Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition

SF Zhou - Xenobiotica, 2008 - Taylor & Francis
1. P-glycoprotein (P-gp/MDR1), one of the most clinically important transmembrane
transporters in humans, is encoded by the ABCB1/MDR1 gene. Recent insights into the …

Importance of P-glycoprotein at blood–tissue barriers

MF Fromm - Trends in pharmacological sciences, 2004 - cell.com
P-glycoprotein is the product of the ABCB1 [also known as multidrug resistance 1 (MDR1)]
gene. It translocates a broad variety of xenobiotics out of cells. P-glycoprotein was first …

P-glycoprotein: from genomics to mechanism

SV Ambudkar, C Kimchi-Sarfaty, ZE Sauna… - Oncogene, 2003 - nature.com
Resistance to chemically different natural product anti-cancer drugs (multidrug resistance, or
MDR) results from decreased drug accumulation, resulting from expression of one or more …

Genetic Polymorphisms of the Human MDR1 Drug Transporter

M Schwab, M Eichelbaum… - Annual review of …, 2003 - annualreviews.org
P-glycoprotein is an ATP-dependent efflux pump that contributes to the protection of the
body from environmental toxins. It transports a huge variety of structurally diverse …

The P-glycoprotein multidrug transporter

O Fardel, V Lecureur, A Guillouzo - General Pharmacology: The Vascular …, 1996 - Elsevier
1. P-glycoprotein (P-gp) is a transmembrane protein involved in ATP-dependent efflux of
various structurally unrelated anticancer drugs. Its overexpression in cancer cells decreases …

Role of P-glycoprotein in drug disposition

Y Tanigawara - Therapeutic drug monitoring, 2000 - journals.lww.com
P-glycoprotein (Pgp), which is coded by human MDR1 (multidrug resistance) gene, is an
energy-dependent efflux pump that exports its substrates out of the cell. Human Pgp is …

New insight into p-glycoprotein as a drug target

A Breier, L Gibalova, M Seres… - Anti-Cancer Agents in …, 2013 - ingentaconnect.com
Multidrug resistance (MDR) of cancer tissue is a phenomenon in which cancer cells exhibit
reduced sensitivity to a large group of unrelated drugs with different mechanisms of …

Drugs as P-glycoprotein substrates, inhibitors, and inducers

RB Kim - Drug metabolism reviews, 2002 - Taylor & Francis
In humans, there are two P-glycoprotein (P-gp) transporters encoded by MDR1 (PGY1) and
MDR3 (also named MDR2 and PGY3) adjacently located at the chromosomal region 7q21 …

Expression and function of p-glycoprotein in normal tissues: effect on pharmacokinetics

F Staud, M Ceckova, S Micuda, P Pavek - Multi-Drug Resistance in …, 2010 - Springer
ATP-binding cassette (ABC) drug efflux transporters limit intracellular concentration of their
substrates by pumping them out of cell through an active, energy dependent mechanism …

The influence of MDR1 polymorphisms on P-glycoprotein expression and function in humans

MF Fromm - Advanced drug delivery reviews, 2002 - Elsevier
The MDR1 (ABCB1) gene product P-glycoprotein is a membrane protein, which functions as
an ATP-dependent exporter of xenobiotics from cells. Its importance was first recognized …