Pharmacological inhibitors of glycogen synthase kinase 3

Trends in Pharmacological Sciences

Volumn 25, Issue 9, 2004, Pages 471-480

  Meijer, Laurent ^a,b   Flajolet, Marc ^a   Greengard, Paul ^a  

^a ROCKEFELLER UNIVERSITY   (United States)

^b STATION BIOLOGIQUE   (France)

Author keywords

[No Author keywords available]

Indexed keywords

2 (2,4 DICHLOROPHENYL) 3 (1 METHYL 3 INDOLYL)MALEIMIDE; 2 (3 CHLORO 4 HYDROXYANILINO) 3 (2 NITROPHENYL)MALEIMIDE; 2 (3 CHLOROANILINO) 4 [2 (3 HYDROXYPROPYLAMINO) 4 PYRIDYL]PYRIMIDINE; 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; 6 BROMOINDIRUBIN 3' ACETOXIME; 6 BROMOINDIRUBIN 3' OXIME; ALOISINE A; ALOISINE B; ALSTERPAULLONE; AMINOPYRIDINE DERIVATIVE; ARA 014418; AZAKENPAULLONE; BERYLLIUM; BISINDOLYLMALEIMIDE; CHIR 98014; CHIR 99021; CT 20026; CT 99021; FLAVOPIRIDOL; GLYCOGEN SYNTHASE KINASE 3; GLYCOGEN SYNTHASE KINASE 3 INHIBITOR; HYMENIALDISINE; INDIRUBIN 3' OXIME; KENPAULLONE; LITHIUM; PHOSPHOTRANSFERASE INHIBITOR; PYRAZOLOPYRIDINE 18; PYRAZOLOPYRIDINE 34; PYRAZOLOPYRIDINE 9; PYRAZOLOPYRIMIDINE DERIVATIVE; PYRIDINE DERIVATIVE; STAUROSPORINE; SU 9516; TWS 119; UNCLASSIFIED DRUG; UNINDEXED DRUG; ZINC;

BIPOLAR DISORDER; CANCER; COLORECTAL CANCER; DRUG ACTIVITY; DRUG MECHANISM; DRUG STRUCTURE; HUMAN; HUNTINGTON CHOREA; NEUROLOGIC DISEASE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PARKINSON DISEASE; PRION DISEASE; PRIORITY JOURNAL; PROTEIN EXPRESSION; REGENERATION; REVIEW; STEM CELL;

ANIMALS; CELL DIFFERENTIATION; DIABETES MELLITUS, TYPE 2; ENZYME INHIBITORS; GLYCOGEN SYNTHASE KINASE 3; HUMANS; NEOPLASMS; NERVOUS SYSTEM DISEASES; PARASITIC DISEASES; SIGNAL TRANSDUCTION; STEM CELLS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 4344619713     PISSN: 01656147     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.tips.2004.07.006     Document Type: Review

References (91)

1. P. Cohen Protein kinases - the major drug targets of the twenty-first century? Nat. Rev. Drug Discov. 1 2002 309 315
2. M.E. Noble Protein kinase inhibitors: insights into drug design from structure Science 303 2004 1800 1805
3. S. Frame, and P. Cohen GSK3 takes centre stage more than 20 years after its discovery Biochem. J. 359 2001 1 16
4. B.W. Doble, and J.R. Woodgett GSK-3: tricks of the trade for a multi-tasking kinase J. Cell Sci. 116 2003 1175 1186
5. R.S. Jope, and G.V.W. Johnson The glamour and gloom of glycogen synthase kinase-3 Trends Biochem. Sci. 29 2004 95 102
6. R. Dajani Crystal structure of glycogen synthase kinase 3β: structural basis for phosphate-primed substrate specificity and autoinhibition Cell 105 2001 721 732
7. E. ter Haar Structure of GSK3β reveals a primed phosphorylation mechanism Nat. Struct. Biol. 8 2001 593 596
8. P.S. Klein, and D.A. Melton A molecular mechanism for the effect of lithium on development Proc. Natl. Acad. Sci. U. S. A. 93 1996 8455 8459
9. C.J. Phiel, and P.S. Klein Molecular targets of lithium action Annu. Rev. Pharmacol. Toxicol. 41 2001 789 813
10. R.S. Jope Lithium and GSK-3: one inhibitor, two inhibitory actions, multiple outcomes Trends Pharmacol. Sci. 24 2003 441 443
11. A. Martinez Glycogen synthase kinase 3 (GSK-3) inhibitors as new promising drugs for diabetes, neurodegeneration, cancer, and inflammation Med. Res. Rev. 22 2002 373 384
12. H. Eldar-Finkelman, and R. Ilouz Challenges and opportunities with glycogen synthase kinase-3 inhibitors for insulin resistance and type 2 diabetes treatment Expert Opin. Investig. Drugs 12 2003 1 9
13. J. Van Wauwe, and B. Haefner Glycogen synthase kinase-3 as drug target: from wallflower to center of attention Drug News Perspect. 16 2003 557 565
14. A.S. Wagman Discovery and development of GSK3 inhibitors for the treatment of Type 2 diabetes Curr. Pharmacol. Des. 10 2004 1105 1137
15. P. Cohen, and M. Goedert GSK3 inhibitors: development and therapeutic potential Nat. Rev. Drug Discov. 3 2004 479 487
16. A. Martinez First non-ATP competitive glycogen synthase kinase 3β (GSK-3β) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease J. Med. Chem. 45 2002 1292 1299
17. S. Conde Thienyl and phenyl alpha-halomethyl ketones: new inhibitors of glycogen synthase kinase (GSK-3β) from a library of compound searching J. Med. Chem. 46 2003 4631 4633
18. J.A. Bertrand Structural characterization of the GSK-3β active site using selective and non-selective ATP-mimetic inhibitors J. Mol. Biol. 333 2003 393 407
19. R. Bhat Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418 J. Biol. Chem. 278 2003 45937 45945
20. L. Meijer GSK-3 selective inhibitors derived from Tyrian purple indirubins Chem. Biol. 10 2003 1255 1266
21. P. Polychronopoulos Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase -3 and cyclin-dependent kinases J. Med. Chem. 47 2004 935 946
22. J. Witherington 5-Aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3) Bioorg. Med. Chem. Lett. 13 2003 1581 1584
23. P.M. Fischer CDK versus GSK-3 inhibition: a purple haze no longer? Chem. Biol. 10 2003 1144 1146
24. M. Knockaert Pharmacological inhibitors of cyclin-dependent kinases Trends Pharmacol. Sci. 23 2002 417 425
25. L.T. Vassilev In vivo activation of the p53 pathway by small-molecule antagonists of MDM2 Science 303 2004 844 848
26. R. Dajani Structural basis for recruitment of glycogen synthase kinase 3beta to the axin-APC scaffold complex EMBO J. 22 2003 494 501
27. M. Fujimuro A novel viral mechanism for dysregulation of beta-catenin in Kaposi's sarcoma-associated herpesvirus latency Nat. Med. 9 2003 300 306
28. S.P. Davies Specificity and mechanism of action of some commonly used protein kinase inhibitors Biochem. J. 351 2000 95 105
29. J. Bain The specificities of protein kinase inhibitors: an update Biochem. J. 371 2003 199 204
30. M. Knockaert Intracellular targets of paullones. Identification following affinity purification on immobilized inhibitor J. Biol. Chem. 277 2002 25493 25501
31. T.D. Gould Glycogen synthase kinase-3: a target for novel bipolar disorder treatments J. Clin. Psychiatry 65 2004 10 21
32. M. Leost Paullones are potent inhibitors of glycogen synthase kinase-3β and cyclin-dependent kinase 5/p25 Eur. J. Biochem. 267 2000 5983 5994
33. S. Leclerc Indirubins inhibit glycogen synthase kinase-3β and CDK5/p25, two kinases involved in abnormal tau phosphorylation in Alzheimer's disease - A property common to most CDK inhibitors? J. Biol. Chem. 276 2001 251 260
34. B. De Strooper, and J. Woodgett Alzheimer's disease: Mental plaque removal Nature 423 2003 392 393
35. J. Ryder Akt/GSK3β serine/threonine kinases: evidence for a signaling pathway mediated by familial Alzheimer's disease mutations Cell. Signal. 16 2004 187 200
36. C.J. Phiel GSK-3alpha regulates production of Alzheimer's disease amyloid-beta peptides Nature 423 2003 435 439
37. J.J. Lucas Decreased nuclear beta-catenin, tau hyperphosphorylation and neurodegeneration in GSK-3beta conditional transgenic mice EMBO J. 20 2001 27 39
38. G.R. Jackson Human wild-type tau interacts with wingless pathway components and produces neurofibrillary pathology in Drosophila Neuron 34 2002 509 519
39. W. Noble Cdk5 is a key factor in tau aggregation and tangle formation in vivo Neuron 38 2003 555 565
40. R.V. Bhat Regulation and localization of tyrosine216 phosphorylation of glycogen synthase kinase-3beta in cellular and animal models of neuronal degeneration Proc. Natl. Acad. Sci. U. S. A. 97 2000 11074 11079
41. J. Wang Cdk5 activation induces hippocampal CA1 cell death by directly phosphorylating NMDA receptors Nat. Neurosci. 6 2003 1039 1047
42. S. Nonaka, and D.M. Chuang Neuroprotective effects of chronic lithium on focal cerebral ischemia in rats NeuroReport 9 1998 2081 2084
43. M. Ren Postinsult treatment with lithium reduces brain damage and facilitates neurological recovery in a rat ischemia/reperfusion model Proc. Natl. Acad. Sci. U. S. A. 100 2003 6210 6215
44. T.D. King Caspase-3 activation induced by inhibition of mitochondrial complex I is facilitated by glycogen synthase kinase-3β and attenuated by lithium Brain Res. 919 2001 106 114
45. P.D. Smith Cyclin-dependent kinase 5 is a mediator of dopaminergic neuron loss in a mouse model of Parkinson's disease Proc. Natl. Acad. Sci. U. S. A. 100 2003 13650 13655
46. J. Carmichael GSK-3β inhibitors prevent cellular polyglutamine toxicity caused by the Huntington's disease mutation J. Biol. Chem. 277 2002 33791 33798
47. M. Perez Prion petide induces neuronal cell death through a pathway involving glycogen synthase kinase 3 Biochem. J. 372 2003 129 136
48. E.S. Emamian Convergent evidence for impaired AKT1-GSK3β signaling in schizophrenia Nat. Genet. 36 2004 131 137
49. J.M. Beaulieu Lithium antagonizes dopamine-dependent behaviors mediated by an AKT/glycogen synthase kinase 3 signaling cascade Proc. Natl. Acad. Sci. U. S. A. 101 2004 5099 5104
50. E. Iwahana Effect of lithium on the circadian rhythms of locomotor activity and glycogen synthase kinase-3 protein expression in the mouse suprachiasmatic nuclei Eur. J. Neurosci. 19 2004 2281 2287
51. E. Harms CK1 and GSK3 in the Drosophila and mammalian circadian clock Novartis Found. Symp. 253 2003 267 277
52. B. Plotkin Insulin mimetic action of synthetic phosphorylated peptide inhibitors of glycogen synthase kinase-3 J. Pharmacol. Exp. Ther. 305 2003 974 980
53. M.P. Coghlan Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription Chem. Biol. 7 2000 793 803
54. D.B. Ring Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo Diabetes 52 2003 588 595
55. S.E. Nikoulina Inhibition of glycogen synthase kinase 3 improves insulin action and glucose metabolism in human skeletal muscle Diabetes 51 2002 2190 2198
56. K. MacAulay Use of lithium and SB-415286 to explore the role of glycogen synthase kinase-3 in the regulation of glucose transport and glycogen synthase Eur. J. Biochem. 270 2003 3829 3838
57. E.J. Henriksen Modulation of insulin resistance by selective inhibition of GSK-3 in Zucker diabetic fatty rats Am. J. Physiol. Endocrinol. Metab. 284 2003 E892 E900
58. G.W. Cline Effects of a novel glycogen synthase kinase 3 inhibitor on insulin-stimulated glucose metabolism in Zucker diabetic fatty (fa/fa) rats Diabetes 51 2002 2903 2910
59. M. Ubeda Glucose-induced expression of the CDK5 activator p35 involved in Alzheimer's disease regulates insulin gene transcription in pancreatic β-cells Endocrinology 145 2004 3023 3031
60. B. Lustig, and J. Behrens The Wnt signalling pathway and its role in tumor development J. Cancer Res. Clin. Oncol. 129 2003 199 221
61. Y. Cohen Cancer morbidity in psychiatric patients: influence of lithium carbonate treatment Med. Oncol. 15 1998 32 36
62. T.D. Gould Effects of glycogen synthase kinase-3 inhibitor, lithium, in adenomatous polyposis coli mutant mice Pharmacol. Res. 48 2003 49 53
63. X. Liao Glycogen synthase kinase-3β suppression eliminates tumor necrosis factor-related apoptosis-inducing ligand resistance in prostate cancer Mol. Cancer Ther. 2 2003 1215 1222
64. J.G. Wakefield A role for glycogen synthase kinase-3 in mitotic spindle dynamics and chromosome alignment J. Cell Sci. 116 2003 637 646
65. S. Ding Synthetic small molecules that control stem cell fate Proc. Natl. Acad. Sci. U. S. A. 100 2003 7632 7637
66. N. Sato Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3 specific inhibitor Nat. Med. 10 2004 55 63
67. E. Droucheau Plasmodium falciparum glycogen synthase kinase-3, molecular model, expression, intracellular localisation and selective inhibitors Biochim. Biophys. Acta 1697 2004 181 196
68. L. Meijer Inhibition of cyclin-dependent kinases, GSK-3β and casein kinase 1 by hymenialdisine, a marine sponge constituent Chem. Biol. 7 2000 51 63
69. C. Kunick 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3β Bioorg. Med. Chem. Lett. 14 2004 413 416
70. Y. Mettey Aloïsines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects J. Med. Chem. 46 2003 222 236
71. L. Naerum Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors Bioorg. Med. Chem. Lett. 12 2002 1525 1528
72. J. Witherington 5-Aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3) Bioorg. Med. Chem. Lett. 13 2003 1577 1580
73. J. Witherington 6-Aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3) Bioorg. Med. Chem. Lett. 13 2003 3055 3057
74. J. Witherington 6-Heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3) Bioorg. Med. Chem. Lett. 13 2003 3059 3062
75. M.A. Ortega Pyrazolo[3,4-b]quinoxalines. a new class of cyclin-dependent kinases inhibitors Bioorg. Med. Chem. 10 2002 2177 2184
76. M.E. Lane A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells Cancer Res. 61 2001 6170 6177
77. H.C. Zhang Macrocyclic bisindolymaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3 Bioorg. Med. Chem. Lett. 13 2003 3049 3053
78. G-H. Kuo Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3β inhibitors J. Med. Chem. 46 2003 4021 4031
79. L. Shen Synthesis and biological evaluation of novel macrocyclic bis-7-azaindolylmaleimides as potent and highly selective glycogen synthase kinase-3 beta (GSK-3 beta) inhibitors Bioorg. Med. Chem. 12 2004 1239 1255
80. I. Hers The protein kinase C inhibitors bisindolylmaleimide I (GF 109203X) and IX (Ro 31-8220) are potent inhibitors of glycogen kinase-3 activity FEBS Lett. 460 1999 433 436
81. D.G. Smith 3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3) Bioorg. Med. Chem. Lett. 11 2001 635 639
82. S. Ruetz Ruetz Chemical and biological profile of dual cdk1 and cdk2 Inhibitors Curr. Med. Chem. Anti-Canc. Agents 3 2003 1 14
83. P.H. Olesen Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylaminomethyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. A new class of selective GSK-3 inhibitors J. Med. Chem. 46 2003 3333 3341
84. A.J. Peat Novel GSK-3 inhibitors with improved cellular activity Bioorg. Med. Chem. Lett. 14 2004 2127 2130
85. R. Ilouz Inhibition of glycogen synthase kinase-3β by bivalent zinc ions: insight into the insulin-mimetic action of zinc Biochim. Biophys. Res. Commun. 295 2002 102 106
86. C. Yost GBP, an inhibitor of GSK-3, is implicated in Xenopus development and oncogenesis Cell 93 1998 1031 1041
87. A.A. Culbert GSK-3 inhibition by adenoviral FRAT1 overexpression is neuroprotective and induces Tau dephosphorylation and β-catenin stabilisation without elevation of glycogen synthase activity FEBS Lett. 507 2001 288 294
88. G.M. Thomas A GSK3-binding peptide from FRAT1 selectively inhibits the GSK3-catalysed phosphorylation of axin and beta-catenin FEBS Lett. 458 1999 247 251
89. C.P. Martin P24, a glycogen synthase kinase (GSK 3) inhibitor Biochim. Biophys. Acta 1586 2002 113 122
90. J-Y. Yu Simultaneous inhibition of GSK3α and GSK3β using hairpin siRNA expression vectors Mol. Ther. 7 2003 228 236
91. F. Zhang Inhibitory phosphorylation of glycogen synthase kinase-3 (GSK-3) in response to lithium: evidence for autoregulation of GSK-3 J. Biol. Chem. 278 2003 33067 33077