O6-methylguanine DNA methyltransferase (MGMT) is a molecular determinant for potency of the DNA-epidermal growth factor receptor (EGFR) targeting combi- molecule ZRS1
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MGMT is a molecular determinant for potency of the DNA-EGFR-combi-molecule ZRS1.
To enhance the potency of current EGFR inhibitors, we developed a novel strategy that seeks to confer them an additional DNA damaging function, leading to the design of drugs termed combi-molecules. ZRS1 is a novel combi-molecule that contains an EGFR tyrosine kinase targeting quinazoline arm and a methyltriazene-based DNA damaging one. We examined its effect on human tumor cell lines with vari...
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To enhance the potency of current EGFR inhibitors, we developed a novel strategy that seeks to confer them an additional DNA damaging function, leading to the design of drugs termed combi-molecules. ZRS1 is a novel combi-molecule that contains an EGFR tyrosine kinase targeting quinazoline arm and a methyltriazenebased DNA damaging one. We examined its effect on human tumor cell lines with varie...
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Background: ATP-binding cassette membrane transporter G2 (ABCG2) gene is one of transporter family and well characterized for their association with chemoresistance. Promoter methylation is a mechanism for regulation of gene expression. O6-Methyl guanine DNA methyl transferase (MGMT) gene plays a fundamental role in DNA repair. MGMT has the ability to remove alkyl adducts from DNA at the O6 pos...
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The present study aimed to evaluate the expression of p53, Ki-67, epidermal growth factor receptor (EGFR) and O6-methylguanine-DNA methyltransferase (MGMT), and to analyze the correlation between their expression and the histological grade of the tumors in 152 patients with gliomas. The tumors were classified according to the recommendations of the World Health Organization (WHO; 2007) into gra...
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Abstract Background: Sporadic colorectal cancer is the fourth most common cancer in Iran. The DNA repair protein O6-methylguanine-DNA methyltransferase (MGMT) is involved in the cellular defense against alkylating agents. Genetic alterations in the MGMT gene may impair the protein’s ability to remove alkyl groups from the O6-position of guanine, thereby raising the mutation rate and increasi...
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