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PARP Inhibitors As Anticancer Agents
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Abstract
Poly(ADP‐ribosyl)ation is posttranslation covalent modification, which is operated by a family of enzymes whose founding member, named PARP‐1, has been involved in a variety of physiological as well as pathological processes. In particular, PARP‐1 is activated by DNA‐strand breaks, and is a key component of the DNA repairing machinery thus acting as a caretaker of genomic stability. Over the last decade, many evidence have accumulated suggesting that PARP inhibitors may find utility as cotherapy with DNA damaging agents in many preclinical models of cancer, and also as monotherapy in some important DNA repair defective tumors. These findings are now translating into clinically useful agents that are undergoing clinical trials. In this chapter, we review the diversity of the PARP family, the significance of poly(ADP‐ribosyl)ation in DNA repairing and the mechanism of PARP inhibitors in cancer therapy. Finally, an overview of the most promising PARP inhibitors under clinical evaluation is given.
Title: PARP
Inhibitors As Anticancer Agents
Description:
Abstract
Poly(ADP‐ribosyl)ation is posttranslation covalent modification, which is operated by a family of enzymes whose founding member, named PARP‐1, has been involved in a variety of physiological as well as pathological processes.
In particular, PARP‐1 is activated by DNA‐strand breaks, and is a key component of the DNA repairing machinery thus acting as a caretaker of genomic stability.
Over the last decade, many evidence have accumulated suggesting that PARP inhibitors may find utility as cotherapy with DNA damaging agents in many preclinical models of cancer, and also as monotherapy in some important DNA repair defective tumors.
These findings are now translating into clinically useful agents that are undergoing clinical trials.
In this chapter, we review the diversity of the PARP family, the significance of poly(ADP‐ribosyl)ation in DNA repairing and the mechanism of PARP inhibitors in cancer therapy.
Finally, an overview of the most promising PARP inhibitors under clinical evaluation is given.
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