Glycogen synthase kinase 3 (GSK-3) inhibitors as new promising drugs for diabetes, neurodegeneration, cancer, and inflammation

Medicinal Research Reviews

Volumn 22, Issue 4, 2002, Pages 373-384

  Martinez, Ana ^a   Castro, Ana ^a   Dorronsoro, Isabel ^a   Alonso, Mercedes ^a  

^a INSTITUTO DE QUÍMICA MÉDICA   (Spain)

Author keywords

Alzheimer's disease; Cancer; Diabetes type II; GSK 3 inhibitors; Inflammation

Indexed keywords

2 (2,4 DICHLOROPHENYL) 3 (1 METHYL 3 INDOLYL)MALEIMIDE; 2 (3 CHLORO 4 HYDROXYANILINO) 3 (2 NITROPHENYL)MALEIMIDE; 2 [1 (3 AMIDINOTHIOPROPYL) 1H INDOL 3 YL] 3 (1 METHYL 1H INDOL 3 YL)MALEIMIDE; 2 [1 (3 DIMETHYLAMINOPROPYL) 3 INDOLYL] 3 (3 INDOLYL)MALEIMIDE; AF 150; ALSTERPAULLONE; CEVIMELINE; CYCLIN DEPENDENT KINASE INHIBITOR; ENZYME INHIBITOR; GLYCOGEN SYNTHASE KINASE 3; GLYCOGEN SYNTHASE KINASE 3 INHIBITOR; GLYCOGEN SYNTHASE KINASE 3ALPHA; GLYCOGEN SYNTHASE KINASE 3BETA; HYMENIALDISINE; INDIRUBIN; INDIRUBIN DERIVATIVE; ISOENZYME; KENPAULLONE; LITHIUM; MALEIMIDE DERIVATIVE; MUSCARINIC AGENT; PAULLONE DERIVATIVE; THIADIAZOLE DERIVATIVE; THIADIAZOLINONE DERIVATIVE; UNCLASSIFIED DRUG; VALPROIC ACID;

CANCER; CELL FUNCTION; CHEMICAL STRUCTURE; CHRONIC INFLAMMATION; DEGENERATIVE DISEASE; DIABETES MELLITUS; ENZYME INHIBITION; ENZYME SPECIFICITY; GLYCOGEN METABOLISM; HUMAN; INFLAMMATION; MANIC DEPRESSIVE PSYCHOSIS; NERVE DEGENERATION; PROCESS OPTIMIZATION; REVIEW; STROKE; STRUCTURE ACTIVITY RELATION;

CA(2+)-CALMODULIN DEPENDENT PROTEIN KINASE; DIABETES MELLITUS; ENZYME INHIBITORS; GLYCOGEN SYNTHASE KINASE 3; GLYCOGEN SYNTHASE KINASES; HUMANS; INFLAMMATION; NEOPLASMS; NEURODEGENERATIVE DISEASES;

EID: 0036273020     PISSN: 01986325     EISSN: None     Source Type: Journal    
DOI: 10.1002/med.10011     Document Type: Review

References (81)

1. The multifaceted roles of glycogen synthase kinase 3beta in cellular signaling
2. Judging a protein by more than its name: GSK-3
3. Glycogen synthase kinase-3 is rapidly inactivated in response to insulin and phosphorylates eukaryotic initation factor eIF-2B
4. GSK3 takes centre stage more than 20 years after its discovery
5. Missing links in GSK-3 regulation
6. Molecular cloning and expression of glycogen synthase kinase-3/factor A
7. Expression analysis of glycogen synthase kinase-3 in human tissues
8. Integrin-linked kinase (ILK): A "hot" therapeutic target
9. Cyclic AMP promotes neuronal survival by phosphorylation of glycogen synthase kinase 3beta
10. Glycogen synthase kinase 3beta negatively regulates both DNA-binding and transcriptional activities of heat shock factor 1
11. The interaction between beta-catenin, GSK3beta and APC after mitogen induced cell-cell dissociation, and their involvement in signal transduction pathways in prostate cancer
12. The NF-kB activation pathway. A paradigm in information transfer from mebrane to nucleus
13. Dishevelled regulates the metabolism of amyloid precursor protein via protein kinase C/mitogen-activated protein kinase and c-Jun terminal kinase
14. Phosphorylation of tau by glycogen synthase kinase 3beta in intact mammalian cells influence the stability of microtubules
15. Glycogen synthase kinase 3-beta regulates presenilin 1 C-terminal fragment levels
16. Neurofibrillary tangles and tau phosphorylation
17. Glycogen synthase kinase 3beta as a target for anti-apoptotic signals
18. Low GSK-3 activity in frontal cortex of schizophrenic patients
19. The reanissance of GSK-3
20. Structure of GSK-3β reveals a primed phosphorylation mechanism
21. Crystal structure of glycogen synthse kinase 3beta: Structural basis for phosphate-primed substrate specificity and autoinhibition
22. The structure of phosphorylated GSK-3beta complexed with a peptide, FRATtide, that inhibits beta-catenin phosphorylation
23. Glycogen synthase kinase 3 phosphorylation of different residues in the presence of different factors: Analysis of tau protein
24. Axin, a negative regulator of the Wnt signaling pathway, forms a complex with GSK-3beta and beta-catenin and promotes GSK-3betadependent phosphorylation of beta-catenin
25. A common phosphate binding site explains the unique specificity of GSK-3 and its inactivation by phosphorylation
26. Identification of the axin and FRAT/GBP binding region of glycogen synthase kinase 3
27. GSK3, a master switch regulating cell-fate specification and tumorigenesis
28. Current therapies and emerging targets for the treatment of diabetes
29. The role of protein phosphorylation in human health and disease
30. Different expression of glycogen synthase kinase 3beta between young and old rat brains after transient middle cerebral artery occlusion
31. Inhibition of tau hyperphosphorylation: A new therapeutical strategy for the treatment of Alzheimer's disease and other neurodegenerative disorders
32. Lithium reduces tau phosphorylation by inhibition of glycogen synthase kinase-3
33. Lithium inhibits Alzheimer's disease tau protein phosphorylation in neurons
34. Lithium inhibits glycogen synthase kinase 3 activity and mimics wingless signalling in intact cells
35. A molecular mechanism for the effect of lithium on development
36. Lithium therapy and signal transduction
37. + deprivation in cerebellar granule cells
38. Lithium inhibits glycogen synthase kinase-3 by competition for magnesium
39. Lithium reduces tau phosphorylation: Effects in living cells and in neurons at therapeutic concentrations
40. Lithium protects cultured neurons against b-amyloid induced neurodegeneration
41. The mood-stabilizing agent valproate inhibits the activity of glycogen synthase kinase-3
42. Histone deacetylase is a direct target of valproic acid, a potent anticonvulsant, mood stabilizer, and teratogen
43. Bipolar disorders: Leads from the molecular and cellular mechanism of action of mood stabilizers
44. Lithium-related genetics of bipolar disorders
45. A structure-based library approach to kinase inhibitors
46. Inhibition of cyclin-dependent kinases, GSK3β and CK1 by hymenialdesine, a marine sponge constituent
47. Requirement for glycogen synthase kinase3beta in cell survival and NF-kappaB activation
48. The natural product hymenaldisine inhibits interleukin-8 production in U937 cells by inhibition of nuclear factor-κB
49. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases
50. Paullones, a series of cyclin-dependent kinase inhibitors: Synthesis, evaluation of CDK1/Cyclin B inhibition, and in vitro antitumor activity
51. Paullones are potent inhibitors of glycogen synthase kinase-3β and cyclin-dependent kinase 5/p25
52. Synthese von 7,12-Dihydro-indolo[3,2-d][1]benzazepin-6-(5H)-onen und 11-Dihydro-thieno-[3′,2′:2,3]azepino[4,5-b]-indol-5(4H)-on
53. Anti-mitotic properties of indirubin-3′monoxime, a CDK/GSK-3 inhibitor: Induction of endoreplication following prophase arrest
54. Indirubin, the active constituent of a chinese antileukaemia medicine, inhibits cyclin-dependent kinases
55. Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors?
56. Phosphorylation of human tau protein by microtubuleassociated kinases: GSK-3beta and cdk5 are key participants
57. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen kinase-3 activity
58. Inhibition of voltage-dependent sodium channels by Ro 31-8220, a "specific" protein kinase C inhibitor
59. 3-Anilino-4-arylmaleimides: Potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3)
60. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription
61. Inhibition of GSK-3 selectively reduces glucose-6-phosphatase and phosphoenolpyruvate carboxykinase gene expression
62. Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death
63. GSK-3 inhibition by adenoviral FRAT1 over-expression is neuroprotective and induces Tau dephosphorylation and β-catetin stabilisation without elevation of glycogen synthase activity
64. Therapeutic strategies in Alzheimer's disease: M1 muscarinic agonists
65. Muscarinic agonist reduce tau phosphorylation in non-neuronal cells via GSK-3beta inhibition and in neurons
66. M1 muscarinic agonists as potential disease-modifying agents in Alzheimer's disease. Rationale and perspectives
67. Firts non-ATP competitive glycogen synthase kinase 3beta (GSK-3β) inhibitors: Thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease
68. Arylimino-1,2,4-thiadiazolidinones: A new family of potassium channel openers
69. Synthesis and potential muscarinic receptor binding and antioxidant properties of 3-(thiadiazolyl)pyridine 1-oxide compounds
70. N-Benzylpiperidine derivatives of 1,2,4-thiadiazolidinone as new acetylcholinesterase inhibitors
71. Chlorination of isothiocyanates. III. N-Aryl and N-Alkyl-S-chloroisothiocarbamoyl chlorides with isocyantes. Synthesis of 1,2,4-thiadiazolidine-3,5 -diones
72. Non-cholinergic pharmacotherapy to the future treatment of Alzheimer's disease
73. Identification of sequence variants and analysis of the role of the glycogen synthase kinase 3 beta gene and promoter in late onset Alzheimer's disease
74. Molecular cloning and characterization of the human glycogen synthase kinase-3beta promoter
75. The molecular bases of Alzheimer's disease and other neurodegenerative disorders
76. Glycogen synthase kinase 3β is a negative regulator of cardiomyocyte hypertrophy
77. Wnt signaling and cancer