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PARP-1, an enzyme that catalyzes the attachment of ADP ribose units to target proteins, plays at least two important roles in transcription regulation. First, PARP-1 modifies histones and creates an anionic poly(ADPribose) matrix that binds histones, thereby promoting the decondensation of higher-order chromatin structures. Second, PARP-1 acts as a component of enhancer/promoter regulatory complexes. Recent studies have shown that both of these activities are critical for gene regulation in vivo.