论文部分内容阅读
聚腺苷二磷酸核糖聚合酶[poly(ADP)-ribose polymerase(PARP)]是与单链DNA损伤修复密切相关的一种核酶,其中PARP-1亚型承担了90%以上的修复任务。在肿瘤细胞中DNA损伤修复通路异常活跃,因此,抑制PARP-1的活性可以抑制肿瘤的生长。近年来,已有多个PARP-1的抑制剂进入临床研究阶段,PARP-1抑制剂已成为抗肿瘤药物研发的热点之一。本文根据PARP-1抑制剂的结构特点对其相关研究进行综述。
Poly (ADP) -ribose polymerase (PARP)] is a ribozyme closely related to the repair of single-stranded DNA, in which the PARP-1 subtype is responsible for more than 90% of the repair tasks. In tumor cells, DNA damage repair pathway is very active, therefore, inhibition of PARP-1 activity can inhibit tumor growth. In recent years, many inhibitors of PARP-1 have entered the clinical research stage. PARP-1 inhibitors have become one of the hot spots in the development of antitumor drugs. This article reviews the related studies based on the structural features of PARP-1 inhibitors.