Poly(ADP-ribosyl)ation polymerases: mechanism and new target of anticancer therapy.

Abstract	Poly(ADP-ribose)polymerase (PARP) is a ubiquitously present nuclear enzyme that is not only involved in many important cellular pathways but also contributes to chromosomal structure and genomic stability. The development of highly selective and potent PARP inhibitors has become of increasing clinical interest because of their promising efficacy in patients with breast or ovarian cancer. Furthermore, recent Phase I and Phase II trials have demonstrated that PARP inhibitors have low toxicity rates. In particular patients with either deficiency or dysfunction of BRCA, which is involved in DNA double strand break repair, appear to benefit from PARP inhibition. This article summarizes the present knowledge regarding the physiological function of PARP and ([poly]ADP-ribose) PAR, the functional product of PARP, the development of PARP inhibitors, the recent clinical data of PARP inhibitors in cancer treatment and the selection of patients who may benefit from PARP inhibition.
Authors	Florian Heitz, Philipp Harter, Nina Ewald-Riegler, Michael Papsdorf, Stefan Kommoss, Andreas du Bois
Journal	Expert review of anticancer therapy (Expert Rev Anticancer Ther) Vol. 10 Issue 7 Pg. 1125-36 (Jul 2010) ISSN: 1744-8328 [Electronic] England
PMID	20645701 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
Chemical References	Antineoplastic Agents Apoptosis Regulatory Proteins BLID protein, human BRCA1 Protein BRCA1 protein, human BRCA2 Protein BRCA2 protein, human DNA, Neoplasm Enzyme Inhibitors Neoplasm Proteins Poly(ADP-ribose) Polymerase Inhibitors Poly Adenosine Diphosphate Ribose PARP1 protein, human Poly (ADP-Ribose) Polymerase-1 Poly(ADP-ribose) Polymerases PTEN Phosphohydrolase PTEN protein, human
Topics	Aged Antineoplastic Agents (pharmacology, therapeutic use) Apoptosis Regulatory Proteins BRCA1 Protein (deficiency, physiology) BRCA2 Protein (deficiency, physiology) Breast Neoplasms (drug therapy, enzymology) Clinical Trials, Phase I as Topic Clinical Trials, Phase II as Topic DNA Breaks, Single-Stranded DNA Repair DNA, Neoplasm (metabolism) Drug Delivery Systems Drug Resistance, Neoplasm Enzyme Inhibitors (pharmacology, therapeutic use) Female Humans Multicenter Studies as Topic Neoplasm Proteins (antagonists & inhibitors, physiology) Ovarian Neoplasms (drug therapy, enzymology) PTEN Phosphohydrolase (deficiency, genetics, physiology) Poly (ADP-Ribose) Polymerase-1 Poly Adenosine Diphosphate Ribose (metabolism) Poly(ADP-ribose) Polymerase Inhibitors Poly(ADP-ribose) Polymerases (physiology)

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