Poly（ADP-ribose） polymerase inhibitors as promising ：ancer therapeutics  

作　　者：Jin-xue HE Chun-hao YANG Ze-hong MIAO 

机构地区：[1]Division of Antitumor Pharmacology [2]Department of Medicinal Chemistry, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhang Jiang Hi-Tech Park, Shanghai 201203, China

出　　处：《Acta Pharmacologica Sinica》2010年第9期1172-1180,共9页中国药理学报（英文版）

基　　金：This work was supported by the grants from the National Natural Science Foundation of China （NSFC） （No 30772588 and No 30721005）, the National Science ＆ Technology Major Project＂Key New Drug Creation and Manufacturing Program＂of China （No 2009ZX09301-001） and the Science and Technology Commission of Shanghai Municipality （STCSM） （No 08DZ1980200）.

摘　　要：The year of 2005 was a watershed in the history of poly（ADP-ribose） polymerase （PARP） inhibitors due to the important findings of selective killing in BRCA-deficient cancers by PARP inhibition. The findings made PARP inhibition one of the most promising new thera- peutic approaches to cancers, especially to those with specific defects. With AZD2281 and BSI-201 entering phase III clinical trials, the final application of PARP inhibitors in clinic would come true soon. This current paper will review the major advances in targeting PARP for cancer therapy and discuss the existing questions, the answers to which may influence the future of PARP inhibitors as cancer therapeutics.The year of 2005 was a watershed in the history of poly（ADP-ribose） polymerase （PARP） inhibitors due to the important findings of selective killing in BRCA-deficient cancers by PARP inhibition. The findings made PARP inhibition one of the most promising new thera- peutic approaches to cancers, especially to those with specific defects. With AZD2281 and BSI-201 entering phase III clinical trials, the final application of PARP inhibitors in clinic would come true soon. This current paper will review the major advances in targeting PARP for cancer therapy and discuss the existing questions, the answers to which may influence the future of PARP inhibitors as cancer therapeutics.

关 键 词：poly（ADP-ribose） polymerase inhibitor DNA repair BRCA1/2 anticancer agents homologous recombination 

分 类 号：Q591.8[生物学—生物化学] TQ465.92[化学工程—制药化工]