Pharmaceutical Research

, Volume 16, Issue 9, pp 1331–1343

Intestinal Peptide Transport Systems and Oral Drug Availability

  • Cheng Y. Yang
  • Anne H. Dantzig
  • Charles Pidgeon
Article

DOI: 10.1023/A:1018982505021

Cite this article as:
Yang, C.Y., Dantzig, A.H. & Pidgeon, C. Pharm Res (1999) 16: 1331. doi:10.1023/A:1018982505021

Abstract

The intestinal peptide transport system has broad substrate specificities. In addition to its physiological function of absorbing di- and tripeptides resulting from the digestion of dietary proteins, this transport system also absorbs some orally administered peptidomimetic drugs, including β-lactam antibiotics, angiotensin converting enzyme inhibitors, renin inhibitors, bestatin, thrombin inhibitors, and thyrotropin-releasing hormone and its analogues. There have been several studies on the mechanism and substrate structure-affinity relationship for this transport system. Rapid progress has been made recently in studies on the molecular basis of the intestinal peptide transport system. A protein apparently involved in peptide transport has been isolated from rabbit small intestines, and genes for human intestinal peptide transporters have been cloned, sequenced and functionally expressed. This review summarizes these studies and addresses the pharmaceutical potential of the intestinal peptide transport system.

peptide transportdrug absorptionintestinePepTlHPT-1PepT2PHT-1

Copyright information

© Plenum Publishing Corporation 1999

Authors and Affiliations

  • Cheng Y. Yang
    • 1
  • Anne H. Dantzig
    • 2
  • Charles Pidgeon
    • 1
  1. 1.Department of Medicinal Chemistry and Molecular Pharmacology, School of PharmacyPurdue UniversityWest Lafayette
  2. 2.Lilly Corporate Center, Eli Lilly and CompanyIndianapolis