Acta Pharmacologica Sinica (2010) 31: 1172–1180; doi: 10.1038/aps.2010.103

Acta Pharmacologica Sinica (2010) 31: 1172–1180; doi: 10.1038/aps.2010.103; published online 2 Aug 2010

Review

poly(ADP-ribose) polymerase inhibitors as promising cancer therapeutics

Jin-xue HE¹, Chun-hao YANG², Ze-hong MIAO^{1, *}

¹Division of Antitumor Pharmacology and ²Department 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

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 therapeutic 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.

Keywords: poly(ADP-ribose) polymerase inhibitor; DNA repair; BRCA1/2; anticancer agents; homologous recombination

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).

* To whom correspondence should be addressed.
E-mail zhmiao@mail.shcnc.ac.cn
Received 2010-05-31 Accepted 2010-06-25

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