286
Views
28
CrossRef citations to date
0
Altmetric
Review

GSK3β: A master switch and a promising target

, , &
Pages 1443-1455 | Published online: 14 Oct 2008

Bibliography

  • Embi N, Rylatt DB, Cohen P. Glycogen synthase kinase-3 from rabbit skeletal muscle. Separation from cyclic-AMP-dependent protein kinase and phosphorylase kinase. Eur J Biochem 1980;107:519-27
  • Frame S, Cohen P, Biondi RM. A common phosphate binding site explains the unique substrate specificity of GSK3 and its inactivation by phosphorylation. Mol Cell 2001;7:1321-7
  • Berman HM, Westbrook J, Feng Z, et al. The Protein Data Bank. Nucleic Acids Res 2000;28:235-42
  • Bax B, Carter PS, Lewis C, et al. The structure of phosphorylated GSK-3β complexed with a peptide, FRATtide, that inhibits β-catenin phosphorylation. Structure 2001;9:1143-52
  • Dajani R, Fraser E, Roe SM, et al. Crystal structure of glycogen synthase kinase 3β: structural basis for phosphate-primed substrate specificity and autoinhibition. Cell 2001;105:721-32
  • ter Haar E, Coll JT, Austen DA, et al. Structure of GSK3β reveals a primed phosphorylation mechanism. Nat Struct Biol 2001;8:593-6
  • Dajani R, Fraser E, Roe SM, et al. Structural basis for recruitment of glycogen synthase kinase 3β to the axin-APC scaffold complex. EMBO J 2003;22:494-501
  • Bertrand JA, Thieffine S, Vulpetti A, et al. Structural characterization of the GSK-3β active site using selective and non-selective ATP-mimetic inhibitors. J Mol Biol 2003;333:393-407
  • Bhat R, Xue Y, Berg S, et al. Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. J Biol Chem 2003;278:45937-45
  • Meijer L, Skaltsounis AL, Magiatis P, et al. GSK-3-selective inhibitors derived from Tyrian purple indirubins. Chem Biol 2003;10:1255-66
  • Shin D, Lee SC, Heo YS, et al. Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3β. Bioorg Med Chem Lett 2007;17:5686-9
  • Gadakar PK, Phukan S, Dattatreya P, Balaji VN. Pose prediction accuracy in docking studies and enrichment of actives in the active site of GSK-3β. J Chem Inf Model 2007;47:1446-59
  • McManus EJ, Sakamoto K, Armit LJ, et al. Role that phosphorylation of GSK3 plays in insulin and Wnt signalling defined by knockin analysis. EMBO J 2005;24:1571-83
  • Bhat RV, Budd SL. GSK3β signalling: casting a wide net in Alzheimer's disease. Neurosignals 2002;11:251-61
  • Kwok JB, Hallupp M, Loy CT, et al. GSK3B polymorphisms alter transcription and splicing in Parkinson's disease. Ann Neurol 2005;58:829-39
  • Michelon L, Meira-Lima I, Cordeiro Q, et al. Association study of the INPP1, 5HTT, BDNF, AP-2β and GSK-3β GENE variants and restrospectively scored response to lithium prophylaxis in bipolar disorder. Neurosci Lett 2006;403:288-93
  • Ring DB, Johnson KW, Henriksen EJ, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes 2003;52:588-95
  • Cohen P, Alessi DR, Cross DA. PDK1, one of the missing links in insulin signal transduction? FEBS Lett 1997;410:3-10
  • Cline GW, Johnson K, Regittnig W, et al. Effects of a novel glycogen synthase kinase-3 inhibitor on insulin-stimulated glucose metabolism in Zucker diabetic fatty (fa/fa) rats. Diabetes 2002;51:2903-10
  • Qu ZS, Tian Q, Zhou XW, et al. Mechanism of tau hyperphosphorylation in brain cortex of diabetic rats and effect of LiCl. Zhongguo Yi Xue Ke Xue Yuan Xue Bao 2006;28:244-8
  • Cedazo-Minguez A, Popescu BO, Blanco-Millan JM, et al. Apolipoprotein E and β-amyloid (1-42) regulation of glycogen synthase kinase-3β. J Neurochem 2003;87:1152-64
  • Gum RJ, Gaede LL, Koterski SL, et al. Reduction of protein tyrosine phosphatase 1B increases insulin-dependent signaling in ob/ob mice. Diabetes 2003;52:21-8
  • Ross SE, Erickson RL, Hemati N, MacDougald OA. Glycogen synthase kinase 3 is an insulin-regulated C/EBPα kinase. Mol Cell Biol 1999;19:8433-41
  • De Sarno P, Li X, Jope RS. Regulation of Akt and glycogen synthase kinase-3β phosphorylation by sodium valproate and lithium. Neuropharmacology 2002;43:1158-64
  • Jope RS, Roh MS. Glycogen synthase kinase-3 (GSK3) in psychiatric diseases and therapeutic interventions. Curr Drug Targets 2006;7:1421-34
  • Hong M, Lee VM. Insulin and insulin-like growth factor-1 regulate tau phosphorylation in cultured human neurons. J Biol Chem 1997;272:19547-53
  • Takashima A. GSK-3 is essential in the pathogenesis of Alzheimer's disease. J Alzheimers Dis 2006;9(3 Suppl):309-17
  • Huang HC, Klein PS. Multiple roles for glycogen synthase kinase-3 as a drug target in Alzheimer's disease. Curr Drug Targets 2006;7:1389-97
  • Engel T, Hernandez F, Avila J, Lucas JJ. Full reversal of Alzheimer's disease-like phenotype in a mouse model with conditional overexpression of glycogen synthase kinase-3. J Neurosci 2006;26:5083-90
  • Ryder J, Su Y, Liu F, et al. Divergent roles of GSK3 and CDK5 in APP processing. Biochem Biophys Res Commun 2003;312:922-9
  • Ryan KA, Pimplikar SW. Activation of GSK-3 and phosphorylation of CRMP2 in transgenic mice expressing APP intracellular domain. J Cell Biol 2005;171:327-35
  • Chen G, Huang LD, Jiang YM, Manji HK. The mood-stabilizing agent valproate inhibits the activity of glycogen synthase kinase-3. J Neurochem 1999;72:1327-30
  • Klein PS, Melton DA. A molecular mechanism for the effect of lithium on development. Proc Natl Acad Sci USA 1996;93:8455-9
  • Ryves WJ, Dajani R, Pearl L, Harwood AJ. Glycogen synthase kinase-3 inhibition by lithium and beryllium suggests the presence of two magnesium binding sites. Biochem Biophys Res Commun 2002;290:967-72
  • Hsiung SC, Adlersberg M, Arango V, et al. Attenuated 5-HT1A receptor signaling in brains of suicide victims: involvement of adenylyl cyclase, phosphatidylinositol 3-kinase, Akt and mitogen-activated protein kinase. J Neurochem 2003;87:182-94
  • Mai L, Jope RS, Li X. BDNF-mediated signal transduction is modulated by GSK3β and mood stabilizing agents. J Neurochem 2002;82:75-83
  • Emamian ES, Hall D, Birnbaum MJ, et al. Convergent evidence for impaired AKT1-GSK3β signaling in schizophrenia. Nat Genet 2004;36:131-7
  • Smith E, Frenkel B. Glucocorticoids inhibit the transcriptional activity of LEF/TCF in differentiating osteoblasts in a glycogen synthase kinase-3β-dependent and -independent manner. J Biol Chem 2005;280:2388-94
  • Robertson LA, Kim AJ, Werstuck GH. Mechanisms linking diabetes mellitus to the development of atherosclerosis: a role for endoplasmic reticulum stress and glycogen synthase kinase-3. Can J Physiol Pharmacol 2006;84:39-48
  • Liang J, Slingerland JM. Multiple roles of the PI3K/PKB (Akt) pathway in cell cycle progression. Cell Cycle 2003;2:339-45
  • M GA, Uddin S, Mahmud D, et al. Regulation of myeloma cell growth through Akt/Gsk3/forkhead signaling pathway. Biochem Biophys Res Commun 2002;297:760-4
  • Viatour P, Dejardin E, Warnier M, et al. GSK3-mediated BCL-3 phosphorylation modulates its degradation and its oncogenicity. Mol Cell 2004;16:35-45
  • Gomez-Ramos A, Dominguez J, Zafra D, et al. Sodium tungstate decreases the phosphorylation of tau through GSK3 inactivation. J Neurosci Res 2006;83:264-73
  • Inoki K, Ouyang H, Zhu T, et al. TSC2 integrates Wnt and energy signals via a coordinated phosphorylation by AMPK and GSK3 to regulate cell growth. Cell 2006;126:955-68
  • Sagae S, Kobayashi K, Nishioka Y, et al. Mutational analysis of β-catenin gene in Japanese ovarian carcinomas: frequent mutations in endometrioid carcinomas. Jpn J Cancer Res 1999;90:510-5
  • Lenferink AE, Busse D, Flanagan WM, et al. ErbB2/neu kinase modulates cellular p27(Kip1) and cyclin D1 through multiple signaling pathways. Cancer Res 2001;61:6583-91
  • Shao J, Jung C, Liu C, Sheng H. Prostaglandin E2 Stimulates the β-catenin/T cell factor-dependent transcription in colon cancer. J Biol Chem 2005;280:26565-72
  • Ohira T, Gemmill RM, Ferguson K, et al. WNT7a induces E-cadherin in lung cancer cells. Proc Natl Acad Sci USA 2003;100:10429-34
  • Rosano L, Spinella F, Di Castro V, et al. Endothelin-1 promotes epithelial-to-mesenchymal transition in human ovarian cancer cells. Cancer Res 2005;65:11649-57
  • Satyamoorthy K, Li G, Vaidya B, et al. Insulin-like growth factor-1 induces survival and growth of biologically early melanoma cells through both the mitogen-activated protein kinase and beta-catenin pathways. Cancer Res 2001;61:7318-24
  • Boyle WJ, Smeal T, Defize LH, et al. Activation of protein kinase C decreases phosphorylation of c-Jun at sites that negatively regulate its DNA-binding activity. Cell 1991;64:573-84
  • McKenzie G, Ward G, Stallwood Y, et al. Cellular Notch responsiveness is defined by phosphoinositide 3-kinase-dependent signals. BMC Cell Biol 2006;7:10. Published online 28 February 2006, doi:10.1186/1471-2121-7-10
  • Buss H, Dorrie A, Schmitz ML, et al. Phosphorylation of serine 468 by GSK-3β negatively regulates basal p65 NF-κB activity. J Biol Chem 2004;279:49571-4
  • Nikolakaki E, Coffer PJ, Hemelsoet R, et al. Glycogen synthase kinase 3 phosphorylates Jun family members in vitro and negatively regulates their transactivating potential in intact cells. Oncogene 1993;8:833-40
  • Shao D, Lazar MA. Modulating nuclear receptor function: may the phos be with you. J Clin Invest 1999;103:1617-8
  • Sears R, Nuckolls F, Haura E, et al. Multiple Ras-dependent phosphorylation pathways regulate Myc protein stability. Genes Dev 2000;14:2501-14
  • Pulverer BJ, Fisher C, Vousden K, et al. Site-specific modulation of c-Myc cotransformation by residues phosphorylated in vivo. Oncogene 1994;9:59-70
  • Turenne GA, Price BD. Glycogen synthase kinase3 beta phosphorylates serine 33 of p53 and activates p53's transcriptional activity. BMC Cell Biol 2001;2:12. Published online 16 July 2001, doi:10.1186/1471-2121-2-12
  • Tang QQ, Gronborg M, Huang H, et al. Sequential phosphorylation of CCAAT enhancer-binding protein β by MAPK and glycogen synthase kinase 3β is required for adipogenesis. Proc Natl Acad Sci USA 2005;102:9766-71
  • Sodhi A, Montaner S, Miyazaki H, Gutkind JS. MAPK and Akt act cooperatively but independently on hypoxia inducible factor-1α in rasV12 upregulation of VEGF. Biochem Biophys Res Commun 2001;287:292-300
  • Takeda K, Takemoto C, Kobayashi I, et al. Ser298 of MITF, a mutation site in Waardenburg syndrome type 2, is a phosphorylation site with functional significance. Hum Mol Genet 2000;9:125-32
  • Fiol CJ, Williams JS, Chou CH, et al. A secondary phosphorylation of CREB341 at Ser129 is required for the cAMP-mediated control of gene expression. A role for glycogen synthase kinase-3 in the control of gene expression. J Biol Chem 1994;269:32187-93
  • Beals CR, Sheridan CM, Turck CW, et al. Nuclear export of NF-ATc enhanced by glycogen synthase kinase-3. Science 1997;275:1930-4
  • Ginger RS, Dalton EC, Ryves WJ, et al. Glycogen synthase kinase-3 enhances nuclear export of a Dictyostelium STAT protein. EMBO J 2000;19:5483-91
  • Martinek S, Inonog S, Manoukian AS, Young MW. A role for the segment polarity gene shaggy/GSK-3 in the Drosophila circadian clock. Cell 2001;105:769-79
  • Yamamoto H, Kishida S, Kishida M, et al. Phosphorylation of axin, a Wnt signal negative regulator, by glycogen synthase kinase-3β regulates its stability. J Biol Chem 1999;274:10681-4
  • Yost C, Torres M, Miller JR, et al. The axis-inducing activity, stability, and subcellular distribution of β-catenin is regulated in Xenopus embryos by glycogen synthase kinase 3. Genes Dev 1996;10:1443-54
  • Rubinfeld B, Albert I, Porfiri E, et al. Binding of GSK3β to the APC-β-catenin complex and regulation of complex assembly. Science 1996;272:1023-6
  • Price MA, Kalderon D. Proteolysis of the Hedgehog signaling effector Cubitus interruptus requires phosphorylation by glycogen synthase kinase 3 and casein kinase 1. Cell 2002;108:823-35
  • Goold RG, Gordon-Weeks PR. The MAP kinase pathway is upstream of the activation of GSK3β that enables it to phosphorylate MAP1B and contributes to the stimulation of axon growth. Mol Cell Neurosci 2005;28:524-34
  • Hanger DP, Hughes K, Woodgett JR, et al. Glycogen synthase kinase-3 induces Alzheimer's disease-like phosphorylation of tau: generation of paired helical filament epitopes and neuronal localisation of the kinase. Neurosci Lett 1992;147:58-62
  • Mazanetz MP, Fischer PM. Untangling tau hyperphosphorylation in drug design for neurodegenerative diseases. Nat Rev Drug Discov 2007;6:464-79
  • Sanchez C, Perez M, Avila J. GSK3β-mediated phosphorylation of the microtubule-associated protein 2C (MAP2C) prevents microtubule bundling. Eur J Cell Biol 2000;79:252-60
  • Krymsky MA, Kudryashov DS, Shirinsky VP, et al. Phosphorylation of kinase-related protein (telokin) in tonic and phasic smooth muscles. J Muscle Res Cell Motil 2001;22:425-37
  • Seidenfaden R, Krauter A, Schertzinger F, et al. Polysialic acid directs tumor cell growth by controlling heterophilic neural cell adhesion molecule interactions. Mol Cell Biol 2003;23:5908-18
  • Diehl JA, Cheng M, Roussel MF, Sherr CJ. Glycogen synthase kinase-3β regulates cyclin D1 proteolysis and subcellular localization. Genes Dev 1998;12:3499-511
  • Welcker M, Singer J, Loeb KR, et al. Multisite phosphorylation by Cdk2 and GSK3 controls cyclin E degradation. Mol Cell 2003;12:381-92
  • Hong YR, Chen CH, Chang JH, et al. Cloning and characterization of a novel human ninein protein that interacts with the glycogen synthase kinase 3β. Biochim Biophys Acta 2000;1492:513-6
  • Hoshi M, Takashima A, Noguchi K, et al. Regulation of mitochondrial pyruvate dehydrogenase activity by tau protein kinase I/glycogen synthase kinase 3β in brain. Proc Natl Acad Sci USA 1996;93:2719-23
  • Li Y, Bharti A, Chen D, et al. Interaction of glycogen synthase kinase 3β with the DF3/MUC1 carcinoma-associated antigen and β-catenin. Mol Cell Biol 1998;18:7216-24
  • Dent P, Lavoinne A, Nakielny S, et al. The molecular mechanism by which insulin stimulates glycogen synthesis in mammalian skeletal muscle. Nature 1990;348:302-8
  • Benjamin WB, Pentyala SN, Woodgett JR, et al. ATP citrate-lyase and glycogen synthase kinase-3β in 3T3-L1 cells during differentiation into adipocytes. Biochem J 1994;300:477-82
  • Welsh GI, Proud CG. Glycogen synthase kinase-3 is rapidly inactivated in response to insulin and phosphorylates eukaryotic initiation factor eIF-2B. Biochem J 1993;294:625-9
  • Ramakrishna S, Benjamin WB. Phosphorylation of ATP-citrate lyase by a cyclic AMP-independent protein kinase from rat liver. FEBS Lett 1981;124:140-4
  • Prager K, Wang-Eckhardt L, Fluhrer R, et al. A structural switch of presenilin 1 by glycogen synthase kinase 3β-mediated phosphorylation regulates the interaction with β-catenin and its nuclear signaling. J Biol Chem 2007;282:14083-93
  • Ramakrishna S, Benjamin WB. Cyclic nucleotide-independent protein kinase from rat liver. Purification and characterization of a multifunctional protein kinase. J Biol Chem 1985;260:12280-6
  • Ramakrishna S, Benjamin WB. Phosphorylation of different sites of acetyl CoA carboxylase by ATP-citrate lyase kinase and cyclic AMP-dependent protein kinase. Biochem Biophys Res Commun 1983;117:435-43
  • Martin CP, Vazquez J, Avila J, Moreno FJ. P24, a glycogen synthase kinase 3 (GSK 3) inhibitor. Biochim Biophys Acta 2002;1586:113-22
  • Park IK, Roach P, Bondor J, et al. Molecular mechanism of the synergistic phosphorylation of phosphatase inhibitor-2. Cloning, expression, and site-directed mutagenesis of inhibitor-2. J Biol Chem 1994;269:944-54
  • Yu JS, Yang SD. Protein kinase FA/glycogen synthase kinase-3 predominantly phosphorylates the in vivo site Thr97-Pro in brain myelin basic protein: evidence for Thr-Pro and Ser-Arg-X-X-Ser as consensus sequence motifs. J Neurochem 1994;62:1596-603
  • Morfini G, Szebenyi G, Elluru R, et al. Glycogen synthase kinase 3 phosphorylates kinesin light chains and negatively regulates kinesin-based motility. EMBO J 2002;21:281-93
  • Doble BW, Woodgett JR. GSK-3: tricks of the trade for a multi-tasking kinase. J Cell Sci 2003;116:1175-86
  • Cohen P. The role of protein phosphorylation in human health and disease. The Sir Hans Krebs Medal Lecture. Eur J Biochem 2001;268:5001-10
  • Kim WY, Zhou FQ, Zhou J, et al. Essential roles for GSK-3s and GSK-3-primed substrates in neurotrophin-induced and hippocampal axon growth. Neuron 2006;52:981-96
  • Fang CH, Li B, James JH, et al. GSK-3β activity is increased in skeletal muscle after burn injury in rats. Am J Physiol Regul Integr Comp Physiol 2007;293:R1545-51

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.