• Curr Clin Pharmacol · Aug 2010

    Review

    Inducing synthetic lethality using PARP inhibitors.

    • David S Boss, Jos H Beijnen, and Jan H M Schellens.
    • The Netherlands Cancer Institute, Department of Medical Oncology, The Netherlands.
    • Curr Clin Pharmacol. 2010 Aug 1; 5 (3): 192-5.

    AbstractThe 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.

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