Identification and use of selective inhibitors of glycogen synth

Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving antigen-antibody binding – specific binding protein...

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

435 4, 435 71, 435 792, 435194, 4352872, 514 1, 514 2, G01N 3353

Patent

active

060571179

ABSTRACT:
The invention provides for use of selective inhibitors of GSK3 for treatment of diseases that are mediated by GSK3 activity, including non-insulin dependent diabetes mellitus (NIDDM) and Alzheimer's disease. Also described are methods of identifying inhibitors of GSK3 activity. The selective GSK3 inhibitor can be a peptide, peptoid, small organic molecule, or polynucleotide.

REFERENCES:
patent: 5252333 (1993-10-01), Horrobin
Wang et al. (1994) Analytical Biochem. 220, pp. 397-402, 1994.
Anderton et al., "Modulation of PHF-Like tau Phosphorylation in Cultured Neurones and Transfected Cells", Neurobiology of Aging 16(3):389-402, 1995.
Borthwick et al., "Inhibition of Glycogen Synthase Kinase-3 by Insulin in Cultured Human Skeletal Muscle Myoblasts", Biochemical and Biophysical Research Communications 210(3):738-745, May 25, 1995.
Huang et al., "Glucose-6-P Control of Glycogen Synthase Phosphorylation in Yeast", The Journal of Biological Chemistry, vol. 272, No. 36, Sep. 5, 1997, pp. 22495-22501.
Ishiguro et al., "Glycogen Synthase Kinase 3.beta. is Identical to Tau Protein Kinase I Generating Several Epitopes of Paired Helical Filaments", FEBS 12596 Lett, Jul. 1993, pp. 167-172.
Ishiguro et al., Chemical Abstract No. 126:291921, "Advances in Neurological Sciences," No. 212, vol. 41, No. 1, Feb. 1997.
Klein and Melton, "A Molecular Mechanism for the Effect of Lithium on Development", Proc. Natl. Acad. Sci. USA 93:8455-8459, Aug., 1996.
Latimer et al., "Stimulation of MAP Kinase by v-raf Transformation of Fibroblasts Fails to Induce Hyperphosphorylation of Transfected tau", FEBS Letters 365:42-46, 1995.
Lovestone et al., "Alzheimer's Disease-Like Phosphorylation of the Microtubule-Associated Protein tau by glycogen Synthase Kinase-3 in Transfected Mammalian Cells", Current Biology 4(12):1077-1086, 1994.
Massillon et al., "Identification of the Glycogenic Compound 5-Iodotubercidin as a General Protein Kinase Inhibitor", Biochem J. 299:123-128, 1994.
Pugazhenthi et al., "Regulation of Glycogen Synthase Activation in Isolated Hepatocytes", Molecular and Cellular Biochemistry, 149/150:95-101, 1995.
Saran, "Antidiabetic Effects of Lithium" J. Clin. Psychiatry 43(9):383-384, Sep., 1982.
Sperber et al., "Glycogen Synthase Kinase-3.beta. Phosphorylates tau Protein at Multiple sites in Intact Cells" Neuroscience Letters 197:149-153, 1995.
Stambolic et al., "Lithium Inhibits Glycogen Synthase Kinase-3 Activity and Mimics Wingless Signalling in Intact Cells" Current Biology 6(12):1664-1668, 1996.
Sutherland et al., "Inactivation of Glycogen Synthase Kinase-3.beta. by Phosphorylation: New Kinase Connections in Insulin and Growth-Factor Signalling" Biochem. J. 196:15-19, 1993.
Takashima et al., "Amyloid .beta. Peptide Induces Cytoplasmic Accumulation of Amyloid Protein Precursor via tau Protein Kinase I/glycogen Synthase Kinase-3.beta. in rat Hippocampal Neurons" Neuroscience Letters 198:83-86, 1995.
Takashima et al., "Exposure of rat hippocampal Neurons to Amyloid .beta. Peptide (25-35) Induces the Inactivation of Phosphatidyl Inositol-3 Kinase and the Activation of tau Protein Kinase I/glycogen Synthase Kinase-3.beta." Neuroscience Letters 203:33-36, 1996.
Takashima et al., "tau Protein Kinase I is Essential for Amyloid .beta.-Protein-Induced Neurotoxicity", Proc. Natl. Acad. Sci., USA 90:7789-7993, Aug. 1993.
Lovestone et al. (1994) Current Biol. 4/12, pp. 1077-1086.
Latimer et al. (1995) FEBS Letters 365, pp. 42-46.
Song et al. (1995) J. Protein Chem. 14/2, pp. 95-105.
Cross et al. (1995) Nature 378, pp. 785-789.
Fiol et al., "Ordered Multisite Protein Phosphorylation", The Journal of Biological Chemistry, vol. 265, No. 11, pp. 6061-6065 (1990).
Hegazy et al., "Inhibition of Glycogen Synthase Kinase 3 by Polycations", 72nd Annual Meeting of the Federation of American Societies for Experimental Biology, Las Vegas, Nevada, USA, May 1-5, 1988, FASETS (Fed. Am. Soc. Exp. Biol.) J2(4) 1988, Abstract.
Baum et al., "Overexpressed tau protein in cultured cells is phosphorylated without formation of PHF: implication of phosphoprotein phosphatase involvement", 1995, Molecular Brain Research, 34:1-17.
Ciudad et al., "Control of glycogen synthase phosphorylation in isolated rat hepatocytes by epinephrine, vasopressin and glucagon", 1984, J Biochem., 142:511-520.
Cross et al., "The inhibition of glycogen synthase kinase-3 by insulin or 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-activated protein kinase pathway in L6 cells between Ras and Raf", 1994, J. Biochem., 303:21-26.
Hegazy et al., "Inhibitory effect of polycations on phophorylation of glycogen synthase by glycogen synthase kinase 3", 1989, BBA, 1011:198-204.
Hiken et al., "Rat skeletal muscle glycogen synthase: Phosphorylation of the purified enzyme by cAMP-dependnet and independent protein kinases", 1985, Archives of Biochemistry and Biophysics, 236:59-71.
Hoshi et al., "Regulation of mitochondrial pyruvate dehyrogenase activity by tau protein kinase I/glycogen synthase kinase 3.beta. in brain" 1996, Proc. Natl. Acad. Sci. USA, 93:2719-2723.
Imazu et al., "Phosphorylation and inactivation liver glycogen synthase by liver protein kinases" 1984, Journal of Biological Chemistry, 259(3):1813-1821.
Lawrence et al., "Control of glycogen synthase by insulin and isoproterenol in rat adipocytes", 1986, Journal Biological Chemistry, 261(2):669-677.
Lint et al. "A specific immunoprecipitation assay for the protein F.sub.A /glycogen synthase kinase 3.sup.1 ", 1993, Analytical Biochemistry, 208:132-137.
Liu et al., "The state of phosphorylation of normal adult brain .tau., fetal .tau. and .tau. from alzheimer paired helical filaments at amino acid residue ser.sup.262 ", 1996, Journal of Neurochemistry, 1131-1139.
Mandelkow et al., "Tau domains, phosphorylation, and interactions with microtubules" 1995, Neurobiology of Aging, 16(3):355-363.
Nitsch et al., "Alzheimer's disease amyloid precursor proteins, signal transduction, and neuronal transplantation" 1993, Annals of the New York Academy of Sciences, 695:209-216.
Singh et al., "Differential phosphorylation of human tau isoforms containing three repeats by several protein kinases" 1996, Archives of Biochemistry and Biophysics, 328(1):43-50.
Takahashi et al., "Localization and developmental changes of .tau. protein kinase I/glycogen synthase kinase-3.beta. in rat brain" 1994 Journal of Neurochemistry, 245-255.
Wang et al., "Use of a synthetic peptide as a selective substrate for glycogen synthase kinase3", 1994, Analytical Biochemistry, 220:397-402.
Wang et al., "Inactivation of rabbit muscle glycogen synthase by glocogen synthase kinase-3", 1993, J. Biol. Chem., 268(32):23876-23880.
Weber, "Advances in enzyme regulation", 1983, Pergamon Press, 21:322-330.
Yang et al., "Synergistic control mechanism for abnormal site phosphorylation of alzheimer's diseased brain tau by kinase F.sub.A /GSK-3.alpha.", 1993, Biochemical and Biophysical Research Communications, 197(2):400-406.
Yang et al., "Protein kinase F.sub.A /GSK-3 phosphorylates .tau. on ser.sup.235 -pro and ser.sup.404 -pro that are abnormally phosphorylated in alzheimer's disease brain", 1993, Journal of Neurochemistry, 1742-1747.
Zhang et al., "Mechanisms of multisite phosphorylation and inactivation of rabbit muscle glycogen synthase", 1993, Archives of Biochemistry and Biophysics, 304:219-225.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Identification and use of selective inhibitors of glycogen synth does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Identification and use of selective inhibitors of glycogen synth, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Identification and use of selective inhibitors of glycogen synth will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-1592768

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.