Recent advances in P-glycoprotein-mediated multidrug resistance reversal mechanisms

Methods Find Exp Clin Pharmacol. 2007 Nov;29(9):607-17. doi: 10.1358/mf.2007.29.9.1139054.

Abstract

Expression of the multidrug resistance (MDR) phenotype is responsible for chemotherapy failure in numerous cancers. Overexpression of mdr1 gene-encoded permeability glycoprotein (P-gp) is known to play a pivotal role in the development of this phenotype. The role of P-gp has been proposed as an important goal in the design of chemotherapy strategies. However, modulation of P-gp activity by chemotherapy has limited possibilities because of toxicity and poor specificity. In this article, we review the latest advancements in different potential P-gp-mediated MDR reversal mechanisms as well as the methods of evaluating MDR reversal activity, which would be helpful in finding novel MDR reversal agents (or chemosensitizers).

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / biosynthesis*
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / pharmacology
  • Apoptosis / physiology
  • Drug Resistance, Multiple / genetics
  • Drug Resistance, Multiple / immunology
  • Drug Resistance, Multiple / physiology*
  • Drug Resistance, Neoplasm / genetics
  • Drug Resistance, Neoplasm / immunology
  • Drug Resistance, Neoplasm / physiology*
  • Genes, MDR
  • Humans

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Antineoplastic Agents