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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A-966492是一种新型有效的PARP1和PARP2抑制剂，Ki分别为1 nM和1.5 nM。
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AZD2461是新型PARP抑制剂，能够避免由Pgp介导的olaparib抗性。
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BMN 673是一种新型的PARP抑制剂，IC50为0.58 nM，也有效抑制PARP-2，但不抑制PARG，对PTEN突变型高度敏感。
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A-966492是一种新型有效的PARP1和PARP2抑制剂，Ki分别为1 nM和1.5 nM。
More
-
AZD2461是新型PARP抑制剂，能够避免由Pgp介导的olaparib抗性。
More
-
BMN 673是一种新型的PARP抑制剂，IC50为0.58 nM，也有效抑制PARP-2，但不抑制PARG，对PTEN突变型高度敏感。
More
