-4166. https://doi.org/10.3892/ol.2017.6724