Novel modulators of poly(ADP-ribose) polymerase

Csaba Szabo, Pal Pacher, Raymond A. Swanson

    Research output: Contribution to journalArticle

    57 Scopus citations

    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.

    Original languageEnglish (US)
    Pages (from-to)626-630
    Number of pages5
    JournalTrends in Pharmacological Sciences
    Volume27
    Issue number12
    DOIs
    StatePublished - Dec 2006

    ASJC Scopus subject areas

    • Toxicology
    • Pharmacology

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