针对PARP的抗肿瘤靶向药物研究进展  

Progress in research of drugs targeting PARP for cancer therapy

作　　者：秦臻 吴逸园 罗侣松 汪来 魏旻 

机构地区：[1]百济神州(北京)生物科技有限公司,北京102206

出　　处：《中国新药杂志》2014年第17期2052-2056,共5页Chinese Journal of New Drugs

基　　金：首都市民健康项目培育(Z121100007512012);科技北京百名领军人才培养工程(Z131102000513020);北京市科技新星计划(Z111102054511011)

摘　　要：聚腺苷二磷酸核糖聚合酶(PARP)通过碱基切除修复方式对单股DNA进行修复,是近年来在癌症治疗领域非常热门的一个靶点。目前,PARP抑制剂在多个肿瘤适应症中进入了临床试验。众多的试验数据表明PARP抑制剂不仅可以作为化疗和放疗的增敏剂,而且在BRCA1/2基因突变的乳腺癌中可单独使用,选择性杀死DNA修复缺陷的癌细胞。本文主要对在研PARP抑制剂的作用机制以及5个最重要的PARP抑制剂的临床研究结果进行了综述。Poly （ADP-ribose） polymerase （PARP） represents a currently important target in cancer thera- py, which is essential to the repair of single strand DNA breaks via the base excision repair pathway. Inhibitors of PARP have been in clinical trials with multiple indications. Recently, clinical data suggested that PARP inhibitors could be used not only as chemo/radiotherapy sensitizers, but also as single agents to selectively kill cancers that are defective in DNA repair, particularly cancers with mutations in the breast cancer associated BRCA1/2 genes. This re- view summarized the mechanism of PARP inhibitors and current clinical data of five most important PARP inhihltar~

关 键 词：PARP抑制剂 BRCA1/2基因突变 靶向肿瘤治疗 临床试验 

分 类 号：R979.1[医药卫生—药品]