Activity of Nonnucleoside Inhibitors of O6-methylguanine-DNA Methyltransferase Repair Enzyme in Human Cells In Vitro

Pub Date : 2023-12-04 DOI:10.3103/s0095452723060105
K. S. Zhuvaka, G. P. Volynets, T. P. Ruban, Z. M. Nidoeva, A. P. Iatsyshyna, L. L. Macewizc, V. G. Bdzhola, S. M. Yarmoluk, L. L. Lukash
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Abstract

The repair enzyme O6-methylguanine-DNA methyltransferase (MGMT) eliminates alkyl lesions that play the main anticancer role in alkylating chemotherapy. The inhibition of MGMT leads to increasing effectiveness of alkylating chemotherapy. In this study, new potential MGMT inhibitors were tested. It was found that some compounds demonstrate low cytotoxicity and high effectiveness in human cells in vitro.

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体外研究o6 -甲基鸟嘌呤- dna甲基转移酶修复酶非核苷类抑制剂的活性
摘要修复酶o6 -甲基鸟嘌呤- dna甲基转移酶(MGMT)可清除烷基化化疗中起主要抗癌作用的烷基病变。MGMT的抑制导致烷基化化疗的有效性增加。在这项研究中,新的潜在的MGMT抑制剂进行了测试。研究发现,一些化合物在体外对人体细胞具有低细胞毒性和高活性。
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