Amitriptyline may have a supportive role in cancer treatment by inhibiting glutathione S-transferase pi (GST-pi) and alpha (GST-alpha)
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.28, sa.1, ss.131-136, 2013 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 28 Sayı: 1
- Basım Tarihi: 2013
- Doi Numarası: 10.3109/14756366.2011.639017
- Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.131-136
- Anahtar Kelimeler: Amitriptyline, anticancer drugs, GST-alpha, GST-pi, GSTs, TRICYCLIC ANTIDEPRESSANTS, ISOENZYMES, BINDING, TARGET, CELLS, TRANSPORTERS, DEPRESSION, SEROTONIN, MECHANISM, CARCINOMA
- Hacettepe Üniversitesi Adresli: Evet
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.