SÜLFONAMİDOBENZOTİYAZOL TÜREVİ hGSTP1-1 İNHİBİTÖRLERİNİN TASARIMI

Amaç: Glutatyon Transferazlar (GST), ekzojen ve endojen kaynaklı, elektrofilik ve hidrofobik bileşiklerin GSH ile konjugasyonunu katalizleyen Faz-II detoksifikasyon enzim ailesidir. GST izozimlerinden en önemlisi olan hGSTP1-1’in çok farklı insan kaynaklı tümörde fazla miktarda salgılandığı ve kanser tedavisinde çoklu ilaç direnç (MDR) gelişimine sebep olduğu bilinmektedir. Tüm bu nedenlerden dolayı son zamanlarda hGSTP1-1 enzimi kanser tedavisi için bir hedef haline gelmiştir. Bu çalışmanın amacı yeni hGSTP1-1 inhibitörleri tasarlamaktır.

DESIGN OF SULFONAMIDOBENZOTHIAZOLE DERIVATIVES AS hGSTP1-1 INHIBITORS

Objective: The glutathione transferases (GSTs) are a family of widely distributed Phase II detoxification enzymes that catalyse the conjugation of exogenius and endogenius electrophilic and hydrophobic compounds. GSTP1-1 is frequently overexpressed in rat and human tumours. It is suggested that overexpression of hGSTP1-1 by human tumor cells may play a role in multi drug resistance (MDR) to cancer chemotherapy. Hence, hGSTP1-1 can be a promising target for cancer treatment. The aim of this study is to design new hGSTP1-1 inhibitors.

Keywords:

anticancer, docking, drug resistance, hGSTP1-1 sulfonamidobenzothiazole,

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