BKM120 (Buparlisib) is one of the most advanced phosphoinositide 3-kinase (PI3K) inhibitors for the treatment of cancer, but it interferes as an off-target effect with microtubule polymerization. Here, we developed two chemical derivatives that differ fr
PI3Kδ inhibitors (PI3Kδi) demonstrate impressive clinical efficacy and, alongside other signaling inhibitors, are revolutionizing the treatment of hematological malignancies. However, only limitedin vivodata are available regarding their mechanism of action. With the rising...
In this article, we describe the PI3K signaling pathway, the prognostic value of PI3K pathway mutations, as well as the mechanism of action of buparlisib. Lastly, we discuss preliminary results of preclinical and clinical studies showing the efficacy and safety profile of this agent in breast ...
Cell panel profiling reveals conserved therapeutic clusters and differentiates the mechanism of action of different PI3K/mTOR, Aurora kinase and EZH2 inhibitors Cell panel profiling reveals conserved therapeutic clusters and differentiates the mechanism of action of different PI3K/mTOR, Aurora kinase and ...
These results clearly indicated that the mechanism of action of Tan I involved, at least partially, an effect on the PI3K/Akt/mTOR signaling pathway, providing new information for anticancer drug design and development. 展开 关键词: tanshinone I, breast cancer, cell cycle, PI3K/Akt/mTOR, ...
Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J 2000; 351: 95–105. Google Scholar Schultz RM, Merriman RL, Andis SL, et al. In vitro and in vivo antitumor activity of the phosphatidylinositol-3-kinase inhibitor, wortmannin. Anticancer Res 1995;...
It was established that abietic acid declined the cell viability of HNE1 cancer cells with minimal effects on the normal NP69 cells indicative of the selective cancer cells activity of test molecule (abietic acid). Investigation of the mechanism of the action of abietic acid revealed that abietic...
Xu et al. [63] investigated the mechanism of action of betulinic acid in inducing apoptosis in Hela cells and found that after treatment with 30 μmol/L betulinic acid (12, 24, 36, and 48 h), the viability of Hela cells generally decreased, caspase-9, Bad, and Reactive Oxygen ...
As shown in Figure 6a, most of the PI3K inhibitors reduced the level of β-TrCP1 in these cells. Notably, PI3K inhibitors, which are known to inhibit preferentially PI3Kα, markedly reduced the β-TrCP1 protein, whereas PI3K inhibitors (TGX221, TG100-115 and IC-87114) specific to other ...
Over the past two decades, new insights have positioned phosphoinositide 3-kinase-γ (PI3Kγ) as a context-dependent modulator of immunity and inflammation. Recent advances in protein structure determination and drug development have allowed for generation of highly specific PI3Kγ inhibitors, with the...