Synthesis and Structure—Activity Relationships of Novel Poly(ADP-Ribose) Polymerase-1 Inhibitors.
✍ Scribed by Ming Tao; Chung Ho Park; Ron Bihovsky; Gregory J. Wells; Jean Husten; Mark A. Ator; Robert L. Hudkins
- Publisher
- John Wiley and Sons
- Year
- 2006
- Weight
- 31 KB
- Volume
- 37
- Category
- Article
- ISSN
- 0931-7597
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## Abstract ## Background In this study, we tested the ability of a novel poly(adenosine diphosphate ribose) polymerase (PARP) inhibitor, 10‐(4‐methyl‐piperazin‐1‐ylmethyl)‐2__H__‐7‐oxa‐1,2‐diaza‐benzo[__de__]‐anthracen‐3‐one (GPI‐15427), to enhance the effect of radiotherapy in a xenograft model
## Abstract Poly(ADP‐ribose) polymerase‐1 (PARP‐1) is a mammalian enzyme that attaches long branching chains of ADP‐ribose to specific nuclear proteins, including itself. Because its activity __in vitro__ is dependent upon interaction with broken DNA, it has been postulated that PARP‐1 plays an imp