Transcriptional regulators of the human multidrug resistance 1 gene: recent views

Biochem Pharmacol. 2002 Sep;64(5-6):943-8. doi: 10.1016/s0006-2952(02)01156-5.


The multidrug resistance (MDR) phenotype is the major cause of failure of cancer chemotherapy. This phenotype is mainly due to the overexpression of the human MDR1 (hMDR1) gene. Several studies have shown that transcriptional regulation of this gene is unexpectedly complex and is far from being completely understood. Current work is aimed mainly at defining unclear and new control regions in the hMDR1 gene promoter as well as clarifying corresponding signaling pathways. Such studies provide new insights into the mechanisms by which xenobiotic molecules might modify the physiological hMDR1 expression as well as the possible role of oncogenes in the pathological dysregulation of the gene. Here we report recent findings on the regulation of hMDR1 which may help define specific targets aimed at modulating its transcription.

Publication types

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

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics*
  • Drug Resistance, Multiple / genetics*
  • Gene Expression Regulation*
  • Humans
  • Promoter Regions, Genetic / physiology
  • Transcription, Genetic / physiology*


  • ATP Binding Cassette Transporter, Subfamily B, Member 1