Abstract
P-glycoprotein (Pgp), coded for by the mdr1 gene, is one of the ABC transporters held responsible for the phenomenon of multidrug resistance (mdr), which is reflected by a rapidly escalating failure of chemotherapy with different classes of cytotoxic agents: anthracyclins, vinca alkaloids, taxanes, epipodophylotoxins. Although overcoming resistance conveyed by Pgp alone may not be sufficient for reaching effective treatment, the abundance of observations available for this paradigmatic multidrug transporter at both in vitro and in vivo setting is a tempting ground for an updated assessment of the main currents of mdr research. In this review we attempt to help keep track of the features of Pgp-mediated drug transport that serve as the major starting points for ongoing efforts of mdr reversal. We will analyze the slowly narrowing gaps that prevail between our ever increasing understanding at the protein, cell and organism level, focusing on the molecular interactions involving Pgp.
Keywords: P-glycoprotein, multidrug resistance, hydrophobicity, membrane microdomains
Current Cancer Drug Targets
Title: Multidrug Resistance Through the Spectacle of P-Glycoprotein
Volume: 9 Issue: 3
Author(s): Katalin Goda, Zsolt Bacso and Gabor Szabo
Affiliation:
Keywords: P-glycoprotein, multidrug resistance, hydrophobicity, membrane microdomains
Abstract: P-glycoprotein (Pgp), coded for by the mdr1 gene, is one of the ABC transporters held responsible for the phenomenon of multidrug resistance (mdr), which is reflected by a rapidly escalating failure of chemotherapy with different classes of cytotoxic agents: anthracyclins, vinca alkaloids, taxanes, epipodophylotoxins. Although overcoming resistance conveyed by Pgp alone may not be sufficient for reaching effective treatment, the abundance of observations available for this paradigmatic multidrug transporter at both in vitro and in vivo setting is a tempting ground for an updated assessment of the main currents of mdr research. In this review we attempt to help keep track of the features of Pgp-mediated drug transport that serve as the major starting points for ongoing efforts of mdr reversal. We will analyze the slowly narrowing gaps that prevail between our ever increasing understanding at the protein, cell and organism level, focusing on the molecular interactions involving Pgp.
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Cite this article as:
Goda Katalin, Bacso Zsolt and Szabo Gabor, Multidrug Resistance Through the Spectacle of P-Glycoprotein, Current Cancer Drug Targets 2009; 9 (3) . https://dx.doi.org/10.2174/156800909788166493
DOI https://dx.doi.org/10.2174/156800909788166493 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
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