parp-mediated

Talazoparib (LT-673) 是一种 PARP 抑制剂，可以抑制 PARP 1和 PARP 2 (Ki=1.2 0.87 nM)，具有口服活性。Talazoparib 具有抗肿瘤活性，可以通过阻断 PARP 酶活性以及将 PARP 捕获在 DNA 损伤位点上来诱导肿瘤细胞死亡。

Dehydrocorydaline (13-Methylpalmatine) 是一种生物碱。它调节Bax，Bcl-2蛋白表达，激活caspase-7，caspase-8，并使PARP 失活。它能增强p38 MAPK 活化，具有抗炎、抗癌等功效。它具有强大的抗疟疾作用，并具低细胞毒性。

JGB1741 (ILS-JGB-1741) 是一种有效的选择性 SIRT1 抑制剂，IC50 为 15 μM。 JGB1741 调节 Bax Bcl2 比率、细胞色素 c 释放和 PARP 裂解并增加乙酰化 p53 水平，导致 p53 介导的细胞凋亡。 JGB1741可用于乳腺癌研究。

ST7710AA1 is a PARP-1 inhibitor that acts by showing significant in vitro target inhibition and capability to substantially bypass the multidrug resistance mediated by Pgp.

Pamiparib is a highly potent and selective PARP inhibitor. BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, pro

Dehydrocorydaline nitrate 是生物碱。Dehydrocorydaline 调节 Bax，Bcl-2蛋白表达，激活 caspase-7，caspase-8，并使 PARP 失活。它能增强 p38 MAPK 活化，具有抗炎、抗癌、抗疟疾等功效。

Cucurbitacin IIA (Dihydrocucurbitacin Q1) 是从园果雪胆中分离得到的一种三萜烯，可诱导细胞凋亡和增强自噬，有助于葫芦素IIA 对炎症相关疾病的抗炎活性。它可降低癌细胞中生存素的表达，降低磷酸化组蛋白 H3 的水平，增加裂解的 PARP 的水平。

CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and Bcl-x(L). CGP74514A treatment (5 microM; 18 hr) resulted in increased p21(CIP1) expression, p27(KIP1) degradation, diminished E2F1 expression, and dephosphorylation of p34(CDC2). It also induced early (i.e., within 2 hr) inhibition of CDK1 activity and dephosphorylation of pRb, followed by pRb degradation, but did not block pRb phosphorylation at CDK2- and CDK4- specific sites. These findings indicate that the selective CDK1 inhibitor, CGP74514A , induces complex changes in cell cycle......

Pamiparib, also known as BGB-290, is a highly potent and selective PARP inhibitor with favorable drug metabolism and pharmacokinetic properties. BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability, and eventually leads to apoptosis. BGB-290 may both potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell chemo- and radioresistance.

Dehydrocavidine (Dehydrocorydaline) 具有抗肿瘤活性，它通过诱导调节 Bax Bcl-2 介导的细胞凋亡、激活半胱天冬酶以及切割 PARP 来抑制 MCF-7 细胞增殖。