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, cilt.28, ss.131-136, 2013 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 28 Konu: 1
  • Basım Tarihi: 2013
  • Doi Numarası: 10.3109/14756366.2011.639017
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Sayfa Sayıları: ss.131-136

Özet

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.