摘要
聚ADP核糖聚合酶-1(PARP-1)在DNA单链断裂的碱基切除修复中具有非常重要的作用,在人类多种肿瘤中过度表达且过度表达者预后较差。利用合成致死原理,对于因BRCAl或BRCA2基因突变而同源重组修复DNA双链断裂缺陷的肿瘤细胞,抑制其PARP-1活性将导致肿瘤细胞死亡PARP抑制剂对于携带BRCA基因突变肿瘤患者具有一定的治疗作用,其临床应用价值已在多项临床试验中得到了证实。PARP-1可能会成为肿瘤治疗的重要靶点。
Poly （ ADP-ribose ） polymerase-1 （ PARP-1 ） has a vital role in base excision repair of single-strand DNA breakage, and its over-expression has often been observed in various human tumor types, which correlates with a poor outcome. PARP-1 inhibition has been exploited in the repair of double-strange DNA breakage through a synthetic lethal approach for killing tumor cells with defects. This process is done via homologous recombination, particularly in the context of BRCA1 or BRCA2 mutation. Many clinical trials have demonstrated the clinical application value of PARP inhibitors in the treatment of cancer with BRCA mutations. PARP- 1 will be an important target of tumor therapy.
出处
《中国肿瘤临床》
CAS
CSCD
北大核心
2011年第24期1612-1615,共4页
Chinese Journal of Clinical Oncology
