a Record control number 000313663400016

a ISSN 1475-6366

a Original cataloging agency NEU GrandLibrary

a Language code of text/sound track or separate title eng

a Classification number QU4

b Item number .A45 2013

a Personal name Kulaksiz-Erkmen, Gulnihal.

h Medium Electronic Document

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

c Statement of responsibility, etc Gülnihal Kulaksiz-Erkmen, Özlem Dalmizrak, Gamze Dincsoy-Tuna, Arın Doğan, I. Hamdi Oğuş, Nazmi Özer

b Name of publisher, distributor, etc Informa Healthcare,

c Date of publication, distribution, etc 2013.

a Summary, etc 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.

a Topical term or geographic name as entry element Near East University Article

a Topical term or geographic name as entry element Yakın Doğu Üniversitesi Makale

a Topical term or geographic name as entry element Biochemistry

a Topical term or geographic name as entry element anticancer drugs;

a Topical term or geographic name as entry element GST-alpha;

a Topical term or geographic name as entry element Serotonın

a Topical term or geographic name as entry element Transporters

g Relationship information Feb 2013, Volume: 28, Issue:1, Pages: 131-136

t Title Journal Of Enzyme Inhıbıtıon And Medıcınal Chemıstry

x International Standard Serial Number 14756366

u Uniform Resource Identifier http://library.neu.edu.tr:2048/login?url=http://dx.doi.org/10.3109/14756366.2011.639017