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[The multidrug-resistance gene MDR1].

K Ueda1, T Komano

  • 1Dept. of Agricultural Chemistry Kyoto University.

Gan to Kagaku Ryoho. Cancer & Chemotherapy
|October 1, 1988
PubMed
Summary

The MDR1 gene produces P-glycoprotein, an efflux pump that removes antitumor drugs from cells. This gene

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Area of Science:

  • Molecular Biology
  • Genetics
  • Biochemistry

Background:

  • The MDR1 gene encodes P-glycoprotein, a transmembrane protein.
  • P-glycoprotein functions as an ATP-dependent efflux pump.
  • This pump actively transports various substrates, including antitumor drugs, out of cells.

Purpose of the Study:

  • To describe the structure and function of P-glycoprotein.
  • To discuss the tissue-specific expression of the MDR1 gene.
  • To explore the normal function and transcriptional regulation of the MDR1 gene.

Main Methods:

  • Analysis of MDR1 gene sequence and protein structure.
  • Investigation of P-glycoprotein binding sites for ATP, drugs, and blockers.
  • Examination of MDR1 gene expression patterns in human tissues.

Main Results:

  • P-glycoprotein is a 1280 amino acid protein with two homologous domains.
  • The protein possesses binding sites for ATP, antitumor drugs, and calcium channel blockers.
  • MDR1 gene expression is observed in human adrenal, kidney, liver, and colon tissues.

Conclusions:

  • The MDR1 gene product, P-glycoprotein, plays a crucial role in drug resistance.
  • Understanding MDR1's tissue-specific expression and regulation is vital for therapeutic strategies.
  • Further research into its normal function and transcriptional control is warranted.

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