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Poly (ADP-ribose) polymerase（PARP）：多腺苷二磷酸多聚酶

PARP家族由17名成员组成，是细胞凋亡核心成员caspase的切割底物，在DNA单链的断裂修复以及细胞凋亡中发挥了至关重要的作用。其作用机制：PARP有四个结构与组成-DNA结合域，caspase切割结构域，自动修饰域和催化结构域。机体代谢，化学物质或者辐射会导致DNA单链断裂损伤。当PARP检测到DNA单链断裂，会结合到DNA上，经过结构上的改变形成PAR链，对许多核蛋白进行聚腺苷二磷酸核糖基化。受它修饰的蛋白质有组蛋白、RNA聚合酶、DNA聚合酶、DNA连接酶等，并能通过组蛋白的ADP-核糖基化使组蛋白脱离下来。

PARP可以通过耗光细胞内的ATP从而导致细胞的裂解和死亡；或者通过生产的PAR刺激线粒体释放AIF，直接诱导细胞凋亡。

下面来介绍一下有关的抑制剂：

A-966492

A-966492 is a highly potent and efficacious poly(ADP-ribose) polymerase (PARP) inhibitor with a Ki and EC50 of 1 nM.

ABT-888 (Veliparib)

ABT-888 (Veliparib) is a potent PARP inhibitor to PARP-1 and PARP-2 with Kis of 5.2 and 2.9 nmol.

AG14361

AG14361 is a potent poly(ADP-ribose) polymerase (PARP-1) inhibitor with a GI50 of 10.9 ?M.

BSI-201

BSI-201 is a potent PARP1 inhibitor with strong anti-neoplastic effect.

INO-1001

INO-1001 is a novel potent PARP inhibitor with an IC50 of 3 nM.

MK-4827

MK-4827 is a potent'' selective PARP 1/2 inhibitor with IC50 of 3.8 and 2.1 nM for PARP1 and 2'' respectively.

Olaparib (AZD2281)

Olaparib (AZD2281) is a potent PARP inhibitor with IC50 of 5 and 1 nM for PARP-1and PARP-2'' respectively.

Rucaparib (AG-014699 '' PF-01367338)

Rucaparib (AG-014699 '' PF-01367338) is a PARP inhibitor (Ki'' 1.4 nmol/L).