Novel modulators of poly(ADP-ribose) polymerase

Csaba Szabo, Pal Pacher, Raymond A. Swanson

Research output: Contribution to journalArticle

54 Citations (Scopus)

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
Externally publishedYes

Fingerprint

Poly(ADP-ribose) Polymerases
Modulators
Purines
DNA Breaks
DNA
Caffeine
Tetracycline
DNA Repair
Estrogens
Cell Death
Cardiovascular Diseases
Phosphotransferases
Cell death
Stroke
Metabolites
Poly (ADP-Ribose) Polymerase-1
Pharmacology
Anti-Bacterial Agents
Catalyst activity
Repair

ASJC Scopus subject areas

  • Pharmacology
  • Toxicology

Cite this

Novel modulators of poly(ADP-ribose) polymerase. / Szabo, Csaba; Pacher, Pal; Swanson, Raymond A.

In: Trends in Pharmacological Sciences, Vol. 27, No. 12, 12.2006, p. 626-630.

Research output: Contribution to journalArticle

Szabo, Csaba ; Pacher, Pal ; Swanson, Raymond A. / Novel modulators of poly(ADP-ribose) polymerase. In: Trends in Pharmacological Sciences. 2006 ; Vol. 27, No. 12. pp. 626-630.
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