Resumen

LINDLEY, David J.; CARL, Stephen M.; MOWERY, Stephanie A.  y  KNIPP, Gregory T.. The evaluation of peptide/histidine transporter 1 (PHT1) function: uptake kinetics utilizing a cos-7 stably transfected cell line. Rev. mex. cienc. farm [online]. 2011, vol.42, n.4, pp.57-65. ISSN 1870-0195.

There have been relatively few studies focused on the proton-dependent oligopeptide transporter (POT) superfamily member, Peptide/Histidine Transporter 1 (PHT1), with respect to its contribution to the ADME of peptides and peptide-based drugs. These studies were conducted to determine hPHT1-mediated, H+-dependent uptake kinetics of histidine, carnosine, Gly-Sar and valacyclovir in stably transfected hPHT1-COS-7 cells comparative to kinetics determined in an empty vector (Mock) stably transfected cell line. The results suggest that Gly-Sar appears to be a substrate for PHT1 based on efflux from the stably transfected hPHT1 COS-7 cells. Histidine and Gly-Sar concentration- and time-dependent studies suggest mixed-uptake kinetics. These studies suggest that stably transfected hPHT1-COS-7 cells exhibit different uptake kinetics than those observed in our previous studies and illustrate the requirement for experiments to delineate the physiological role of hPHT1.

Palabras llave : proton-dependent oligopeptide transporter; peptide/histidine transporter 1; PHT1; COS-7 cells; stable transfection; peptide transport; transporter screening.

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