Inducing Synthetic Lethality using PARP Inhibitors

Author(s): David S. Boss, Jos H. Beijnen, Jan H.M. Schellens

Journal Name: Current Clinical Pharmacology
Continued as Current Reviews in Clinical and Experimental Pharmacology

Volume 5 , Issue 3 , 2010


The enzyme poly(ADP)-ribose polymerase-1 (PARP-1) plays an important role in the repair of DNA damage via a mechanism called base excision repair (BER). Initially, inhibition of PARP-1 showed to be a promising anti-tumor strategy in preclinical models using BRCA1 and BRCA2 deficient tumor cell lines. More recently, several small molecules targeting PARP-1 entered the clinic and demonstrated compelling anti-tumor activity in patients with BRCA deficient breast and ovarian cancers, and in patients with triple-negative breast cancer. In this review we aim to summarize the most recent advances in the development of PARP inhibitors, with a focus on the clinical data.

Keywords: Synthetic lethality, repair mechanism, PARP, BRCA deficient, olaparib

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Article Details

Year: 2010
Published on: 01 March, 2012
Page: [192 - 195]
Pages: 4
DOI: 10.2174/157488410791498798
Price: $65

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