Transport of peptidomimetic drugs by the intestinal Di/tri-peptide transporter, PepT1

Research output: Contribution to journalJournal articlepeer-review

Standard

Transport of peptidomimetic drugs by the intestinal Di/tri-peptide transporter, PepT1. / Brodin, Birger; Nielsen, Carsten Uhd; Steffansen, Bente; Frøkjaer, Sven.

In: Basic & Clinical Pharmacology & Toxicology, Vol. 90, No. 6, 2002, p. 285-96.

Research output: Contribution to journalJournal articlepeer-review

Harvard

Brodin, B, Nielsen, CU, Steffansen, B & Frøkjaer, S 2002, 'Transport of peptidomimetic drugs by the intestinal Di/tri-peptide transporter, PepT1', Basic & Clinical Pharmacology & Toxicology, vol. 90, no. 6, pp. 285-96. https://doi.org/10.1034/j.1600-0773.2002.900601.x

APA

Brodin, B., Nielsen, C. U., Steffansen, B., & Frøkjaer, S. (2002). Transport of peptidomimetic drugs by the intestinal Di/tri-peptide transporter, PepT1. Basic & Clinical Pharmacology & Toxicology, 90(6), 285-96. https://doi.org/10.1034/j.1600-0773.2002.900601.x

Vancouver

Brodin B, Nielsen CU, Steffansen B, Frøkjaer S. Transport of peptidomimetic drugs by the intestinal Di/tri-peptide transporter, PepT1. Basic & Clinical Pharmacology & Toxicology. 2002;90(6):285-96. https://doi.org/10.1034/j.1600-0773.2002.900601.x

Author

Brodin, Birger ; Nielsen, Carsten Uhd ; Steffansen, Bente ; Frøkjaer, Sven. / Transport of peptidomimetic drugs by the intestinal Di/tri-peptide transporter, PepT1. In: Basic & Clinical Pharmacology & Toxicology. 2002 ; Vol. 90, No. 6. pp. 285-96.

Bibtex

@article{b38958c62d4e44a2984465b0dabbcd09,
title = "Transport of peptidomimetic drugs by the intestinal Di/tri-peptide transporter, PepT1",
abstract = "The apical membrane of small intestinal enterocytes possess an uptake system for di- and tripeptides. The physiological function of the system is to transport small peptides resulting from digestion of dietary protein. Moreover, due to the broad substrate specificity of the system, it is also capable of transporting a number of orally administered peptidomimetic drugs. Absorbed peptides may be hydrolysed in the cells due to the high peptidase activity present in the cytosol. Peptidomimetic drugs may, if resistant to the cellular enzyme activity, pass the basolateral membrane via a basolateral peptide transport mechanism and enter the systemic circulation. As the number of new peptide and peptidomimetic drugs are rapidly increasing, the peptide transport system has gained increasing attention as a possible drug delivery system for small peptides and peptide-like compounds. In this paper we give an updated introduction to the transport system and discuss the substrate characteristics of the di/tri-peptide transporter system with special emphasis on chemically modified substrates and prodrugs.",
keywords = "Animals, Biological Transport, Carrier Proteins, Humans, Intestinal Absorption, Intestinal Mucosa, Molecular Mimicry, Oligopeptides, Peptides, Pharmaceutical Preparations, Pharmacokinetics, Prodrugs, Symporters",
author = "Birger Brodin and Nielsen, {Carsten Uhd} and Bente Steffansen and Sven Fr{\o}kjaer",
year = "2002",
doi = "10.1034/j.1600-0773.2002.900601.x",
language = "English",
volume = "90",
pages = "285--96",
journal = "Basic and Clinical Pharmacology and Toxicology",
issn = "1742-7835",
publisher = "Wiley-Blackwell",
number = "6",

}

RIS

TY - JOUR

T1 - Transport of peptidomimetic drugs by the intestinal Di/tri-peptide transporter, PepT1

AU - Brodin, Birger

AU - Nielsen, Carsten Uhd

AU - Steffansen, Bente

AU - Frøkjaer, Sven

PY - 2002

Y1 - 2002

N2 - The apical membrane of small intestinal enterocytes possess an uptake system for di- and tripeptides. The physiological function of the system is to transport small peptides resulting from digestion of dietary protein. Moreover, due to the broad substrate specificity of the system, it is also capable of transporting a number of orally administered peptidomimetic drugs. Absorbed peptides may be hydrolysed in the cells due to the high peptidase activity present in the cytosol. Peptidomimetic drugs may, if resistant to the cellular enzyme activity, pass the basolateral membrane via a basolateral peptide transport mechanism and enter the systemic circulation. As the number of new peptide and peptidomimetic drugs are rapidly increasing, the peptide transport system has gained increasing attention as a possible drug delivery system for small peptides and peptide-like compounds. In this paper we give an updated introduction to the transport system and discuss the substrate characteristics of the di/tri-peptide transporter system with special emphasis on chemically modified substrates and prodrugs.

AB - The apical membrane of small intestinal enterocytes possess an uptake system for di- and tripeptides. The physiological function of the system is to transport small peptides resulting from digestion of dietary protein. Moreover, due to the broad substrate specificity of the system, it is also capable of transporting a number of orally administered peptidomimetic drugs. Absorbed peptides may be hydrolysed in the cells due to the high peptidase activity present in the cytosol. Peptidomimetic drugs may, if resistant to the cellular enzyme activity, pass the basolateral membrane via a basolateral peptide transport mechanism and enter the systemic circulation. As the number of new peptide and peptidomimetic drugs are rapidly increasing, the peptide transport system has gained increasing attention as a possible drug delivery system for small peptides and peptide-like compounds. In this paper we give an updated introduction to the transport system and discuss the substrate characteristics of the di/tri-peptide transporter system with special emphasis on chemically modified substrates and prodrugs.

KW - Animals

KW - Biological Transport

KW - Carrier Proteins

KW - Humans

KW - Intestinal Absorption

KW - Intestinal Mucosa

KW - Molecular Mimicry

KW - Oligopeptides

KW - Peptides

KW - Pharmaceutical Preparations

KW - Pharmacokinetics

KW - Prodrugs

KW - Symporters

U2 - 10.1034/j.1600-0773.2002.900601.x

DO - 10.1034/j.1600-0773.2002.900601.x

M3 - Journal article

C2 - 12403049

VL - 90

SP - 285

EP - 296

JO - Basic and Clinical Pharmacology and Toxicology

JF - Basic and Clinical Pharmacology and Toxicology

SN - 1742-7835

IS - 6

ER -

ID: 37899682