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PDBsum entry 1q5k
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protein ligands Protein-protein interface(s) links
Transferase PDB id
1q5k

 

 

 

 

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JSmol PyMol  
Contents
Protein chain
345 a.a. *
Ligands
TMU ×2
Waters ×373
* Residue conservation analysis
PDB id:
1q5k
Name: Transferase
Title: Crystal structure of glycogen synthase kinase 3 in complexed with inhibitor
Structure: Glycogen synthase kinase-3 beta. Chain: a, b. Synonym: gsk-3 beta. Engineered: yes
Source: Homo sapiens. Human. Organism_taxid: 9606. Gene: gsk3b. Expressed in: trichoplusia ni. Expression_system_taxid: 7111. Expression_system_cell: high five cells.
Biol. unit: Dimer (from PQS)
Resolution:
1.94Å     R-factor:   0.222     R-free:   0.242
Authors: R.Bhat,Y.Xue,S.Berg,S.Hellberg,M.Ormo,Y.Nilsson,A.C.Radesater, E.Jerning,P.O.Markgren,T.Borgegard,M.Nylof,A.Gimenez-Cassina, F.Hernandez,J.J.Lucas,J.Diaz-Mido,J.Avila
Key ref:
R.Bhat et al. (2003). Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. J Biol Chem, 278, 45937-45945. PubMed id: 12928438 DOI: 10.1074/jbc.M306268200
Date:
08-Aug-03     Release date:   10-Aug-04    
PROCHECK
Go to PROCHECK summary
 Headers
 References

Protein chains
Pfam   ArchSchema ?
P49841  (GSK3B_HUMAN) -  Glycogen synthase kinase-3 beta from Homo sapiens
Seq:
Struc: 		420 a.a.
345 a.a.
Key:    PfamA domain  Secondary structure  CATH domain

 Enzyme reactions 
   Enzyme class 1: E.C.2.7.11.1  - non-specific serine/threonine protein kinase.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
      Reaction:
1. L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H+
2. L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H+
L-seryl-[protein]
 + ATP
 = O-phospho-L-seryl-[protein]
Bound ligand (Het Group name = TMU)
matches with 41.18% similarity 		+ ADP
 + H(+)
L-threonyl-[protein]
 + ATP
 = O-phospho-L-threonyl-[protein]
Bound ligand (Het Group name = TMU)
matches with 41.18% similarity 		+ ADP
 + H(+)
   Enzyme class 2: E.C.2.7.11.26  - [tau protein] kinase.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
      Reaction:
1. L-seryl-[tau protein] + ATP = O-phospho-L-seryl-[tau protein] + ADP + H+
2. L-threonyl-[tau protein] + ATP = O-phospho-L-threonyl-[tau protein] + ADP + H+
L-seryl-[tau protein]
 + ATP
 = O-phospho-L-seryl-[tau protein]
Bound ligand (Het Group name = TMU)
matches with 41.18% similarity 		+ ADP
 + H(+)
L-threonyl-[tau protein]
 + ATP
 = O-phospho-L-threonyl-[tau protein]
Bound ligand (Het Group name = TMU)
matches with 41.18% similarity 		+ ADP
 + H(+)
Note, where more than one E.C. class is given (as above), each may correspond to a different protein domain or, in the case of polyprotein precursors, to a different mature protein.
Molecule diagrams generated from .mol files obtained from the KEGG ftp site

 

 
    reference    
 
 
DOI no: 10.1074/jbc.M306268200 J Biol Chem 278:45937-45945 (2003)
PubMed id: 12928438  
 
 
Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418.
R.Bhat, Y.Xue, S.Berg, S.Hellberg, M.Ormö, Y.Nilsson, A.C.Radesäter, E.Jerning, P.O.Markgren, T.Borgegård, M.Nylöf, A.Giménez-Cassina, F.Hernández, J.J.Lucas, J.Díaz-Nido, J.Avila.
 
  ABSTRACT  
 
Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in pathological conditions such as diabetes and Alzheimer's disease. We report the characterization of a GSK3 inhibitor, AR-A014418, which inhibits GSK3 (IC50 = 104 +/- 27 nM), in an ATP-competitive manner (Ki = 38 nM). AR-A014418 does not significantly inhibit cdk2 or cdk5 (IC50 > 100 microM) or 26 other kinases demonstrating high specificity for GSK3. We report the co-crystallization of AR-A014418 with the GSK3beta protein and provide a description of the interactions within the ATP pocket, as well as an understanding of the structural basis for the selectivity of AR-A014418. AR-A014418 inhibits tau phosphorylation at a GSK3-specific site (Ser-396) in cells stably expressing human four-repeat tau protein. AR-A014418 protects N2A neuroblastoma cells against cell death mediated by inhibition of the phosphatidylinositol 3-kinase/protein kinase B survival pathway. Furthermore, AR-A014418 inhibits neurodegeneration mediated by beta-amyloid peptide in hippocampal slices. AR-A014418 may thus have important applications as a tool to elucidate the role of GSK3 in cellular signaling and possibly in Alzheimer's disease. AR-A014418 is the first compound of a family of specific inhibitors of GSK3 that does not significantly inhibit closely related kinases such as cdk2 or cdk5.
 
  Selected figure(s)  
 
Figure 4.
FIG. 4. Binding of AR-A014418 to GSK3 Left, surface representation of the inhibitor binding pocket. Right, interactions between the ligand and the protein. For clarity only residues in the linker/hinge region and those involved in the important ion-pair interaction (Lys-85, Glu-97, and Asp-200) are shown. Hydrogen bonds between the inhibitor and the protein molecule are shown as yellow lines. Single-letter codes are used for amino acids. 		Figure 7.
FIG. 7. Surface representation of the ATP pocket of GSK3 -AR-A014418 (in cyan), and that of cdk2-ATP (magenta).
 
  The above figures are reprinted by permission from the ASBMB: J Biol Chem (2003, 278, 45937-45945) copyright 2003.  
  Figures were selected by an automated process.  

Literature references that cite this PDB file's key reference

  PubMed id Reference
21210815 A.Valerio, P.Bertolotti, A.Delbarba, C.Perego, M.Dossena, M.Ragni, P.Spano, M.O.Carruba, M.G.De Simoni, and E.Nisoli (2011).
Glycogen synthase kinase-3 inhibition reduces ischemic cerebral damage, restores impaired mitochondrial biogenesis and prevents ROS production.
  J Neurochem, 116, 1148-1159.  
20821241 G.E.Atilla-Gokcumen, L.Di Costanzo, and E.Meggers (2011).
Structure of anticancer ruthenium half-sandwich complex bound to glycogen synthase kinase 3β.
  J Biol Inorg Chem, 16, 45-50.
PDB code: 3m1s
21443429 J.L.Johnson, S.G.Rupasinghe, F.Stefani, M.A.Schuler, and E.Gonzalez de Mejia (2011).
Citrus flavonoids luteolin, apigenin, and quercetin inhibit glycogen synthase kinase-3β enzymatic activity by lowering the interaction energy within the binding cavity.
  J Med Food, 14, 325-333.  
21212533 K.Saeki, M.Machida, Y.Kinoshita, R.Takasawa, and S.Tanuma (2011).
Glycogen synthase kinase-3β2 has lower phosphorylation activity to tau than glycogen synthase kinase-3β1.
  Biol Pharm Bull, 34, 146-149.  
  21469159 S.Y.Lu, Y.J.Jiang, J.Lv, J.W.Zou, and T.X.Wu (2011).
Role of bridging water molecules in GSK3β-inhibitor complexes: insights from QM/MM, MD, and molecular docking studies.
  J Comput Chem, 32, 1907-1918.  
21588684 A.J.Lough, J.W.Hicks, J.F.Valliant, A.A.Wilson, and N.Vasdev (2010).
N-(4-Meth-oxy-phen-yl)-N'-(5-nitro-1,3-thia-zol-2-yl)urea.
  Acta Crystallogr Sect E Struct Rep Online, 66, o2339.  
20842339 A.Schneider, P.Falkai, and A.Papassotiropoulos (2010).
[Molecular principles of tau-induced toxicity: new experimental therapy strategies for treatment of Alzheimer's disease].
  Nervenarzt, 81, 1289.  
20526333 E.L.Clayton, N.Sue, K.J.Smillie, T.O'Leary, N.Bache, G.Cheung, A.R.Cole, D.J.Wyllie, C.Sutherland, P.J.Robinson, and M.A.Cousin (2010).
Dynamin I phosphorylation by GSK3 controls activity-dependent bulk endocytosis of synaptic vesicles.
  Nat Neurosci, 13, 845-851.  
20559321 I.Lassot, I.Robbins, M.Kristiansen, R.Rahmeh, F.Jaudon, M.M.Magiera, S.Mora, L.Vanhille, A.Lipkin, B.Pettmann, J.Ham, and S.Desagher (2010).
Trim17, a novel E3 ubiquitin-ligase, initiates neuronal apoptosis.
  Cell Death Differ, 17, 1928-1941.  
20420491 J.Avila, F.Wandosell, and F.Hernández (2010).
Role of glycogen synthase kinase-3 in Alzheimer's disease pathogenesis and glycogen synthase kinase-3 inhibitors.
  Expert Rev Neurother, 10, 703-710.  
  20473358 L.B.Bennett, K.H.Taylor, G.L.Arthur, F.B.Rahmatpanah, S.I.Hooshmand, and C.W.Caldwell (2010).
Epigenetic regulation of WNT signaling in chronic lymphocytic leukemia.
  Epigenomics, 2, 53-70.  
20101221 L.Santo, S.Vallet, T.Hideshima, D.Cirstea, H.Ikeda, S.Pozzi, K.Patel, Y.Okawa, G.Gorgun, G.Perrone, E.Calabrese, M.Yule, M.Squires, M.Ladetto, M.Boccadoro, P.G.Richardson, N.C.Munshi, K.C.Anderson, and N.Raje (2010).
AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition.
  Oncogene, 29, 2325-2336.  
20401887 M.Bartolini, and V.Andrisano (2010).
Strategies for the inhibition of protein aggregation in human diseases.
  Chembiochem, 11, 1018-1035.  
20809259 M.V.Hoang, L.E.Smith, and D.R.Senger (2010).
Moderate GSK-3β inhibition improves neovascular architecture, reduces vascular leakage, and reduces retinal hypoxia in a model of ischemic retinopathy.
  Angiogenesis, 13, 269-277.  
  20637111 P.Mishra, S.Senthivinayagam, A.Rana, and B.Rana (2010).
Glycogen Synthase Kinase-3beta regulates Snail and beta-catenin during gastrin-induced migration of gastric cancer cells.
  J Mol Signal, 5, 9.  
19855063 R.Wong, A.M.Aponte, C.Steenbergen, and E.Murphy (2010).
Cardioprotection leads to novel changes in the mitochondrial proteome.
  Am J Physiol Heart Circ Physiol, 298, H75-H91.  
20331603 S.Phukan, V.S.Babu, A.Kannoji, R.Hariharan, and V.N.Balaji (2010).
GSK3beta: role in therapeutic landscape and development of modulators.
  Br J Pharmacol, 160, 1.  
20962236 S.W.Perry, J.Barbieri, N.Tong, O.Polesskaya, S.Pudasaini, A.Stout, R.Lu, M.Kiebala, S.B.Maggirwar, and H.A.Gelbard (2010).
Human immunodeficiency virus-1 Tat activates calpain proteases via the ryanodine receptor to enhance surface dopamine transporter levels and increase transporter-specific uptake and Vmax.
  J Neurosci, 30, 14153-14164.  
20300959 T.Takadera, Y.Nakajima, and Y.Kanai (2010).
Colchicine-induced apoptosis was prevented by glycogen synthase kinase-3 inhibitors in PC12 cells.
  Cell Mol Neurobiol, 30, 863-868.  
20167573 X.Ma, B.Hibbert, B.Dhaliwal, T.Seibert, Y.X.Chen, X.Zhao, and E.R.O'Brien (2010).
Delayed re-endothelialization with rapamycin-coated stents is rescued by the addition of a glycogen synthase kinase-3beta inhibitor.
  Cardiovasc Res, 86, 338-345.  
20541704 Z.Wang, M.Iwasaki, F.Ficara, C.Lin, C.Matheny, S.H.Wong, K.S.Smith, and M.L.Cleary (2010).
GSK-3 promotes conditional association of CREB and its coactivators with MEIS1 to facilitate HOX-mediated transcription and oncogenesis.
  Cancer Cell, 17, 597-608.  
19549598 B.De Rybel, D.Audenaert, G.Vert, W.Rozhon, J.Mayerhofer, F.Peelman, S.Coutuer, T.Denayer, L.Jansen, L.Nguyen, I.Vanhoutte, G.T.Beemster, K.Vleminckx, C.Jonak, J.Chory, D.Inzé, E.Russinova, and T.Beeckman (2009).
Chemical inhibition of a subset of Arabidopsis thaliana GSK3-like kinases activates brassinosteroid signaling.
  Chem Biol, 16, 594-604.  
19363289 D.Paquet, R.Bhat, A.Sydow, E.M.Mandelkow, S.Berg, S.Hellberg, J.Fälting, M.Distel, R.W.Köster, B.Schmid, and C.Haass (2009).
A zebrafish model of tauopathy allows in vivo imaging of neuronal cell death and drug evaluation.
  J Clin Invest, 119, 1382-1395.  
19478088 E.E.Congdon, Y.H.Figueroa, L.Wang, G.Toneva, E.Chang, J.Kuret, C.Conrad, and K.E.Duff (2009).
Inhibition of tau polymerization with a cyanine dye in two distinct model systems.
  J Biol Chem, 284, 20830-20839.  
19366350 G.V.Rayasam, V.K.Tulasi, R.Sodhi, J.A.Davis, and A.Ray (2009).
Glycogen synthase kinase 3: more than a namesake.
  Br J Pharmacol, 156, 885-898.  
19338355 I.N.Gaisina, F.Gallier, A.V.Ougolkov, K.H.Kim, T.Kurome, S.Guo, D.Holzle, D.N.Luchini, S.Y.Blond, D.D.Billadeau, and A.P.Kozikowski (2009).
From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.
  J Med Chem, 52, 1853-1863.  
19440740 K.H.Kim, I.Gaisina, F.Gallier, D.Holzle, S.Y.Blond, A.Mesecar, and A.P.Kozikowski (2009).
Use of molecular modeling, docking, and 3D-QSAR studies for the determination of the binding mode of benzofuran-3-yl-(indol-3-yl)maleimides as GSK-3beta inhibitors.
  J Mol Model, 15, 1463-1479.  
19208634 K.Ning, L.C.Miller, H.A.Laidlaw, K.R.Watterson, J.Gallagher, C.Sutherland, and M.L.Ashford (2009).
Leptin-dependent phosphorylation of PTEN mediates actin restructuring and activation of ATP-sensitive K+ channels.
  J Biol Chem, 284, 9331-9340.  
19475596 S.Kruggel, and T.Lemcke (2009).
Generation and evaluation of a homology model of PfGSK-3.
  Arch Pharm (Weinheim), 342, 327-332.  
19405981 S.Mamaghani, S.Patel, and D.W.Hedley (2009).
Glycogen synthase kinase-3 inhibition disrupts nuclear factor-kappaB activity in pancreatic cancer, but fails to sensitize to gemcitabine chemotherapy.
  BMC Cancer, 9, 132.  
19688630 T.B.Nguyen, G.R.Lucero, G.Chana, B.J.Hult, E.T.Tatro, E.Masliah, I.Grant, C.L.Achim, and I.P.Everall (2009).
Glycogen synthase kinase-3beta (GSK-3beta) inhibitors AR-A014418 and B6B3O prevent human immunodeficiency virus-mediated neurotoxicity in primary human neurons.
  J Neurovirol, 15, 434-438.  
19920820 V.Bilim, A.Ougolkov, K.Yuuki, S.Naito, H.Kawazoe, A.Muto, M.Oya, D.Billadeau, T.Motoyama, and Y.Tomita (2009).
Glycogen synthase kinase-3: a new therapeutic target in renal cell carcinoma.
  Br J Cancer, 101, 2005-2014.  
18952114 W.W.Min, C.J.Yuskaitis, Q.Yan, C.Sikorski, S.Chen, R.S.Jope, and R.P.Bauchwitz (2009).
Elevated glycogen synthase kinase-3 activity in Fragile X mice: key metabolic regulator with evidence for treatment potential.
  Neuropharmacology, 56, 463-472.  
18851699 A.Kannoji, S.Phukan, V.Sudher Babu, and V.N.Balaji (2008).
GSK3beta: a master switch and a promising target.
  Expert Opin Ther Targets, 12, 1443-1455.  
17893926 D.Simón, M.J.Benitez, A.Gimenez-Cassina, J.J.Garrido, R.V.Bhat, J.Díaz-Nido, and F.Wandosell (2008).
Pharmacological inhibition of GSK-3 is not strictly correlated with a decrease in tyrosine phosphorylation of residues 216/279.
  J Neurosci Res, 86, 668-674.  
19035373 G.E.Atilla-Gokcumen, N.Pagano, C.Streu, J.Maksimoska, P.Filippakopoulos, S.Knapp, and E.Meggers (2008).
Extremely tight binding of a ruthenium complex to glycogen synthase kinase 3.
  Chembiochem, 9, 2933-2936.
PDB code: 2jld
18189317 J.M.Boggs, W.Gao, and Y.Hirahara (2008).
Signal transduction pathways involved in interaction of galactosylceramide/sulfatide-containing liposomes with cultured oligodendrocytes and requirement for myelin basic protein and glycosphingolipids.
  J Neurosci Res, 86, 1448-1458.  
18829575 W.Wilson, and A.S.Baldwin (2008).
Maintenance of constitutive IkappaB kinase activity by glycogen synthase kinase-3alpha/beta in pancreatic cancer.
  Cancer Res, 68, 8156-8163.  
18544676 Y.Xia, C.Z.Wang, J.Liu, N.C.Anastasio, and K.M.Johnson (2008).
Lithium protection of phencyclidine-induced neurotoxicity in developing brain: the role of phosphatidylinositol-3 kinase/Akt and mitogen-activated protein kinase kinase/extracellular signal-regulated kinase signaling pathways.
  J Pharmacol Exp Ther, 326, 838-848.  
17355201 A.Baki, A.Bielik, L.Molnár, G.Szendrei, and G.M.Keserü (2007).
A high throughput luminescent assay for glycogen synthase kinase-3beta inhibitors.
  Assay Drug Dev Technol, 5, 75-83.  
17685868 A.J.Stewart, A.Fox, B.H.Morimoto, and I.Gozes (2007).
Looking for novel ways to treat the hallmarks of Alzheimer's disease.
  Expert Opin Investig Drugs, 16, 1183-1196.  
17544131 A.R.Cole, A.Astell, C.Green, and C.Sutherland (2007).
Molecular connexions between dementia and diabetes.
  Neurosci Biobehav Rev, 31, 1046-1063.  
17697341 A.Tighe, A.Ray-Sinha, O.D.Staples, and S.S.Taylor (2007).
GSK-3 inhibitors induce chromosome instability.
  BMC Cell Biol, 8, 34.  
17463171 A.V.Ougolkov, N.D.Bone, M.E.Fernandez-Zapico, N.E.Kay, and D.D.Billadeau (2007).
Inhibition of glycogen synthase kinase-3 activity leads to epigenetic silencing of nuclear factor kappaB target genes and induction of apoptosis in chronic lymphocytic leukemia B cells.
  Blood, 110, 735-742.  
17997701 J.Avila, and F.Hernández (2007).
GSK-3 inhibitors for Alzheimer's disease.
  Expert Rev Neurother, 7, 1527-1533.  
17906685 M.L.Selenica, H.S.Jensen, A.K.Larsen, M.L.Pedersen, L.Helboe, M.Leist, and J.Lotharius (2007).
Efficacy of small-molecule glycogen synthase kinase-3 inhibitors in the postnatal rat model of tau hyperphosphorylation.
  Br J Pharmacol, 152, 959-979.  
17541419 M.P.Mazanetz, and P.M.Fischer (2007).
Untangling tau hyperphosphorylation in drug design for neurodegenerative diseases.
  Nat Rev Drug Discov, 6, 464-479.  
18615180 S.Chen, X.J.Zhang, L.Li, and W.D.Le (2007).
Current experimental therapy for Alzheimer's disease.
  Curr Neuropharmacol, 5, 127-134.  
17575052 Y.Fang, S.Sathyanarayanan, and A.Sehgal (2007).
Post-translational regulation of the Drosophila circadian clock requires protein phosphatase 1 (PP1).
  Genes Dev, 21, 1506-1518.  
17698586 Y.Jossin, and A.M.Goffinet (2007).
Reelin signals through phosphatidylinositol 3-kinase and Akt to control cortical development and through mTor to regulate dendritic growth.
  Mol Cell Biol, 27, 7113-7124.  
16397900 A.Gómez-Ramos, J.Domínguez, D.Zafra, H.Corominola, R.Gomis, J.J.Guinovart, and J.Avila (2006).
Sodium tungstate decreases the phosphorylation of tau through GSK3 inactivation.
  J Neurosci Res, 83, 264-273.  
16300633 A.Habas, G.Kharebava, E.Szatmari, and M.Hetman (2006).
NMDA neuroprotection against a phosphatidylinositol-3 kinase inhibitor, LY294002 by NR2B-mediated suppression of glycogen synthase kinase-3beta-induced apoptosis.
  J Neurochem, 96, 335-348.  
17115923 A.M.de Raemy-Schenk, S.Troublé, P.Gaillard, P.Page, J.P.Gotteland, A.Scheer, P.Lang, and K.Yeow (2006).
A cellular assay for measuring the modulation of glucose production in H4IIE cells.
  Assay Drug Dev Technol, 4, 525-533.  
16892358 A.P.Kozikowski, I.N.Gaisina, P.A.Petukhov, J.Sridhar, L.T.King, S.Y.Blond, T.Duka, M.Rusnak, and A.Sidhu (2006).
Highly potent and specific GSK-3beta inhibitors that block tau phosphorylation and decrease alpha-synuclein protein expression in a cellular model of Parkinson's disease.
  ChemMedChem, 1, 256-266.  
16951223 A.V.Ougolkov, M.E.Fernandez-Zapico, V.N.Bilim, T.C.Smyrk, S.T.Chari, and D.D.Billadeau (2006).
Aberrant nuclear accumulation of glycogen synthase kinase-3beta in human pancreatic cancer: association with kinase activity and tumor dedifferentiation.
  Clin Cancer Res, 12, 5074-5081.  
16981824 C.A.Dickey, and L.Petrucelli (2006).
Current strategies for the treatment of Alzheimer's disease and other tauopathies.
  Expert Opin Ther Targets, 10, 665-676.  
16935409 E.Beurel, and R.S.Jope (2006).
The paradoxical pro- and anti-apoptotic actions of GSK3 in the intrinsic and extrinsic apoptosis signaling pathways.
  Prog Neurobiol, 79, 173-189.  
17062013 N.Dessalew, and P.V.Bharatam (2006).
Investigation of potential glycogen synthase kinase 3 inhibitors using pharmacophore mapping and virtual screening.
  Chem Biol Drug Des, 68, 154-165.  
16706678 T.D.Gould (2006).
Targeting glycogen synthase kinase-3 as an approach to develop novel mood-stabilising medications.
  Expert Opin Ther Targets, 10, 377-392.  
16307379 A.Caricasole, A.Bakker, A.Copani, F.Nicoletti, G.Gaviraghi, and G.C.Terstappen (2005).
Two sides of the same coin: Wnt signaling in neurodegeneration and neuro-oncology.
  Biosci Rep, 25, 309-327.  
16181430 C.Hawkes, J.H.Jhamandas, and S.Kar (2005).
Selective loss of basal forebrain cholinergic neurons by 192 IgG-saporin is associated with decreased phosphorylation of Ser glycogen synthase kinase-3beta.
  J Neurochem, 95, 263-272.  
15791206 E.J.McManus, K.Sakamoto, L.J.Armit, L.Ronaldson, N.Shpiro, R.Marquez, and D.R.Alessi (2005).
Role that phosphorylation of GSK3 plays in insulin and Wnt signalling defined by knockin analysis.
  EMBO J, 24, 1571-1583.  
15855730 H.Yamamoto (2005).
[Regulation of phosphorylation of tau by insulin and Ca2+ signals]
  Nippon Yakurigaku Zasshi, 125, 129-135.  
16133867 S.Bhattacharya, R.M.Ray, and L.R.Johnson (2005).
Decreased apoptosis in polyamine depleted IEC-6 cells depends on Akt-mediated NF-kappaB activation but not GSK3beta activity.
  Apoptosis, 10, 759-776.  
15867159 W.Noble, E.Planel, C.Zehr, V.Olm, J.Meyerson, F.Suleman, K.Gaynor, L.Wang, J.LaFrancois, B.Feinstein, M.Burns, P.Krishnamurthy, Y.Wen, R.Bhat, J.Lewis, D.Dickson, and K.Duff (2005).
Inhibition of glycogen synthase kinase-3 by lithium correlates with reduced tauopathy and degeneration in vivo.
  Proc Natl Acad Sci U S A, 102, 6990-6995.  
15152189 G.Morfini, G.Szebenyi, H.Brown, H.C.Pant, G.Pigino, S.DeBoer, U.Beffert, and S.T.Brady (2004).
A novel CDK5-dependent pathway for regulating GSK3 activity and kinesin-driven motility in neurons.
  EMBO J, 23, 2235-2245.  
15173837 P.Cohen, and M.Goedert (2004).
GSK3 inhibitors: development and therapeutic potential.
  Nat Rev Drug Discov, 3, 479-487.  
15189333 R.V.Bhat, S.L.Budd Haeberlein, and J.Avila (2004).
Glycogen synthase kinase 3: a drug target for CNS therapies.
  J Neurochem, 89, 1313-1317.  
14700633 L.Meijer, A.L.Skaltsounis, P.Magiatis, P.Polychronopoulos, M.Knockaert, M.Leost, X.P.Ryan, C.A.Vonica, A.Brivanlou, R.Dajani, C.Crovace, C.Tarricone, A.Musacchio, S.M.Roe, L.Pearl, and P.Greengard (2003).
GSK-3-selective inhibitors derived from Tyrian purple indirubins.
  Chem Biol, 10, 1255-1266.
PDB code: 1uv5
14700620 P.M.Fischer (2003).
CDK versus GSK-3 inhibition: a purple haze no longer?
  Chem Biol, 10, 1144-1146.  
The most recent references are shown first. Citation data come partly from CiteXplore and partly from an automated harvesting procedure. Note that this is likely to be only a partial list as not all journals are covered by either method. However, we are continually building up the citation data so more and more references will be included with time. Where a reference describes a PDB structure, the PDB code is shown on the right.

 

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