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Membrane transporters.

V H Lee1

  • 1Department of Pharmaceutical Sciences, School of Pharmacy, University of Southern California, 1985 Zonal Avenue, PSC 708, Los Angeles, CA 90089-9121, USA. vincentL@hsc.usc.edu

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
|October 18, 2000
PubMed
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Carrier-mediated drug transport, particularly dipeptide transporters like PepT1, offers a promising avenue for enhancing oral drug absorption. Targeting these transporters can improve the bioavailability of various medications, including antibiotics and antivirals.

Area of Science:

  • Pharmacology
  • Biochemistry
  • Drug Delivery

Background:

  • Carrier-mediated drug transport is less explored than passive routes.
  • Transporter proteins offer targets for improving epithelial drug absorption.
  • Dipeptide transporters play a key role in oral drug uptake.

Purpose of the Study:

  • To highlight the potential of carrier-mediated transport for drug absorption.
  • To focus on the structure-function, trafficking, and regulation of the dipeptide transporter PepT1.
  • To discuss factors influencing PepT1 function.

Main Methods:

  • Review of existing literature on carrier-mediated drug transport.
  • Focus on cloned proton-coupled peptide transporters, specifically PepT1.
  • Discussion of prodrug strategies utilizing dipeptide transporters.

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Main Results:

  • Dipeptide transporters are crucial for the oral absorption of drugs like beta-lactam antibiotics and ACE inhibitors.
  • Dipeptide transporter systems can be leveraged to enhance oral bioavailability of drugs such as zidovudine and acyclovir.
  • At least four proton-coupled peptide transporters have been identified and cloned.

Conclusions:

  • Targeting dipeptide transporters represents a significant strategy for improving oral drug bioavailability.
  • Understanding PepT1's structure, function, trafficking, and regulation is key to its therapeutic application.
  • Factors like disease, diet, and excipients can modulate PepT1 activity, requiring further investigation.