@article{oai:kanazawa-u.repo.nii.ac.jp:00015281,
 author = {Mitsuoka, Keisuke and Kato, Yukio and Miyoshi, Sosuke and Murakami, Yoshihiro and Hiraiwa, Mariko and Kubo, Yoshiyuki and Nishimura, Shintaro and Tsuji, Akira},
 issue = {3},
 journal = {European Journal of Pharmaceutical Sciences},
 month = {Jun},
 note = {Oligopeptide transporters are abundantly expressed in various types of cancer cells. We here synthesized two novel dipeptides, l-phenylalanyl sarcosine (Phe-Sar) and 4-(4-methoxyphenyl)-l-phenylalanyl sarcosine (Bip(OMe)-Sar), and examined their effect on the growth of human pancreatic cancer AsPC-1 cells, which are known to highly express oligopeptide transporter PEPT1/SLC15A1. Growth of AsPC-1 cells was inhibited by these two peptides and a typical PEPT1/SLC15A1 substrate Gly-Sar. Growth inhibition by Gly-Sar, Phe-Sar and Bip(OMe)-Sar was concentration-dependent with half-maximal inhibitory concentration of 50, 0.91 and 0.55mM, respectively. These peptides also inhibited PEPT1-mediated [3H]Gly-Sar uptake with half-maximal inhibitory concentration of 2.6, 0.81 and 0.27mM, respectively. Thus, the rank order of the tumor cell growth inhibition by these three peptides was the same as that of PEPT1-inhibitory activity. Growth of AsPC-1 cells was also inhibited by 2-aminobicyclo(2,2,1)heptane-2-carboxylic acid (BCH), which is a typical inhibitor of amino acid transporter system L. The growth inhibition by BCH and Gly-Sar was additive, suggesting that these compounds act at distinct loci. Oligopeptide transporters thus appear to be a promising target for inhibition of pancreatic cancer progression. These results also proposed the idea that oligopeptide transporter is required for growth of AsPC-1 cells. © 2010 Elsevier B.V., 金沢大学医薬保健研究域薬学系},
 pages = {202--208},
 title = {Inhibition of oligopeptide transporter suppress growth of human pancreatic cancer cells},
 volume = {40},
 year = {2010}
}