sepsis as the host responsive syndrome is one of the main concerning issues and costly disease on intensive care unit (icu) in the 21st century. epidemiological studies have showed that mortality rates of sepsis in icu and hospitals among 37 countries were 39.2% and 49.6% respectively [1].  complicated nature of sepsis is still not well understood and this makes it hard to treat and manage. acc...

Protein kinase CK2 is a highly pleiotropic protein capable of phosphorylating hundreds substrates. It involved in numerous cellular functions, including cell viability, apoptosis, proliferation and survival, angiogenesis, or ER-stress response. As activity found perturbed many pathological states, cancers, it becomes an attractive target for the pharma. A large number low-mass ATP-competitive i...

Most of the signal transduction pathways are mediated by protein kinases regulating every aspect of cell function. Mutations which deregulate their expression or their function or both result in cancers. Therefore, protein kinase inhibitors has become the focus of development of new therapies for cancer. Almost all 120 protein tyrosine kinases are involved in signaling, whereas only a handful o...

Although metal-based anticancer drugs have been recognized as the most effective agents over the organic compounds, non-selectivity and high toxic effects have limited their applications in a way that only three Pt-analogues have progressed into clinical use. These problems have spurred chemists to develop different strategies based on alternative targets. This work focuses on predicting potenc...

In the August issue of TiPS, Epand and Lester analysed the effect of the physicochemical properties of the membrane on protein kinase C activity. In addition to those substrates discussed that require the presence of Ca2+ and phospholipids, other substrates can be phosphorylated in the absence of these activators. It is possible that this differential substrate requirement could be exploited ph...

Glycogen synthase kinase-3 beta (GSK-3β) is implicated in abnormal hyperphosphorylation of the tau protein and its inhibitors may be a promising therapeutic approach for treating Alzheimer’s disease. Here, series C-glycosylfavone derivatives as GSK-3β was selected to perform two-dimensional quantitative structure activity relationship (2D-QSAR) method docking analysis. The 2D-QSAR model generat...

Western blot analysis of neuronal tissues taken from fear-conditioned rats showed a selective activation of phosphatidylinositol 3-kinase (PI-3 kinase) in the amygdala. PI-3 kinase was also activated in response to long-term potentiation (LTP)-inducing tetanic stimulation. PI-3 kinase inhibitors blocked tetanus-induced LTP as well as PI-3 kinase activation. In parallel, these inhibitors interfe...

Although metal-based anticancer drugs have been recognized as the most effective agents over the organic compounds, non-selectivity and high toxic effects have limited their applications in a way that only three Pt-analogues have progressed into clinical use. These problems have spurred chemists to develop different strategies based on alternative targets. This work focuses on predicting potenc...