Human peptide transporter

Both influx and efflux transporters are located in intestinal epithelial cells and can either increase or decrease oral absorption. Influx transporters such as human peptide transporter 1 (hPEPTl), apical sodium bile acid transporter (ASBT), and nucleoside transporters actively transport drugs that mimic their native substrates across the epithelial cell, whereas efflux transporters such as P-glycoprotein (P-gp), multidrug resistance-associated protein (MRP), and breast cancer resistance protein (BCRP) actively pump absorbed drugs back into the intestinal lumen. 

Han, H. K., et al. CHO/hPEPTl cells overexpressing the human peptide transporter (hPEPTl) as an alternative in vitro model for peptidomimetic drugs. J. Pharm. Sci. 1999, 88, 347-350. 

Han, H.-K., D.-M. Oh, and G. L. Amidon. Cellular uptake mechanism of amino acid ester prodrugs in Caco-2/hPEPTl cells overexpressing a human peptide transporter. Pharm. 

Li YH, Tanno M, Itoh T, Yamada H (1999) Role of the monocarboxylic acid transport system in the intestinal absorption of an orally active beta-lactam prodrug carindacillin as a model. Int I Pharm 191(2) 151—159 Nielsen CU, Brodin B, Jorgensen F et al. (2002) Human peptide transporters therapeutic applications. Exp Opin 12 1329-1350... 

Nielsen, C.U., Brodin, B., Jorgensen, F.S., Frokjaer, S. and Steffansen, B. (2002) Human peptide transporters therapeutic applications. Expert Opinion on Therapeutic Patents, 12, 1329-1350. 

Shimakura, J., Terada, T., Shimada, Y., Katsura, T. and Inui, K. (2006) The transcription factor Cdx2 regulates the intestine-specific expression of human peptide transporter 1 through functional interaction with Spl. Biochemical Pharmacology, 71 (11), 1581—1588. 

Swaan, P.W., Bensman, T., Bahadduri, P., Hall, M.W., Sarker, A., Ekins, S. et al. (2008) Bacterial dipeptide recognition and immune activation facilitated by the human peptide transporter PEPT2. American Journal of Respiratory Cell and Molecular Biology, 39 (5). 536-542. 

Both cefalexin and valaciclovir are substrates for human peptide transporter 1 (hPEPTl), and in vitro and animal data indicated that cefalexin might markedly reduce valaciclovir absorption. However, the findings in this clinical study show a minimal interaction. No special precautions appear to be needed on concurrent use. 

Pharm. Sci., 88, 347 (1999). CHO/hPEPTl Cells Overexpressing the Human Peptide Transporter (hPEPTl) as an Alternative In Vitro Model for Peptidomimetic Drugs. 

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