The erythropoietin (Epo) receptor belongs to the cytokine receptor superfamily. Although the cytokine receptors do not possess a tyrosine kinase consensus sequence in the intracellular domain, rapid stimulation of a tyrosine kinase activity occurs after activation by the ligand. We and others have shown that Epo induces the tyrosine phosphorylation of its cognate receptor as well as phosphoryla...

The specialized plasma membrane structures termed caveolae and the caveolar-coat protein caveolin are highly expressed in insulin-sensitive cells such as adipocytes and muscle. Stimulation of 3T3-L1 adipocytes with insulin significantly increased the tyrosine phosphorylation of caveolin and a 29-kD caveolin-associated protein in caveolin-enriched Triton-insoluble complexes. Maximal phosphorylat...

Products of the ras gene family, termed p21ras, are GTP-binding proteins that have been implicated in signal transduction via receptors encoding tyrosine kinase domains. Recent findings have defined a superfamily of hemopoietin receptors that includes receptors for a number of interleukins and colony-stimulating factors. The intracellular portions of these receptors show only restricted homolog...

Tyrosine kinase inhibitors are molecules that block various intracellular signaling pathways. Trials with some tyrosine kinase inhibitors showed promising results in thyroid cancer. They are thought to owe their antitumor property mainly to their effect on vascular endothelial growth factor receptor which is important in angiogenesis. Axl is a receptor tyrosine kinase shown to be involved in pr...

Since in most tumors multiple signaling pathways are involved, many of the inhibitors in clinical development are designed to affect a wide range of targeted kinases. The most important tyrosine kinase families in the development of tyrosine kinase inhibitors are the ABL, SCR, platelet derived growth factor, vascular endothelial growth factor receptor and epidermal growth factor receptor famili...

The diarylurea is a scaffold of great importance in medicinal chemistry as it present numerous heterocyclic compounds with antithrombotic, antimalarial, antibacterial, and anti-inflammatory properties. Some diarylureas, serine-threonine kinase or tyrosine inhibitors, were recently reported literature. first to come into the market an anticancer agent was sorafenib, followed by some others. In t...

It was shown previously that OAT3 activity was differentially regulated by protein kinases including MAPK, PKA, and PKC. The present study investigated the short-term effect of tyrosine kinase and phosphatidylinositol 3-kinase (PI3K) on OAT3-mediated organic anion transport in S2 segments of renal proximal tubules. Genistein, a tyrosine kinase inhibitor, and wortmannin, a PI3K inhibitor, inhibi...

Protein tyrosine kinase activity was assayed in a variety of chicken tissues during embryonic development and in the adult. In some tissues protein tyrosine kinase activity decreased during embryonic development; however, in other tissues it remained high throughout development, it contrast to the level of protein tyrosine phosphorylation, which decreased during development. The highest levels ...

Abstract BACKGROUND Glioblastoma is associated with dismal outcomes a survival of 15-18 months. A major challenge in glioblastoma the inability to effectively target glioma stem cells (GSCs) that have capacity for self-renewal. GSCs are resistant radiation and traditional chemotherapy agents. Ibrutinib first-in-class, potent, small-molecule tyrosine kinase inhibitor Bruton’s Tyrosine Kinase (BT...