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Novel modulators of poly(ADP-ribose) polymerase |
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| Authors: | Szabo Csaba Pacher Pal Swanson Raymond A |
| Institution: | 1Department of Surgery, University of Medicine and Dentistry, New Jersey Medical School, 185 South Orange Avenue, University Heights Newark, NJ 07103, USA 2Section on Oxidative Stress Tissue Injury, Laboratory of Physiological Studies, National Institutes of Health and National Institute on Alcohol Abuse and Alcoholism, 5625 Fishers Lane, Bethesda, MD 20892-9413, USA 3Department of Neurology, University of California and Veterans Affairs Center, 4150 Clement Street, San Francisco, CA 94121, USA |
| Abstract: | The nuclear enzyme poly(ADP-ribose) polymerase (PARP)-1 has an important role in regulating cell death and cellular responses to DNA repair. Pharmacological inhibitors of PARP have entered clinical testing as cytoprotective agents in cardiovascular diseases and as adjunct antitumor therapeutics. Initially, it was assumed that the regulation of PARP occurs primarily at the level of DNA breakage: recognition of DNA breaks was considered to be the primary regulator (activator) or the catalytic activity of PARP. Recent studies have provided evidence that PARP-1 activity can also be modulated by several endogenous factors, including various kinases, purines and caffeine metabolites. There is a gender difference in the contribution of PARP-1 to stroke and inflammatory responses, which is due, at least in part, to endogenous estrogen levels. Several tetracycline antibiotics are also potent PARP-1 inhibitors. In this article, we present an overview of novel PARP-1 modulators. |
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