The effect of PARP inhibitor on ischaemic cell death, its related inflammation and survival signals - Koh, Park, et al. - 2004Koh SH, Park Y, Song CW et al. The effect of PARP inhibitor on ischaemic cell death, its related inflammation and survival signals. Eur J Neurosci 2004; 20:...
PARP抑制剂不良反应可能与药物在靶效应(on-target effect)和脱靶效应(off-target effect)相关,特点如下:(1)不同PARP抑制剂的不良反应特征相似,但不同药物具体的不良反应发生率、严重程度等存在各自特征[11]。在绝大多数药物相关的不良反应处理上,不同药...
PARP抑制剂不良反应可能与药物在靶效应(on-target effect)和脱靶效应(off-target effect)相关,特点如下:(1)不同PARP抑制剂的不良反应特征相似,但不同药物具体的不良反应发生率、严重程度等存在各自特征[11]。在绝大多数药物相关的不良反应处理上,不同药物可以遵循相同的处理原则,但某药物独有的不良反应应该采取独特...
和几种已经被FDA获批的PARP1 inhibitor(例如Olaparib 和Talazoparib)比起来, nimbolide 展现出了更强的PARP1捕获能力。然而,与传统的PARP抑制剂不同,Nimbolide的处理诱导了PARP1(实际是PARylated-PARP1)和PARylation依赖的DNA损伤修复因子(如XRCC1)的双重捕获,从而...
(PARPs) using NAD+as ADP-ribose donor. PARPs play an indispensable role in DNA damage repair and small molecule PARP inhibitors have emerged as potent anticancer drugs. However, to date, PARP inhibitor treatment has been restricted to patients with BRCA1/2 mutation-associated breast and ovarian ...
The aim of our study was to evaluate whether PARP is expressed in post-ischemic liver, and to examine the effect of the administration of PJ-34 PARP inhibitor on liver function, histopathology, terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling (TUNEL) reaction, and the ...
Recently, a first-in-class ARH3 inhibitor was reported, and the availability of compounds abrogating the activity of dePARylating enzymes beyond PARG and ARH3 seems in reach [56]. PARP1 in DNA repair and chromatin remodeling In the context of DNA repair, the best-studied role of PARP1 ...
It has been reported that talazoparib is the most effective PARP trapping agent14, as well as the most potent PARP inhibitor in SCLC clinical testing15. Fig. 1 Properties of PARP inhibitors. a Structures of 5 clinical therapeutic PARP inhibitors and the 2 PARP imaging agents. b Heatmap ...
changed receptor binding profiles of mutant viruses as detected by glycan range analysis. Indicating the inhibitor functionalization to 2,6-α-sialyllactose (SL) and modifying the linker yielded a rationally created inhibitor covering a long spectral range of inhibited IAV strains. These outcomes high...
Moreover, we have demonstrated that the cytotoxic effect of talazoparib can be potentiated when combined with the HDAC inhibitor (HDACi) romidepsin. This combination synergizes the downregulation of the DNA-repair genes and stimulates apoptosis via the Blimp-1 (PRDM1)/Bax axis. We conclude that...