Peptide transporters: structure, function, regulation and application for drug delivery

Area of Science:

• Biochemistry
• Molecular Biology
• Pharmacology

Background:

• Proton-coupled peptide transporters (PEPT1 and PEPT2) are vital for nutrient absorption and peptide-bound nitrogen conservation in the intestines and kidneys.
• These transporters are critical for the pharmacokinetics and pharmacodynamics of peptide-like drugs, including beta-lactam antibiotics.
• Advances in molecular characterization have elucidated the structure, function, and regulation of PEPT1 and PEPT2.

Purpose of the Study:

• To review recent progress in understanding the cellular and molecular aspects of PEPT1, PEPT2, and related basolateral peptide transporters.
• To highlight the significance of these transporters in drug delivery systems, particularly for peptide-like prodrugs.
• To consolidate current knowledge on the function and localization of intestinal and renal peptide transporters.

Main Methods:

• Literature review of recent scientific findings.
• Analysis of molecular and cellular data on peptide transporter families.
• Synthesis of information on structure-function relationships and regulatory mechanisms.

Main Results:

• Identification and characterization of PEPT1 and PEPT2 have improved understanding of their roles.
• Intestinal PEPT1's ability to transport prodrugs like valacyclovir opens new avenues for drug delivery.
• Distinct basolateral peptide transporters with similar substrate specificities but different functions have been identified.

Conclusions:

• PEPT1 and PEPT2 are key players in peptide absorption and drug transport, with significant implications for pharmaceutical development.
• Understanding basolateral peptide transporters is essential for a comprehensive view of peptide transport.
• Continued research into these transporters will facilitate the design of improved drug delivery strategies.