Transport of peptidomimetic drugs by the intestinal Di/tri-peptide transporter, PepT1
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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 journal › Journal article › peer-review
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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