IGF1R
The pleiotropic actions of insulin are mediated by a single receptor tyrosine kinase (RTK class II, Insulin receptor family). A generally accepted paradigm is that insulin receptors, acting through insulin receptor substrates (insulin, and Insulin-like growth factors (IGF) I and II), stimulate the lipid kinase activity of phosphatidylinositol 3-kinase (PI3K)[1]. The rapid rise in Tris-phosphorylated inositol (PIP3) that ensues triggers a cascade of PIP3-dependent serine/threonine kinases. Among the latter, Akt and atypical protein kinase C isoforms are thought to be involved in insulin regulation of glucose transport and oxidation; glycogen, lipid, and protein synthesis; and modulation of gene expression. "Insulin insensitivity", or a decrease in insulin receptor signaling, leads to diabetes mellitus type 2 – the cells are unable to take up glucose, and the result is hyperglycemia (an increase in circulating glucose), and all the sequelae that result from diabetes.
[1] The Insulin Receptor and Its Cellular Targets. Y. Kido, J. Nakae, D. Accili. J. Clin.Endocrin. Met. 2001, 86, 972-979.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
2267 | GSK 1838705A | Potent IGF-IR and insulin receptor (IR) kinase inhibitor with additional affinity for ALK | €110.00 | |
3830 | GSK1904529A | Potent, selective and orally active inhibitor of the insulin-like growth factor-1 receptor (IGF-1R) | Inquire | |
2238 | NT 157 | Unique allosteric inhibitor of IGF1R signaling | €95.00 | |
1702 | OSI 906 | IGF1R tyrosine kinase inhibitor | €60.00 | |
3341 | PQ401 | Potent IGF1R tyrosine kinase inhibitor | €100.00 | |
3866 | TAE226 | Potent and ATP-competitive dual FAK and IGF-1R inhibitor | €110.00 | |
3973 | XL-228 | Multitargeted protein kinase inhibitor (IGF1R, Aurora,FGFR, ABL,ALK and SRC) | Inquire |