Cancer Letters
Volume 230, Issue 1 , Pages 72-80, 8 December 2005

Regulation of human peptide transporter 1 (PEPT1) in gastric cancer cells by anticancer drugs

Department of Pharmacy, Faculty of Medicine, Kyoto University Hospital, Kyoto University, Sakyo-ku, Kyoto 606-8507, Japan

Received 25 October 2004; received in revised form 15 December 2004; accepted 18 December 2004.

Abstract 

Human peptide transporter 1 (PEPT1) mediates the cellular uptake of di- and tripeptides and peptide-like drugs in the small intestine. In the present study, we examined the regulation of PEPT1 by anticancer drugs in the gastric cancer cell line MKN45. PEPT1 was expressed and functioned in MKN45 cells. The transport activity and mRNA expression of the facilitative glucose transporter 1 (GLUT1) were significantly decreased by 5-fluorouracil treatment, but those of PEPT1 were slightly increased. Cisplatin treatment affected neither PEPT1 nor GLUT1 activity. In conclusion, PEPT1 expressed in MKN45 cells are resistant against the cellular injury induced by 5-fluorouracil and cisplatin.

Keywords: Peptide transporter, Gastric cancer, 5-Fluorouracil, Cisplatin

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PII: S0304-3835(04)01001-8

doi:10.1016/j.canlet.2004.12.023

Cancer Letters
Volume 230, Issue 1 , Pages 72-80, 8 December 2005

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