Cancer cell‐targeted drug delivery utilizing oligopeptide transport activity

Abstract

To study the drug delivery to tumor by utilization of an oligopeptide transport activity, we examined the accumulation of dipeptides and the peptide-mimetic anti-cancer drug, bestatin, a substrate of oligopeptide transporter PepT1.

Functional Expression of Stereoselective Metabolism of Cephalexin by Exogenous Transfection of Oligopeptide Transporter PEPT1

“…Human embryonic kidney (HEK) 293 cells were obtained from the Japanese Cancer Research Resources Bank (Tokyo, Japan). HeLa cells stably expressing human PEPT1 (HeLa/PEPT1) or vector alone (mock) were previously established in our laboratory (Nakanishi et al, 2000). The protein assay kit was purchased from Bio-Rad Laboratories, Inc. (Hercules, CA).…”

Suppression of Cell Proliferation by Inhibition of Estrone-3-Sulfate Transporter in Estrogen-Dependent Breast Cancer Cells

“…Na + -taurocholate-cotransporting polypeptide (SLC10A1) and organic anion-transporting polypeptide OATP1B3 (formerly termed OATP8, SLC21A8) are expressed in hepatocellular and gastrointestinal carcinomas, respectively (15,16). Moreover, although the responsible molecule has not been identified, transport activity for di-and tripeptides and peptide-mimetic drugs has been observed in various cancer cell lines (17,18). Therefore, these transporters may be applicable to deliver chemotherapeutic agents to target cancer cells.…”

PEPT (SLC15A) Family

“…Gene expression analysis indicates that PEPT2 is more widely expressed than PEPT1 in cancer cell lines (Mitsuoka et al, 2008). Oligopeptide transport activity was originally found in human tumor cell lines such as HT1080, AsPC-1, Capan-2, MKN45, MG-63, T24, and SK-ChA-1 (Gonzalez et al, 1998;Nakanishi et al, 1997Nakanishi et al, , 2000Knütter et al, 2002). An antitumor agent, bestatin, (2S,3R)-3-amino-2-hydroxy-4-phenylbutyryl-L-leucine, which induces apoptosis in glioma, is also a substrate of PEPTs (Tomita et al, 1990).…”