PDD 00017273 | PARG 抑制剂 | MCE - MCE-生物活性分子大师
pdd 00017273 是一种有效的 parg 抑制剂，ic 50 为 26 nm，k d 为 1.45 nm。 pdd 00017273 (10 μm) 不抑制五种常见的细胞色素 p450 酶。pdd 00017273 (30 μm) 适度增加磷酸化 h2ax (γh2ax) 强度，pdd 00017273 也通过 dna 损伤后的 parg 抑制降低 nad/h。
Selective small molecule PARG inhibitor causes replication fork ...
2019年12月11日 · We sought to test PARG inhibition in cancer cells and found that although existing PARG inhibitors (PARGi) have proven valuable 29,30,31,36, issues with potency, bioavailability, rapid clearance...
Poly (ADP-Ribose) Glycohydrolase (PARG) vs. Poly (ADP-Ribose ...
PARGi or PARG depletion has been observed to be synthetically lethal in BRCA2 depleted and deficient breast cancer cells (Fathers et al., 2012; Gravells et al., 2017). PARG inhibition caused an increase in replication fork collapse and replication associated DNA damage ( Fathers et al., 2012 ; Gravells et al., 2017 ).
Frontiers | Poly (ADP-Ribose) Glycohydrolase (PARG) vs. Poly (ADP ...
2020年8月27日 · PARGi or PARG depletion has been observed to be synthetically lethal in BRCA2 depleted and deficient breast cancer cells (Fathers et al., 2012; Gravells et al., 2017). PARG inhibition caused an increase in replication fork collapse and replication associated DNA damage ( Fathers et al., 2012 ; Gravells et al., 2017 ).
Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes ... - PubMed
2021年10月27日 · Inhibition of PARG leads to DNA repair interruption and consequently induces cell death. This study aims to evaluate the effect of a PARG inhibitor (PARGi) on epithelial ovarian cancer (OC) cell lines, alone and in combination with a PARP inhibitor (PARPi) and/or Cisplatin.
Replication catastrophe is responsible for intrinsic PAR glycohydrolase ...
2021年10月16日 · PARGi sensitivity was identified in both ovarian cancer cell lines and patient-derived OCMs, with sensitivity accompanied by markers of persistent replication stress, and a pre-mitotic cell cycle block. Moreover, DNA replication genes are down-regulated in PARGi-sensitive cell lines consistent with an inherent DNA replication vulnerability.
PARG inhibition induces nuclear aggregation of PARylated PARP1
2024年11月7日 · Here, we report a previously unknown effect of PARG inhibition resulting in the formation of nuclear PARylated PARP1 aggregates. PARGi have been shown to cause increased PARylation of PARP1; however, the functional consequences on DNA repair, DNA replication, and overall cell health were unclear.
The interplay of TARG1 and PARG protects against genomic …
2023年9月26日 · PARGi treatment of TARG1-KO cells significantly decreased cell proliferation, as shown by reduced EdU incorporation, induced G 2 /M arrest, and a slight but significant increase in the percentage of polyploid cells with >4 N DNA …
Targeting PARG induces tumor cell growth inhibition and …
PARG inhibition (PARGi) decreases basal and IL-6-induced phosphorylated STAT3 (pSTAT3) in immune cells and stimulates immune activation in vitro. (A) Splenocytes from tumor-free mice were isolated and cultured in the presence of vehicle (DMSO), 10 µM olaparib (PARPi), or 10 µM COH34 (PARGi) overnight.
CHK1 inhibitor induced PARylation by targeting PARG causes …
2024年6月11日 · PARGi in OC cells induces replication stress and ATR-mediated CHK1 phosphorylation. PARG is the major cellular enzyme that exhibits exo and endo-glycohydrolase activity and responsible for recycling ADP-ribose .