PARP
PARP (Poly (ADP-ribose) polymerase) is a family of proteins involved in a number of cellular processes involving mainly DNA repair and programmed cell death. The PARP family comprises 17 members. They have all very different structures and functions in the cell. PARP1, PARP2, VPARP (PARP4), Tankyrase-1 and -2 (PARP-5a or TNKS, and PARP-5b or TNKS2) have a confirmed PARP activity. Others include PARP3, PARP6, TIPARP (or "PARP7"), PARP8, PARP9, PARP10, PARP11, PARP12, PARP14, PARP15, and PARP16. PARP is found in the cell’s nucleus. The main role is to detect and signal single-strand DNA breaks (SSB) to the enzymatic machinery involved in the SSB repair. PARP activation is an immediate cellular response to metabolic, chemical, or radiation-induced DNA SSB damage.
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NU 1025是活性的 PARP 抑制剂。
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Veliparib (ABT-888)是一种有效的PARP1和PARP2抑制剂，Ki分别为5.2 nM和2.9 nM，抑制SIRT2。
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XAV-939能够通过抑制tankyrase1/2而选择性抑制Wnt/β-catenin介导的转录，IC50分别为11 nM/4 nM，对CRE， NF-κB和TGF-β无抑制作用。
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PJ34是一种PARP抑制剂，EC50为20 nM，同等效果作用于PARP1/2。
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AG14361是PARP1抑制剂，Ki<5 nM，比苯甲酰胺的抑制性强1000倍。
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NU 1025是活性的 PARP 抑制剂。
More
-
Veliparib (ABT-888)是一种有效的PARP1和PARP2抑制剂，Ki分别为5.2 nM和2.9 nM，抑制SIRT2。
More
-
XAV-939能够通过抑制tankyrase1/2而选择性抑制Wnt/β-catenin介导的转录，IC50分别为11 nM/4 nM，对CRE， NF-κB和TGF-β无抑制作用。
More
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PJ34是一种PARP抑制剂，EC50为20 nM，同等效果作用于PARP1/2。
More
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AG14361是PARP1抑制剂，Ki<5 nM，比苯甲酰胺的抑制性强1000倍。
More
