Webb1 sep. 2024 · We report on 3-bromomethyl-benzofuran-2-carboxylic acid ethyl ester (designated: MCC1019) as selective PLK1 inhibitor targeting PLK1 PBD. Cytotoxicity and fluorescence polarization-based screening were applied to a library of 1162 drug-like compounds to identify potential inhibitors of PLK1 PBD. Webb(a) Representative photomicrographs of Day 4 lenses after inhibitor addition (Plk3 inhibitor GW843682X 1 μM, Atm inhibitor KU55933 10 μM). GW843682X or KU55933 was added …
MCC1019, a selective inhibitor of the Polo-box domain of Polo-like ...
Webb10 sep. 2024 · Mechanistically, PLK3 inhibition suppresses the degradation of hypoxia-inducible factor-1α (HIF-1α) and reactive oxygen species (ROS)-mediated oxidative stress, thus protecting the renal tubular epithelial cells from cell death and preventing macrophage activation and renal inflammation. Webb24 juni 2009 · To unravel the growth inhibition mechanism of Polo-like kinase 3 (Plk3), the effect of overexpression of Plk3 was examined in 293T cells. Cell rounding, changes in actin organization and cellular detachment were induced by Plk3 transfection in a kinase activity-dependent manner. oliver projectes
Targeting Polo-Like Kinases: A Promising Therapeutic Approach …
Webb12 apr. 2024 · PI3K inhibitors are usually given to treat certain cancers that have relapsed or are unresponsive to other cancer treatments. Typically, at least two other cancer treatments need to have been tried and been unsuccessful or not tolerated before PI3K inhibitors are given. WebbTAK-960 dihydrochloride Inhibitor 99.19% TAK-960 dihydrochloride 是一种有效的,可口服的,选择性的 polo-like kinase 1 (PLK1) 抑制剂,IC 50 为 0.8 nM。 TAK-960 dihydrochloride 对 PLK2 和 PLK3 也有抑制作用,IC 50 分别为 16.9 和 50.2 nM。 TAK-960 dihydrochloride 抑制多种肿瘤细胞系的增殖,对多种肿瘤异种移植具有显著的疗效。 Webb20 juni 2024 · PLK3 was suggested to control cell response to various forms of stress including osmotic stress, hypoxia, DNA damage, and Golgi stress . Whereas PLK1 is rapidly inhibited after stress, activity of PLK3 is believed to be stimulated by stress [10,12,13]. oliver project runway