Amitriptyline may have a supportive role in cancer treatment by inhibiting glutathione S-transferase pi (GST-pi) and alpha (GST-alpha)

KULAKSIZ ERKMEN G., DALMIZRAK Ö., Dincsoy-Tuna G., Dogan A., ÖĞÜŞ İ. H., ÖZER N.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.28, no.1, pp.131-136, 2013 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 28 Issue: 1
  • Publication Date: 2013
  • Doi Number: 10.3109/14756366.2011.639017
  • Journal Name: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.131-136
  • Keywords: Amitriptyline, anticancer drugs, GST-alpha, GST-pi, GSTs, TRICYCLIC ANTIDEPRESSANTS, ISOENZYMES, BINDING, TARGET, CELLS, TRANSPORTERS, DEPRESSION, SEROTONIN, MECHANISM, CARCINOMA
  • Hacettepe University Affiliated: Yes

Abstract

A tricyclic anti-depressant, amitriptyline, is a highly prescribed drug for cancer patients for mood elevation but there are limited studies about the interaction of amitriptyline with glutathione S-transferases pi (GST-pi) and glutathione S-transferases alpha (GST-alpha). GST isozymes have been implicated in chemotherapeutic drug resistance. We demonstrated that the concentration dependent inhibition of GST-pi and GST-alpha by amitriptyline followed inverse hyperbolic inhibition curves with IC50 values of 5.54 and 8.32 mM, respectively.