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New PARP targets for cancer therapy

机译:癌症治疗的新PARP目标

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Poly(ADP-ribose) polymerases (PARPs) modify target proteins post-translationally with poly(ADP-ribose) (PAR) or mono(ADP-ribose) (MAR) using NAD~+ as substrate. The best-studied PARPs generate PAR modifications and include PARPl and the tankyrase PARP5A, both of which are targets for cancer therapy with inhibitors in either clinical trials or preclinical development. There are 15 additional PARPs, most of which modify proteins with MAR, and their biology is less well understood. Recent data identify potentially cancer-relevant functions for these PARPs, which indicates that we need to understand more about these PARPs to effectively target them.
机译:聚(ADP-核糖)聚合酶(PARP)使用NAD〜+作为底物,用聚(ADP-核糖)(PAR)或单(ADP-核糖)(MAR)在翻译后修饰靶蛋白。研究最深入的PARP会产生PAR修饰,包括PARP1和tankyrase PARP5A,两者都是在临床试验或临床前开发中使用抑制剂进行癌症治疗的靶标。另外还有15种PARPs,其中大多数都用MAR修饰蛋白质,其生物学研究还很少。最近的数据确定了这些PARP的潜在癌症相关功能,这表明我们需要更多地了解这些PARP才能有效地针对它们。

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