H+ coupled active transport of bestatin via the dipeptide transport system in rabbit intestinal brush-border membranes.

@article{Inui1992HCA,
  title={H+ coupled active transport of bestatin via the dipeptide transport system in rabbit intestinal brush-border membranes.},
  author={Ken-ichi Inui and Yoshihiko Tomita and Toshiya Katsura and Takashi Okano and Mikihisa Takano and Ryohei Hori},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={1992},
  volume={260 2},
  pages={
          482-6
        }
}
Bestatin [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl-L-leucine], a dipeptide containing an unusual amino acid, has been used clinically as an anticancer agent in p.o. dosage form. We examined the transport characteristics of [3H]bestatin by rabbit intestinal brush-border membrane vesicles. Bestatin uptake was stimulated by an inward H+ gradient (overshoot phenomenon) and by an interior-negative membrane potential. About half of the apparent bestatin uptake at 1 mM by brush-border membrane… CONTINUE READING

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