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来自“大蓝”的表观遗传调节剂:对抗癌症的瑰宝。

Epigenetic modulators from "The Big Blue": a treasure to fight against cancer.

作者信息

Schnekenburger Michael, Dicato Mario, Diederich Marc

机构信息

Laboratoire de Biologie Moléculaire et Cellulaire du Cancer, Hôpital Kirchberg, 9, rue Edward Steichen, L-2540 Luxembourg, Luxembourg.

College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea.

出版信息

Cancer Lett. 2014 Sep 1;351(2):182-97. doi: 10.1016/j.canlet.2014.06.005. Epub 2014 Jun 22.

Abstract

Cancer remains a major public health problem in our society. The development of potent novel anti-cancer drugs selective for tumor cells is therefore still required. Deregulation of the epigenetic machinery including DNA methylation, histone modifications and non-coding RNAs is a hallmark of cancer, which provides potential new therapeutic targets. Natural products or their derivatives represent a major class of anti-cancer drugs in the arsenal available to the clinician. However, regarding epigenetically active anti-cancer agents for clinics, the oceans represent a largely untapped resource. This review focuses on marine natural compounds with epigenetic activities and their synthetic derivatives displaying anti-cancer properties including largazole, psammaplins, trichostatins and azumamides.

摘要

癌症仍然是我们社会中的一个主要公共卫生问题。因此,仍需要开发对肿瘤细胞具有选择性的强效新型抗癌药物。包括DNA甲基化、组蛋白修饰和非编码RNA在内的表观遗传机制失调是癌症的一个标志,这提供了潜在的新治疗靶点。天然产物或其衍生物是临床医生可用的抗癌药物中的一大类。然而,对于临床上具有表观遗传活性的抗癌药物而言,海洋在很大程度上仍是未开发的资源。本综述重点关注具有表观遗传活性的海洋天然化合物及其显示抗癌特性的合成衍生物,包括拉佐菌素、沙马普林、曲古抑菌素和天冬酰胺。

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