Membrane transporters and channels in chemoresistance and -sensitivity of tumor cells

Cancer Lett. 2006 Aug 8;239(2):168-82. doi: 10.1016/j.canlet.2005.07.032. Epub 2005 Oct 5.


Membrane transporters play important roles in mediating chemosensitivity and -resistance of tumor cells. ABC transporters, such as ABCB1/MDR1, ABCC1/MRP1 and ABCG2/BCRP, are frequently associated with decreased cellular accumulation of anticancer drugs and multidrug resistance of tumors. SLC transporters, such as folate, nucleoside, and amino acid transporters, commonly increase chemosensitivity by mediating the cellular uptake of hydrophilic drugs. Ion channels and pumps variably affect sensitivity to anticancer therapy by modulating viability of tumor cells. A pharmacogenomic approach, using correlations between drug potency and transporter gene expression in multiple cancer cell lines, has shown promise for identifying potential drug-transporter relationships and predicting anticancer drug response, in an effort to optimize chemotherapy for individual patients.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • ATP-Binding Cassette Transporters / metabolism*
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm*
  • Humans
  • Ion Channels / metabolism*


  • ATP-Binding Cassette Transporters
  • Ion Channels