Grant Detail
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Abnormal Hyperphosphorylation of Tau
1 February 2001 - 30 April 2012
NATIONAL INSTITUTE ON AGING
Total Funding: $ 3,687,819
DESCRIPTION (provided by applicant): The overall objective of this proposal is to understand the molecular mechanism of neurofibrillary degeneration of abnormally hyperphosphorylated tau protein and, based on this knowledge, identify specific therapeutic targets for Alzheimer disease (AD), Down syndrome and other tauopathies which are characterized by this brain lesion. The activity of protein phosphatase (PP)-2A, which regulates phosphorylation of tau, is in turn regulated partly by its inhibitor I2PP2A. In a large percentage of neurons in AD brain, I2PP2A is translocated from its primary localization in the nucleus to the cytoplasm. As PP-2A and tau are localized in the cytoplasm, the increased cytoplasmic localization of I2PP2A in AD brain explains the inhibition of PP-2A, tau hyperphosphorylation and formation of neurofibrillary tangles. We propose (1) to investigate the molecular mechanism which controls the nuclear vs. cytoplasmic localization of I2PP2A in normal neurons. The transport factors (karyopherins) that mediate the import and export of I2PP2A into and out of the nuclei, and the I2PP2A domains which interact with these factors will be identified;(2) to elucidate the cause(s) of modified neuronal I2PP2A localization in Alzheimer's disease. We will investigate the effect of the cleavage of I2PP2A, which occurs in AD brains, on the I2PP2A interaction with the transport factors. We will also investigate the effects of the interactions of I2PP2A with other soluble and fixed proteins on I2PP2A localization in normal and AD brain, and the role of I2PP2A phosphorylation;(3) to generate transgenic mice which express the N-terminal half I2PP2A (observed in the cytoplasm of neurons in the AD brain) or a control variant of this protein localized in the nuclei, under the control of an inducible expression system. The effect of these transgenes on PP-2A activity, the activities of tau kinases regulated by PP-2A and abnormal hyperphosphorylation of tau, and as well as neurodegeneration and cognitive impairment, will be studied. These studies will lead to the elucidation of the mechanism of neurofibrillary degeneration and to the identification of one or more therapeutic targets. The studies will lead also to the generation of a cellular and an animal model of tauopathies, which can be used for the development of therapeutic drugs for diseases characterized by this lesion.
74 Resulting Publications
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1.
2013Jian-Zhi Wang; Yi-Yuan Xia; Inge Grundke-Iqbal; Khalid Iqbal
Journal of Alzheimer's disease : JAD 2013;33 Suppl 1():S123-39. -
2.
2012Jianhua Shi; Shiliang Wu; Chun-ling Dai; Yi Li; Inge Grundke-Iqbal; Khalid Iqbal; Fei Liu; Cheng-Xin Gong
Diverse regulation of AKT and GSK-3β by O-GlcNAcylation in various types of cells.
FEBS letters 2012;586(16):2443-50. -
3.
2012Shaohong Ding; Jianhua Shi; Wei Qian; Khalid Iqbal; Inge Grundke-Iqbal; Cheng-Xin Gong; Fei Liu
Regulation of alternative splicing of tau exon 10 by 9G8 and Dyrk1A.
Neurobiology of aging 2012;33(7):1389-99. -
4.
2012Yang Yu; Lan Zhang; Xiaojing Li; Xiaoqin Run; Zhihou Liang; Yi Li; Ying Liu; Moon H Lee; Inge Grundke-Iqbal; Khalid Iqbal; et al.
Differential effects of an O-GlcNAcase inhibitor on tau phosphorylation.
PloS one 2012;7(4):e35277. -
5.
2012Ying Liu; Xiaojing Li; Yang Yu; Jianhua Shi; Zhihou Liang; Xiaoqin Run; Yi Li; Chun-ling Dai; Inge Grundke-Iqbal; Khalid Iqbal; et al.
PloS one 2012;7(8):e43724. -
6.
2011Khalid Iqbal; Inge Grundke-Iqbal
Opportunities and challenges in developing Alzheimer disease therapeutics.
Acta neuropathologica 2011;122(5):543-9. -
7.
2011Lisette Arnaud; She Chen; Fei Liu; Bin Li; Sabiha Khatoon; Inge Grundke-Iqbal; Khalid Iqbal
Mechanism of inhibition of PP2A activity and abnormal hyperphosphorylation of tau by I2(PP2A)/SET.
FEBS letters 2011;585(17):2653-9. -
8.
2011Ying Liu; Fei Liu; Inge Grundke-Iqbal; Khalid Iqbal; Cheng-Xin Gong
Deficient brain insulin signalling pathway in Alzheimer's disease and diabetes.
The Journal of pathology 2011;225(1):54-62. -
9.
2011Jianhua Shi; Wei Qian; Xiaomin Yin; Khalid Iqbal; Inge Grundke-Iqbal; Xiaosong Gu; Fei Ding; Cheng-Xin Gong; Fei Liu
The Journal of biological chemistry 2011;286(16):14639-48. -
10.
2011Wei Qian; Xiaomin Yin; Wen Hu; Jianhua Shi; Jianlan Gu; Inge Grundke-Iqbal; Khalid Iqbal; Cheng-Xin Gong; Fei Liu
Activation of protein phosphatase 2B and hyperphosphorylation of Tau in Alzheimer's disease.
Journal of Alzheimer's disease : JAD 2011;23(4):617-27. -
11.
2010K Iqbal; F Liu; C-X Gong; I Grundke-Iqbal
Tau in Alzheimer disease and related tauopathies.
Current Alzheimer research 2010;7(8):656-64. -
12.
2010Xiaochuan Wang; Julie Blanchard; Erik Kohlbrenner; Nathalie Clement; R Michael Linden; Aurelian Radu; Inge Grundke-Iqbal; Khalid Iqbal
FASEB journal : official publication of the Federation of American Societies for Experimental Biology 2010;24(11):4420-32. -
13.
2010Alejandra D Alonso; John Di Clerico; Bin Li; Christopher P Corbo; Maria E Alaniz; Inge Grundke-Iqbal; Khalid Iqbal
Phosphorylation of tau at Thr212, Thr231, and Ser262 combined causes neurodegeneration.
The Journal of biological chemistry 2010;285(40):30851-60. -
14.
2010Khalid Iqbal; Inge Grundke-Iqbal
Alzheimer's disease, a multifactorial disorder seeking multitherapies.
Alzheimer's & dementia : the journal of the Alzheimer's Association 2010;6(5):420-4. -
15.
2010Khalid Iqbal; Xiaochuan Wang; Julie Blanchard; Fei Liu; Cheng-Xin Gong; Inge Grundke-Iqbal
Alzheimer's disease neurofibrillary degeneration: pivotal and multifactorial.
Biochemical Society transactions 2010;38(4):962-6. -
16.
2010Wei Qian; Jianhua Shi; Xiaomin Yin; Khalid Iqbal; Inge Grundke-Iqbal; Cheng-Xin Gong; Fei Liu
PP2A regulates tau phosphorylation directly and also indirectly via activating GSK-3beta.
Journal of Alzheimer's disease : JAD 2010;19(4):1221-9. -
17.
2009Sonia Chalbot; Henrik Zetterberg; Kaj Blennow; Tormod Fladby; Inge Grundke-Iqbal; Khalid Iqbal
Clinical chemistry 2009;55(12):2171-9. -
18.
2009Yanqiu Deng; Bin Li; Ying Liu; Khalid Iqbal; Inge Grundke-Iqbal; Cheng-Xin Gong
The American journal of pathology 2009;175(5):2089-98. -
19.
2009Ying Liu; Fei Liu; Inge Grundke-Iqbal; Khalid Iqbal; Cheng-Xin Gong
Journal of neurochemistry 2009;111(1):242-9. -
20.
2009Khalid Iqbal; Fei Liu; Cheng-Xin Gong; Alejandra Del C Alonso; Inge Grundke-Iqbal
Mechanisms of tau-induced neurodegeneration.
Acta neuropathologica 2009;118(1):53-69. -
21.
2009Yang Yu; Xiaoqin Run; Zhihou Liang; Yi Li; Fei Liu; Ying Liu; Khalid Iqbal; Inge Grundke-Iqbal; Cheng-Xin Gong
Developmental regulation of tau phosphorylation, tau kinases, and tau phosphatases.
Journal of neurochemistry 2009;108(6):1480-94. -
22.
2009Xiaoqin Run; Zhihou Liang; Lan Zhang; Khalid Iqbal; Inge Grundke-Iqbal; Cheng-Xin Gong
Anesthesia induces phosphorylation of tau.
Journal of Alzheimer's disease : JAD 2009;16(3):619-26. -
23.
2009Zhihou Liang; Fei Liu; Khalid Iqbal; Inge Grundke-Iqbal; Cheng-Xin Gong
Dysregulation of tau phosphorylation in mouse brain during excitotoxic damage.
Journal of Alzheimer's disease : JAD 2009;17(3):531-9. -
24.
2008Jianhua Shi; Tianyi Zhang; Chunlei Zhou; Muhammad Omar Chohan; Xiaosong Gu; Jerzy Wegiel; Jianhua Zhou; Yu-Wen Hwang; Khalid Iqbal; Inge Grundke-Iqbal; et al.
The Journal of biological chemistry 2008;283(42):28660-9. -
25.
2008Khalid Iqbal; M Omar Chohan; Inge Grundke-Iqbal
Journal of Alzheimer's disease : JAD 2008;15(2):339-45. -
26.
2008Fei Liu; Zhihou Liang; Jerzy Wegiel; Yu-Wen Hwang; Khalid Iqbal; Inge Grundke-Iqbal; Narayan Ramakrishna; Cheng-Xin Gong
Overexpression of Dyrk1A contributes to neurofibrillary degeneration in Down syndrome.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology 2008;22(9):3224-33. -
27.
2008Khalid Iqbal; Alejandra del C Alonso; Inge Grundke-Iqbal
Journal of Alzheimer's disease : JAD 2008;14(4):365-70. -
28.
2008She Chen; Bin Li; Inge Grundke-Iqbal; Khalid Iqbal
The Journal of biological chemistry 2008;283(16):10513-21. -
29.
2008Yanqiu Deng; Bin Li; Fei Liu; Khalid Iqbal; Inge Grundke-Iqbal; Roland Brandt; Cheng-Xin Gong
FASEB journal : official publication of the Federation of American Societies for Experimental Biology 2008;22(1):138-45. -
30.
2008Bin Li; Hidenaga Yamamori; Yoshitaka Tatebayashi; Bridget Shafit-Zagardo; Hitoshi Tanimukai; She Chen; Khalid Iqbal; Inge Grundke-Iqbal
Failure of neuronal maturation in Alzheimer disease dentate gyrus.
Journal of neuropathology and experimental neurology 2008;67(1):78-84. -
31.
2008K Iqbal; I Grundke-Iqbal
Alzheimer neurofibrillary degeneration: significance, etiopathogenesis, therapeutics and prevention.
Journal of cellular and molecular medicine 2008;12(1):38-55. -
32.
2008C-X Gong; K Iqbal
Current medicinal chemistry 2008;15(23):2321-8. -
33.
2007Zhihou Liang; Fei Liu; Inge Grundke-Iqbal; Khalid Iqbal; Cheng-Xin Gong
Journal of neurochemistry 2007;103(6):2462-70. -
34.
2007Fei Liu; Bin Li; E-Jan Tung; Inge Grundke-Iqbal; Khalid Iqbal; Cheng-Xin Gong
The European journal of neuroscience 2007;26(12):3429-36. -
35.
2007K Iqbal; I Grundke-Iqbal
Developing pharmacological therapies for Alzheimer disease.
Cellular and molecular life sciences : CMLS 2007;64(17):2234-44. -
36.
2007Hidenaga Yamamori; Sabiha Khatoon; Inge Grundke-Iqbal; Kaj Blennow; Michael Ewers; Harald Hampel; Khalid Iqbal
Neuroscience letters 2007;418(2):186-9. -
37.
2007Bin Li; Muhammad Omar Chohan; Inge Grundke-Iqbal; Khalid Iqbal
Disruption of microtubule network by Alzheimer abnormally hyperphosphorylated tau.
Acta neuropathologica 2007;113(5):501-11. -
38.
2007Jian-Zhi Wang; Inge Grundke-Iqbal; Khalid Iqbal
Kinases and phosphatases and tau sites involved in Alzheimer neurofibrillary degeneration.
The European journal of neuroscience 2007;25(1):59-68. -
39.
2006Amitabha Sengupta; Inge Grundke-Iqbal; Khalid Iqbal
Regulation of phosphorylation of tau by protein kinases in rat brain.
Neurochemical research 2006;31(12):1473-80. -
40.
2006Fei Liu; Zhihou Liang; Jianhua Shi; Dongmei Yin; Ezzat El-Akkad; Inge Grundke-Iqbal; Khalid Iqbal; Cheng-Xin Gong
FEBS letters 2006;580(26):6269-74. -
41.
2006Amitabha Sengupta; Michal Novak; Inge Grundke-Iqbal; Khalid Iqbal
FEBS letters 2006;580(25):5925-33. -
42.
2006Muhammad Omar Chohan; Khalid Iqbal
From tau to toxicity: emerging roles of NMDA receptor in Alzheimer's disease.
Journal of Alzheimer's disease : JAD 2006;10(1):81-7. -
43.
2006Muhammad Omar Chohan; Sabiha Khatoon; Inge-Grundke Iqbal; Khalid Iqbal
Involvement of I2PP2A in the abnormal hyperphosphorylation of tau and its reversal by Memantine.
FEBS letters 2006;580(16):3973-9. -
44.
2006Alejandra del C Alonso; Bin Li; Inge Grundke-Iqbal; Khalid Iqbal
Polymerization of hyperphosphorylated tau into filaments eliminates its inhibitory activity.
Proceedings of the National Academy of Sciences of the United States of America 2006;103(23):8864-9. -
45.
2006A Rahman; I Grundke-Iqbal; K Iqbal
Journal of neural transmission (Vienna, Austria : 1996) 2006;113(2):219-30. -
46.
2006Khalid Iqbal; Inge Grundke-Iqbal
Journal of Alzheimer's disease : JAD 2006;9(3 Suppl):219-42. -
47.
2005Fei Liu; Inge Grundke-Iqbal; Khalid Iqbal; Yoshiya Oda; Kazuhito Tomizawa; Cheng-Xin Gong
Truncation and activation of calcineurin A by calpain I in Alzheimer disease brain.
The Journal of biological chemistry 2005;280(45):37755-62. -
48.
2005Khalid Iqbal; Michael Flory; Sabiha Khatoon; Hilkka Soininen; Tuula Pirttila; Maarit Lehtovirta; Irina Alafuzoff; Kaj Blennow; Niels Andreasen; Eugeen Vanmechelen; et al.
Subgroups of Alzheimer's disease based on cerebrospinal fluid molecular markers.
Annals of neurology 2005;58(5):748-57. -
49.
2005M O Chohan; N Haque; A Alonso; E El-Akkad; I Grundke-Iqbal; A Grover; K Iqbal
Hyperphosphorylation-induced self assembly of murine tau: a comparison with human tau.
Journal of neural transmission (Vienna, Austria : 1996) 2005;112(8):1035-47. -
50.
2005Khalid Iqbal; Inge Grundke-Iqbal
Pharmacological approaches of neurofibrillary degeneration.
Current Alzheimer research 2005;2(3):335-41. -
51.
2005C-X Gong; F Liu; I Grundke-Iqbal; K Iqbal
Post-translational modifications of tau protein in Alzheimer's disease.
Journal of neural transmission (Vienna, Austria : 1996) 2005;112(6):813-38. -
52.
2005Hitoshi Tanimukai; Inge Grundke-Iqbal; Khalid Iqbal
Up-regulation of inhibitors of protein phosphatase-2A in Alzheimer's disease.
The American journal of pathology 2005;166(6):1761-71. -
53.
2005Abdur Rahman; Inge Grundke-Iqbal; Khalid Iqbal
Neurochemical research 2005;30(2):277-87. -
54.
2005Ichiro Tsujio; Tanweer Zaidi; Jiliu Xu; Leszek Kotula; Inge Grundke-Iqbal; Khalid Iqbal
FEBS letters 2005;579(2):363-72. -
55.
2005Yu Huang; Fei Liu; Inge Grundke-Iqbal; Khalid Iqbal; Cheng-Xin Gong
Neuroscience letters 2005;373(2):115-8. -
56.
2005Khalid Iqbal; Alejandra del C Alonso; She Chen; M Omar Chohan; Ezzat El-Akkad; Cheng-Xin Gong; Sabiha Khatoon; Bin Li; Fei Liu; Abdur Rahman; et al.
Tau pathology in Alzheimer disease and other tauopathies.
Biochimica et biophysica acta 2005;1739(2-3):198-210. -
57.
2005Li Sun; XiaoChuang Wang; Shengyuan Liu; Quan Wang; JianZhi Wang; Malika Bennecib; Cheng-Xin Gong; Amitabha Sengupta; Inge Grundke-Iqbal; Khalid Iqbal
FEBS letters 2005;579(1):251-8. -
58.
2005Khalid Iqbal; Inge Grundke-Iqbal
Metabolic/signal transduction hypothesis of Alzheimer's disease and other tauopathies.
Acta neuropathologica 2005;109(1):25-31. -
59.
2004Yu Huang; Hitoshi Tanimukai; Fei Liu; Khalid Iqbal; Inge Grundke-Iqbal; Cheng-Xin Gong
Elevation of the level and activity of acid ceramidase in Alzheimer's disease brain.
The European journal of neuroscience 2004;20(12):3489-97. -
60.
2004Shi Jie Liu; Jia Yu Zhang; Hong Lian Li; Zheng Yu Fang; Qun Wang; Heng Mei Deng; Cheng Xin Gong; Inge Grundke-Iqbal; Khalid Iqbal; Jian Zhi Wang
Tau becomes a more favorable substrate for GSK-3 when it is prephosphorylated by PKA in rat brain.
The Journal of biological chemistry 2004;279(48):50078-88. -
61.
2004Niloufar Haque; Cheng-Xin Gong; Amitabha Sengupta; Khalid Iqbal; Inge Grundke-Iqbal
Brain research. Molecular brain research 2004;129(1-2):163-70. -
62.
2004Alejandra del C Alonso; Anna Mederlyova; Michal Novak; Inge Grundke-Iqbal; Khalid Iqbal
Promotion of hyperphosphorylation by frontotemporal dementia tau mutations.
The Journal of biological chemistry 2004;279(33):34873-81. -
63.
2004K Iqbal; I Grundke-Iqbal
Current drug targets 2004;5(6):495-502. -
64.
2004Hitoshi Tanimukai; Inge Grundke-Iqbal; Khalid Iqbal
Inhibitors of protein phosphatase-2A: topography and subcellular localization.
Brain research. Molecular brain research 2004;126(2):146-56. -
65.
2004Fei Liu; Khalid Iqbal; Inge Grundke-Iqbal; Gerald W Hart; Cheng-Xin Gong
O-GlcNAcylation regulates phosphorylation of tau: a mechanism involved in Alzheimer's disease.
Proceedings of the National Academy of Sciences of the United States of America 2004;101(29):10804-9. -
66.
2004Liang Li; Amitabha Sengupta; Niloufar Haque; Inge Grundke-Iqbal; Khalid Iqbal
FEBS letters 2004;566(1-3):261-9. -
67.
2004Yoshitaka Tatebayashi; Niloufar Haque; Yunn-Chyn Tung; Khalid Iqbal; Inge Grundke-Iqbal
Journal of cell science 2004;117(Pt 9):1653-63. -
68.
2004Cheng-Xin Gong; Fei Liu; Guoxin Wu; Sandra Rossie; Jerzy Wegiel; Liang Li; Inge Grundke-Iqbal; Khalid Iqbal
Dephosphorylation of microtubule-associated protein tau by protein phosphatase 5.
Journal of neurochemistry 2004;88(2):298-310. -
69.
2003Jin-Jing Pei; Cheng-Xin Gong; Wen-Lin An; Bengt Winblad; Richard F Cowburn; Inge Grundke-Iqbal; Khalid Iqbal
The American journal of pathology 2003;163(3):845-58. -
70.
2003Wen-Lin An; Richard F Cowburn; Lin Li; Heiko Braak; Irina Alafuzoff; Khalid Iqbal; Inge-Grundke Iqbal; Bengt Winblad; Jin-Jing Pei
The American journal of pathology 2003;163(2):591-607. -
71.
2003Jin-Jing Pei; Sabiha Khatoon; Wen-Lin An; Maria Nordlinder; Toshihisa Tanaka; Heiko Braak; Ichiro Tsujio; Masatoshi Takeda; Irina Alafuzoff; Bengt Winblad; et al.
Role of protein kinase B in Alzheimer's neurofibrillary pathology.
Acta neuropathologica 2003;105(4):381-92. -
72.
2003Khalid Iqbal; Alejandra del C Alonso; Ezzat El-Akkad; Cheng-Xin Gong; Niloufar Haque; Sabiha Khatoon; Jin-Jing Pei; Hitoshi Tanimukai; Ichiro Tsujio; Jian-Zhi Wang; et al.
Alzheimer neurofibrillary degeneration: therapeutic targets and high-throughput assays.
Journal of molecular neuroscience : MN 2003;20(3):425-9. -
73.
2002Jin-Jing Pei; Heiko Braak; Wen-Lin An; Bengt Winblad; Richard F Cowburn; Khalid Iqbal; Inge Grundke-Iqbal
Brain research. Molecular brain research 2002;109(1-2):45-55. -
74.
2002Fei Liu; Khalid Iqbal; Inge Grundke-Iqbal; Cheng-Xin Gong
Involvement of aberrant glycosylation in phosphorylation of tau by cdk5 and GSK-3beta.
FEBS letters 2002;530(1-3):209-14.
Scientific Context
This section shows information that has been computed by using the fingerprint of the grant, including related publications, related experts and related grants - all with fingerprints representing significant amounts of overlap between their fingerprint and this grant. The red dots indicate whether those experts or terms actually appear within this grant, showing potential and actual connections.
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Related Publications
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2009Khalid Iqbal; Fei Liu; Cheng-Xin Gong; Alejandra Del C Alonso; Inge Grundke-Iqbal
Mechanisms of tau-induced neurodegeneration.
Acta neuropathologica 2009;118(1):53-69. -
2.
2005Khalid Iqbal; Alejandra del C Alonso; She Chen; M Omar Chohan; Ezzat El-Akkad; Cheng-Xin Gong; Sabiha Khatoon; Bin Li; Fei Liu; Abdur Rahman; et al.
Tau pathology in Alzheimer disease and other tauopathies.
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