多肽类DNA甲基化转移酶抑制剂
近年来，DNA 甲基化作为研究较为广泛的表观遗传修饰方式之一受到越来越多学者的关注。异常的DNA甲基化可以诱发肿瘤的发生，DNA甲基化转移酶抑制剂可改变异常的DNA甲基化从而达到恶性肿瘤的效果。目前已报道了各种作用于DNA甲基化转移酶的抑制剂，其中包括多肽类化合物。本文就现有研究开发的用于肿瘤的多肽类DNA甲基化转移抑制剂进行了综述分析。 安徽大学学报
标签：异常DNA甲基化；DNA甲基化转移酶抑制剂；多肽类抑制剂
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【Abstract 】 Recently, the epigenetics has come to the fore in cancer research. DNA methylation, one of the best studied of epigenetic modifications, has accepted more and more attention. Aberrant DNA methylation can induce cancer. DNMT inhibitors can invert the aberrant methylation and thereby cure the cancer. Diverse classes of chemical compounds including peptide are being discovered and evaluated as DNMT inhibitors targeting DNA hypermethylation. This review will mainly discuss the developing peptide inhibitors of DNMT for cancer.
【Key words】Aberrant DNA methylation； DNMT inhibitors； Peptide inhibitors.
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百家讲坛周汝昌
［4］Vucic EA, Brown CJ, Lam WL. Epigenetics of cancer progression. Pharmacogenomics,2008,:1-8.
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［10］Winquist E, Knox J, Ayoub JP. Phase II trial of DNA methyltransferase 1inhibition with the antisense oligonucleotide MG98 in patients with metastatic renalcarcinoma: A National Cancer Institute of Canada Clinical TrialsGroup investigational new drug study. Invest New Drugs, 2006, 24:159-167.
［11］Vlieghe P, Lisowski V, Martinez J, et al. Synthetic therapeutic peptides: science and market. Drug Discovery Today, 2010, 15:3219-3235.2012年浙江高考作文
［20］Kuck D, Singh N, Lyko F, et al. Novel and selective DNA methyltransferase inhibitors: docking-based virtual screening and experimental evaluation. Bioorganic & Medicinal Chemistry, 2010, 18:822-829.
［21］Franco JM, Vallejo FL, Kuck D, et al. Natural products as DNA methyltransferase inhibitors: a computer-aided discovery approach. Mol Divers, 2010,15(2):293-304.酶制剂
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