TY  - GEN
AU  - Kulaksiz-Erkmen,Gulnihal
TI  - Amitriptyline may have a supportive role in cancer treatment by inhibiting glutathione S-transferase pi (GST-pi) and alpha (GST-alpha) 
SN  - 1475-6366
AV  - QU4 
PY  - 2013///
PB  - Informa Healthcare
KW  - Near East University Article
KW  - Yakın Doğu Üniversitesi Makale
KW  - Biochemistry
KW  - anticancer drugs
KW  - GST-alpha
KW  - Serotonın
KW  - Transporters
N2  - 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. 

When the varied substrate was GSH, amitriptyline inhibited both isozymes competitively and similar K-i values were found for GST-pi (K-i = 1.61 +/- 0.17 mM) and GST-alpha (K-i = 1.45 +/- 0.20 mM). On the other hand, when the varied substrate was CDNB, the inhibition types were non-competitive for GST-pi (K-i = 1.98 +/- 0.31 mM) and competitive for GST-alpha (K-i = 1.57 +/- 0.16 mM). 

Amitriptyline, in addition to its antidepressant effect, might also have a minor supportive role on the effectiveness of the anticancer drugs by decreasing their elimination through inhibiting GST-pi and GST-alpha
UR  - http://library.neu.edu.tr:2048/login?url=http://dx.doi.org/10.3109/14756366.2011.639017 
ER  -