GSK-3
GSK-3, a key component in glycogen metabolism, has been heavily implicated in the incidence and progression of a number of diseases including diabetes, cancer and AD. Its most well-known function is constitutive phosphorylation of glycogen synthase. Conversely, GSK-3 inhibition prevents Tau hyperphosphorylation and serves as a protectant against neuronal apoptosis, as well as blocking the accumulation and toxicity of Ab/tau. Unlike most other kinases, GSK-3 is constitutively active, and its effects are regulated primarily through inhibition of its activity. Increased expression and activity of GSK-3 have been implicated both in Type II diabetes and AD, whereas, decreases in its constitutive cellular function are closely linked to various forms of cancer. The therapeutic potential of GSK-3 inhibitors has become a major area of pharmaceutical interest, and the development of GSK-3 targeted therapeutics hold excellent opportunities for the treatment of GSK-3-associated disease states.
Inhibition of GSK-3b Inhibition of GSK-3b by Ro31-8220. GSK-3b, active (Millipore cat. no. 14-306) was incubated with various concentrations of Ro31-8220 and assayed by measuring incorporation of radioactivity from g3 3p-ATP into PhosphoGlycogen Synthase Peptide-2 (Millipore cat.no. 12-241). IC50s were determined at both 10 and 100 mM ATP and were 16 nM and 79 nM respectively. |
References
- Yuan Z, Agarwal-Mawal A, Paudel HK. 14-3-3 binds to and mediates phosphorylation of microtubule-associated tau protein by Ser9-phosphorylated glycogen synthase kinase 3beta in the brain. JBC. Jun 2004; 279(25): 26105–14.
- Schubert M, Gautam D, Surjo D, Ueki K, Baudler S, Schubert D, Kondo T, Alber J, Galldiks N, Kustermann E, Arndt S, Jacobs AH, Krone W, Kahn CR, Bruning JC. Role for neuronal insulin resistance in neurodegenerative diseases. PNAS. Mar 2004;101(9): 3100-5.
- Wang X, Chen L, Maures TJ, Herrington J, Carter-Su C. SH2-B is a positive regulator of nerve growth factor-mediated activation of the Akt/Forkhead pathway in PC12 cells. JBC. Jan 2004; 279(1): 133-41.
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