Human peptide transporters: Therapeutic applications

Carsten Uhd Nielsen; Birger Brodin; Flemming Steen Jørgensen; Sven Frokjaer; Bente Steffansen

doi:10.1517/13543776.12.9.1329

Human peptide transporters: Therapeutic applications

Carsten Uhd Nielsen^*, Birger Brodin, Flemming Steen Jørgensen, Sven Frokjaer, Bente Steffansen

^*Corresponding author af dette arbejde

44 Citationer (Scopus)

Abstract

Peptide transporters are epithelial solute carriers. Their functional role has been characterised in the small intestine and proximal tubules, where they are involved in absorption of dietary peptides and peptide reabsorption, respectively. Currently, two peptide transporters, PepT1 and PepT2, which possess transport activity, have been identified. The transporters are not drug targets per se, but due to uniquely broad substrate specificity they have proven to be relevant in drug therapy at the level of drug transport. Therapeutic agents such as orally active β-lactam antibiotics, bestatin, prodrugs of acyclovir and gancyclovir have oral bioavailabilities, which are largely a result of their interaction with PepT1. The transporters have therefore received considerable attention in relation to drug delivery. The aim of the present review is to highlight structural requirements for binding to peptide transporters, as well as their role in drug delivery and in potential future drug design and targeted tissue delivery of peptides and peptidomimetics.

Originalsprog	Engelsk
Tidsskrift	Expert Opinion on Therapeutic Patents
Vol/bind	12
Udgave nummer	9
Sider (fra-til)	1329-1350
Antal sider	22
ISSN	1354-3776
DOI	https://doi.org/10.1517/13543776.12.9.1329
Status	Udgivet - 1 sep. 2002

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10.1517/13543776.12.9.1329

http://www.scopus.com/inward/record.url?scp=0036740580&partnerID=8YFLogxK

Citationsformater

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title = "Human peptide transporters: Therapeutic applications",

abstract = "Peptide transporters are epithelial solute carriers. Their functional role has been characterised in the small intestine and proximal tubules, where they are involved in absorption of dietary peptides and peptide reabsorption, respectively. Currently, two peptide transporters, PepT1 and PepT2, which possess transport activity, have been identified. The transporters are not drug targets per se, but due to uniquely broad substrate specificity they have proven to be relevant in drug therapy at the level of drug transport. Therapeutic agents such as orally active β-lactam antibiotics, bestatin, prodrugs of acyclovir and gancyclovir have oral bioavailabilities, which are largely a result of their interaction with PepT1. The transporters have therefore received considerable attention in relation to drug delivery. The aim of the present review is to highlight structural requirements for binding to peptide transporters, as well as their role in drug delivery and in potential future drug design and targeted tissue delivery of peptides and peptidomimetics.",

keywords = "β-lactams, Angiotensin converting (ACE) inhibitors, Bestatin, Bisphosphonates, Carrier-mediated drug delivery, Cephalosporins, Di/tripeptide transporter, Drug absorption, hPepT1, hPepT2, Oligopeptide transporter, Renin inhibitors, Thrombin inhibitors, Valacyclovir, Valgancyclovir",

author = "Nielsen, {Carsten Uhd} and Birger Brodin and J{\o}rgensen, {Flemming Steen} and Sven Frokjaer and Bente Steffansen",

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T1 - Human peptide transporters

T2 - Therapeutic applications

AU - Nielsen, Carsten Uhd

AU - Brodin, Birger

AU - Jørgensen, Flemming Steen

AU - Frokjaer, Sven

AU - Steffansen, Bente

PY - 2002/9/1

Y1 - 2002/9/1

N2 - Peptide transporters are epithelial solute carriers. Their functional role has been characterised in the small intestine and proximal tubules, where they are involved in absorption of dietary peptides and peptide reabsorption, respectively. Currently, two peptide transporters, PepT1 and PepT2, which possess transport activity, have been identified. The transporters are not drug targets per se, but due to uniquely broad substrate specificity they have proven to be relevant in drug therapy at the level of drug transport. Therapeutic agents such as orally active β-lactam antibiotics, bestatin, prodrugs of acyclovir and gancyclovir have oral bioavailabilities, which are largely a result of their interaction with PepT1. The transporters have therefore received considerable attention in relation to drug delivery. The aim of the present review is to highlight structural requirements for binding to peptide transporters, as well as their role in drug delivery and in potential future drug design and targeted tissue delivery of peptides and peptidomimetics.

AB - Peptide transporters are epithelial solute carriers. Their functional role has been characterised in the small intestine and proximal tubules, where they are involved in absorption of dietary peptides and peptide reabsorption, respectively. Currently, two peptide transporters, PepT1 and PepT2, which possess transport activity, have been identified. The transporters are not drug targets per se, but due to uniquely broad substrate specificity they have proven to be relevant in drug therapy at the level of drug transport. Therapeutic agents such as orally active β-lactam antibiotics, bestatin, prodrugs of acyclovir and gancyclovir have oral bioavailabilities, which are largely a result of their interaction with PepT1. The transporters have therefore received considerable attention in relation to drug delivery. The aim of the present review is to highlight structural requirements for binding to peptide transporters, as well as their role in drug delivery and in potential future drug design and targeted tissue delivery of peptides and peptidomimetics.

KW - β-lactams

KW - Angiotensin converting (ACE) inhibitors

KW - Bestatin

KW - Bisphosphonates

KW - Carrier-mediated drug delivery

KW - Cephalosporins

KW - Di/tripeptide transporter

KW - Drug absorption

KW - hPepT1

KW - hPepT2

KW - Oligopeptide transporter

KW - Renin inhibitors

KW - Thrombin inhibitors

KW - Valacyclovir

KW - Valgancyclovir

U2 - 10.1517/13543776.12.9.1329

DO - 10.1517/13543776.12.9.1329

M3 - Journal article

AN - SCOPUS:0036740580

SN - 1354-3776

VL - 12

SP - 1329

EP - 1350

JO - Expert Opinion on Therapeutic Patents

JF - Expert Opinion on Therapeutic Patents

IS - 9

ER -

Human peptide transporters: Therapeutic applications

Abstract

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