Dipartimento di Chimica

Directed Enzyme Prodrugs Therapy (DEPT) as an alternative method against conventional cancer treatments

Tuğba Güngör, Çanakkale Onsekiz Mart University, Turchia

 

The seminar will be held in Aula V, ground floor, Caglioti building (CU032), 29th november at 1 pm.
 

Abstract

Directed Enzyme Prodrugs Therapy (DEPT) as an alternative method against conventional cancer treatments, in which the non-toxic prodrugs is converted to highly cytotoxic derivative, has attracted an ample attention in recent years for cancer therapy studies. Nitroreductase enzymes (NTR) catalyze the conversion of the nitro group of prodrugs via hydroxylamine to amine group and the active drug inhibits tumor formation by binding to DNA. E. coli nitroreductase/CB1954 (5-aziridinyl-2,4-dinitrobenzamide) is the best known combination for different cancer types. For this purpose, more effective NTR/prodrug combinations should be investigated for cancer therapies.

Our group synthesized and characterized various type of aromatic and heterocyclic prodrugs containing nitro group and investigated the enzymatic interaction of these potential prodrugs with our two novel nitroreductases (Ssap-NtrB and Gk-Ntr). Metabolite profiles were determined by HPLC analysis, and kinetic parameters were calculated. The prodrugs were evaluated by MTT and SRB assay in different cancer cell lines and healthy cell. Also, biological data was supported with in silico studies. According to the results, our promising enzyme/prodrug combinations may use NTR based cancer therapy.

 

Biosketch Dr. Tuğba Güngör

Dr. Tuğba Güngör was born in 1985 in Ankara, Turkey. She graduated from Ankara University, Department of Chemistry in 2007, as the top student in this department. She completed master's degree at Ankara University in 2010 with the title of “Synthesis of dioxane based thiophene and pyrrole monomers and investigation of their conductive polymer properties”. She completed doctorate program at Çanakkale Onsekiz Mart University in 2016 with the title of “Development of aromatic and heterocyclic prodrug compounds for nitroreductase based cancer therapy”. During PhD education, she went to Oregon State University, Department of Chemistry, USA in 2015 for 6 months to get some experience on natural product chemistry with the supervisor of Prof. Rich G. Carter. She started working as research assistant at Çanakkale Onsekiz Mart University since 2011. She is ongoing research in design, synthesize and characterization of novel organic bioactive molecules using for various essential medicinal applications such as anticancer, antiinflammatory, etc in Natural Products and Drug Research Laboratory. Now, she is working at Çanakkale Onsekiz Mart University, Department of Chemistry as Assoc. Proffesor.