Intestinal peptide transporter and application for improving oral absorption
HE Zhong-gui
Abstract
HE Zhong-gui
Abstract
Peptide transporters that expressed in the intestinal brush border membrane (PEPT1) and peptide transporter that expressed in the basolateral membrane were the two subtypes of peptide transporter (PEPT) . They played an essential role in absorption of oligopeptides and peptidomimetic drugs. PEPT1 was a key target for approach of prodrug. Not well absorbed drugs could be appropriately designed in the form of di-/ tripeptide analogues to be well absorbed across the intestinal brush border membrane via PEPT1 and thus increase the valuable oral bioavailability.
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Peptide transporters that expressed in the intestinal brush border membrane (PEPT1) and peptide transporter that expressed in the basolateral membrane were the two subtypes of peptide transporter (PEPT) . They played an essential role in absorption of oligopeptides and peptidomimetic drugs. PEPT1 was a key target for approach of prodrug. Not well absorbed drugs could be appropriately designed in the form of di-/ tripeptide analogues to be well absorbed across the intestinal brush border membrane via PEPT1 and thus increase the valuable oral bioavailability.
Key concepts: Tripeptide, Peptide, Transporter, Prodrug, Brush border, Oligopeptide, Peptidomimetic, Bioavailability