Inhibition of hyaluronan export from human fibroblasts by inhibitors of multidrug resistance transporters

Standard

Inhibition of hyaluronan export from human fibroblasts by inhibitors of multidrug resistance transporters. / Prehm, Peter; Schumacher, Udo.

in: BIOCHEM PHARMACOL, Jahrgang 68, Nr. 7, 01.10.2004, S. 1401-10.

Publikationen: SCORING: Beitrag in Fachzeitschrift/ZeitungSCORING: ZeitschriftenaufsatzForschungBegutachtung

Harvard

APA

Vancouver

Bibtex

@article{91558371bf46488680046faa5eb717c2,
title = "Inhibition of hyaluronan export from human fibroblasts by inhibitors of multidrug resistance transporters",
abstract = "In a previous report we described the export of hyaluronan from Streptococcus pyogenes by an ABC transporter. Extending these findings a sequence homology search against human proteins revealed a strong homology to the multidrug resistance transporter ABC-B (MDR-1) and ABC-C (MRP 5). Using several inhibitors directed against these and other transporters, a decreased hyaluronan production in cell culture as well as in hyaluronan synthase activity in purified membrane fractions was observed. The inhibitory capacity (IC(50) concentrations) was compared the with reported IC(50)- or the K(i)-concentrations for individual transporters. These analyses revealed that hyaluronan is synthesized within the cytoplasm of mammalian cells and actively secreted into the pericellular space by energy dependent transport proteins. While inhibition of several transport proteins resulted in a decrease of hyaluronan export, inhibition of the MRP5 transporter was the most effective one to decrease hyaluronan in the cell culture supernatant indicating that hyaluronan export is one physiological role of this transport protein.",
keywords = "ATP-Binding Cassette Transporters, Biological Transport, Cell Division, Cells, Cultured, Cyclosporins, Drug Resistance, Multiple, Fibroblasts, Humans, Hyaluronic Acid, Multidrug Resistance-Associated Proteins, Synovial Membrane",
author = "Peter Prehm and Udo Schumacher",
year = "2004",
month = oct,
day = "1",
doi = "10.1016/j.bcp.2004.06.017",
language = "English",
volume = "68",
pages = "1401--10",
journal = "BIOCHEM PHARMACOL",
issn = "0006-2952",
publisher = "Elsevier Inc.",
number = "7",

}

RIS

TY - JOUR

T1 - Inhibition of hyaluronan export from human fibroblasts by inhibitors of multidrug resistance transporters

AU - Prehm, Peter

AU - Schumacher, Udo

PY - 2004/10/1

Y1 - 2004/10/1

N2 - In a previous report we described the export of hyaluronan from Streptococcus pyogenes by an ABC transporter. Extending these findings a sequence homology search against human proteins revealed a strong homology to the multidrug resistance transporter ABC-B (MDR-1) and ABC-C (MRP 5). Using several inhibitors directed against these and other transporters, a decreased hyaluronan production in cell culture as well as in hyaluronan synthase activity in purified membrane fractions was observed. The inhibitory capacity (IC(50) concentrations) was compared the with reported IC(50)- or the K(i)-concentrations for individual transporters. These analyses revealed that hyaluronan is synthesized within the cytoplasm of mammalian cells and actively secreted into the pericellular space by energy dependent transport proteins. While inhibition of several transport proteins resulted in a decrease of hyaluronan export, inhibition of the MRP5 transporter was the most effective one to decrease hyaluronan in the cell culture supernatant indicating that hyaluronan export is one physiological role of this transport protein.

AB - In a previous report we described the export of hyaluronan from Streptococcus pyogenes by an ABC transporter. Extending these findings a sequence homology search against human proteins revealed a strong homology to the multidrug resistance transporter ABC-B (MDR-1) and ABC-C (MRP 5). Using several inhibitors directed against these and other transporters, a decreased hyaluronan production in cell culture as well as in hyaluronan synthase activity in purified membrane fractions was observed. The inhibitory capacity (IC(50) concentrations) was compared the with reported IC(50)- or the K(i)-concentrations for individual transporters. These analyses revealed that hyaluronan is synthesized within the cytoplasm of mammalian cells and actively secreted into the pericellular space by energy dependent transport proteins. While inhibition of several transport proteins resulted in a decrease of hyaluronan export, inhibition of the MRP5 transporter was the most effective one to decrease hyaluronan in the cell culture supernatant indicating that hyaluronan export is one physiological role of this transport protein.

KW - ATP-Binding Cassette Transporters

KW - Biological Transport

KW - Cell Division

KW - Cells, Cultured

KW - Cyclosporins

KW - Drug Resistance, Multiple

KW - Fibroblasts

KW - Humans

KW - Hyaluronic Acid

KW - Multidrug Resistance-Associated Proteins

KW - Synovial Membrane

U2 - 10.1016/j.bcp.2004.06.017

DO - 10.1016/j.bcp.2004.06.017

M3 - SCORING: Journal article

C2 - 15345330

VL - 68

SP - 1401

EP - 1410

JO - BIOCHEM PHARMACOL

JF - BIOCHEM PHARMACOL

SN - 0006-2952

IS - 7

ER -