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

Kulaksız Erkmen, Gülnihal; Dalmizrak, Ozlem; Dincsoy-Tuna, GAMZE; Dogan, Arin; Ogus, I.; Ozer, Nazmi

doi:10.3109/14756366.2011.639017

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

Kulaksız Erkmen G., Dalmizrak O., Dincsoy-Tuna G., Dogan A., Ogus I. H., Ozer N.

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

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
Dokuz Eylül University Affiliated: No

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.