GSK3 polypeptides

The invention provides truncated GSK3 polypeptides capable of crystallization, including GSK3α and GSK3β polypeptides, and use of these polypeptides to identify and optimize GSK3 inhibitors. Also provided are GSK3 polypeptides having at least one substituted amino acid that differs from wild-type GS...

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Main Authors Harrison, Stephen D, Hall, John A, Calderon-Cacia, Maria, Zhong, Ziyang, Fang, Eric Y, Coit, Doris G, Nguyen, Steve H, Medina-Selby, Angelica
Format Patent
LanguageEnglish
Published 14.11.2006
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Abstract The invention provides truncated GSK3 polypeptides capable of crystallization, including GSK3α and GSK3β polypeptides, and use of these polypeptides to identify and optimize GSK3 inhibitors. Also provided are GSK3 polypeptides having at least one substituted amino acid that differs from wild-type GSK3, wherein the substituted amino acid is incapable of being phosphorylated. The invention finds use in providing methods of identifying and optimizing compounds useful for treating diseases mediated by GSK3 activity, including Alzheimer's disease, type 2 diabetes, and inflammation.
AbstractList The invention provides truncated GSK3 polypeptides capable of crystallization, including GSK3α and GSK3β polypeptides, and use of these polypeptides to identify and optimize GSK3 inhibitors. Also provided are GSK3 polypeptides having at least one substituted amino acid that differs from wild-type GSK3, wherein the substituted amino acid is incapable of being phosphorylated. The invention finds use in providing methods of identifying and optimizing compounds useful for treating diseases mediated by GSK3 activity, including Alzheimer's disease, type 2 diabetes, and inflammation.
Author Harrison, Stephen D
Calderon-Cacia, Maria
Medina-Selby, Angelica
Zhong, Ziyang
Coit, Doris G
Fang, Eric Y
Hall, John A
Nguyen, Steve H
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References Database EMBL Entry, Accession No. P49841, 1996.
Mulot et al., PHF-Tau from Alzheimer's Brain Comprises Four Species on SDS-PAGE Which Can Be Mimicked by in Vitro Phosphorylation of Human Brain Tau by Glycogen Synthase Kinase-3β, FEBS Letters, 349(3):359-364, 1994.
Database EMBL Entry, Accession No. U31862, 1995.
Welsh et al., Glycogen Synthase Kinase-3 is Rapidly Inactivated in Response to Insulin and Phosphorylates Eukaryotic Initiation Factor eIF-2B, Biochemical Journal, 294(Part 3):625-629, 1993.
(WO-99/65897) 19991200
GenBank accession No. AAA 84444 1996.
Peifer et al., Phosphorylation of the Drosophilia Adherens Junction Protein Armadillo: Roles for Wingless Signals and Zeste-White 3 Kinase, Developmental Biology, 166(2):543-556, 1994.
US 6,057,286, 05/2000, Harrison et al. (withdrawn)
Cross et al., The Inhibition of Glycogen Synthase Kinase-3 by Insulin-Like Growth Factor 1 in the Rat Skeletal Muscle Cell Line L6 is Blocked by Wortmannin, but Not by Rapamycin: Evidence that Wortmannin Blocks Activation of the Mitogen-Activiated Protein Kinase Pathway in L6 Cells Between Ras and Raf, Biochemical Journal, 303(Part 1):21-26, 1994.
Harrison et al. (6057117) 20000500
Summers et al., The Role of Glycogen Synthase Kinase 3β in Insulin-Stimulated Glucose Metabolism, Journal of Biological Chemistry, 274(25):17934-17940, 1999.
Database EMBL Entry, Accession No. P49840, 1996.
Woodgett, A Common Denominator Linking Glycogen Metabolism, Nuclear Oncogenes and Development, TIBS, 16(5):177-181, 1991.
Van Der Linden et al., Domain Organization of Penicillin-Binding Protein 5 from Escherichia coli Analysed by C-Terminal Truncation, Biochemical Journal, 289(Part 2):593-598, 1993.
Latimer et al., Stimulation of MAP Kinase by V-Raf Transformation of Fibroblasts Fails to Induce Hyperphosporylation of Transfected Tau, FEBS Letters, 365(1):42-46, 1995.
Ranty et al., Truncation of Ribulose-1, 5-Bisphosphate Carboxylase/Oxygenase (Rubisco) from Holoenzyme Assembly and Activity, EMBO Journal, 9:1365-1373, 1990.
Mandelkow et al., Tau as a Marker for Alzheimer's Disease, TIBS, 18(12):480-483, 1993.
Jancarik et al.., Sparse Matrix Sampling: A Screening Method for Crystallization of Proteins, J. of Applied Crystallography, 24(4):409-411, 1991.
Lovestone et al., Alzheimer's Disease-Like Physphorylation of the Microtubule-Associated Protein Tau by Glycogen Synthase Kinase-3 in Transfected Mammalian Cells, Current Biology, 4(12):1077-1086, 1994.
Saito et al., The Mechanism by Which Epidermal Growth Factor Inhibits Glycogen Synthase Kinase 3 in A431 Cells, Biochemical Journal, 303(Part 1):27-31, 1994.
Database EMBL Entry, Accession No. Q91627, 1996.
Bax et al., Structure 9:1143-1152, 2001.
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