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针对癌症治疗中的 DNA 损伤反应激酶。

Targeting DNA damage response kinases in cancer therapy.

机构信息

Fundación Instituto Leloir - Instituto de Investigaciones Bioquímicas de Buenos Aires. Consejo de Investigaciones Científicas y Técnicas. Avenida Patricias Argentinas 435, C1405BWE, Buenos Aires, Argentina.

出版信息

Mutat Res. 2020 May-Dec;821:111725. doi: 10.1016/j.mrfmmm.2020.111725. Epub 2020 Nov 1.

Abstract

Cancer cells die when their decimated DNA damage response (DDR) unsuccessfully handles DNA damage. This notion has been successfully exploited when targeting PARP (poly ADP-ribose polymerase) in homologous recombination-deficient cells. With the greater understanding of DDR achieved in the last decade, new cancer therapy targets within the DDR network have been identified. Intriguingly, many of the molecules that have advanced into clinical trials are inhibitors of DDR kinases. This special issue is devoted to discussing the mechanism of cell killing and the level of success that such inhibitors have reached in pre-clinical and clinical settings.

摘要

当受损的 DNA 损伤反应 (DDR) 未能处理 DNA 损伤时,癌细胞会死亡。当靶向同源重组缺陷细胞中的 PARP(多聚 ADP-核糖聚合酶)时,这一概念已被成功利用。在过去十年中,随着对 DDR 理解的加深,DDR 网络中的新癌症治疗靶标已经被确定。有趣的是,许多进入临床试验的分子是 DDR 激酶抑制剂。本期特刊专门讨论细胞杀伤的机制以及此类抑制剂在临床前和临床环境中取得的成功程度。

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