Emerging targets for diabetes

Current Science

Volumn 88, Issue 2, 2005, Pages 241-249

  Vats, Rakesh Kumar ^a   Kumar, Vivek ^a   Kothari, Abhishek ^a   Mital, Alka ^a   Ramachandran, Uma ^a  

^a NATIONAL INSTITUTE OF PHARMACEUTICAL EDUCATION AND RESEARCH NIPER   (India)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 20444369561     PISSN: 00113891     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (76)

1. Joe, M. C. and Arshag, D. M., A rational approach to drug therapy of type 2 diabetes mellitus. Drugs, 2000, 60, 95-113.
2. Moller, D. E., New drug targets for type 2 diabetes and metabolic syndrome. Nature, 2001, 414, 821.
3. www.who.int, 2001.
4. Taylor, S. I., Accili, D. and Imai, Y., Insulin resistance or insulin deficiency, which is the primary cause of NIDDM? Diabetes, 1994, 43, 735-747.
5. Ramarao, P. and Kaul, C. L., Insulin resistance: Current therapeutic approaches. Drugs Today, 1999, 35, 895-911.
6. Mollar, N., Novel targets and therapeutic strategies for type-2 diabetes. Trends Endocrinol. Metab., 2003, 14, 169-175.
7. Wagman, A. S. and Nuss, J. M., Current therapies and emerging targets for treatment of diabetes. Curr. Pharm. Des., 2001, 7, 417-450.
8. Chakrabarti, R. et al., Antidiabetic and hypolipidemic potential of DRF-2519 a dual activator of PPARα and PPARγ. Eur. J. Pharmacol., 2004, 491, 195-206.
9. Sauerberg, P. et al., Novel tricyclic-α-alkoxy phenylpropionic acids: Dual PPARα/γ agonists with hypolipidemic and antidiabetic activity. J. Med. Chem., 2002, 45, 789-804.
10. Ramachandran, U. et al., Tricyclic compounds having antioxidant properties. WTO Indian Patent DEL/1268, 2003.
11. Leung, C. et al., The difluoromethylenesulfonic acid group as a monoanionic phosphate surrogate for obtaining PTP-1B inhibitors. Bioorg. Med. Chem., 2002, 10, 2309-2323.
12. Zhang, Z. Y., Protein tyrosine phosphatases: prospects for therapeutics. Curr. Opin. Chem. Biol., 2001, 5, 416-423.
13. Ockey, D. A. and Gadek, T. R., Discovery of novel PTP-1B inhibitors. Bioorg. Med. Chem. Lett., 2004, 14, 389-391.
14. Johnson, T. O., Ermolieff, J. and Jirousek, M. R., Protein tyrosine phosphatase-1B inhibitors for diabetes. Nature Rev. Drug Discov., 2002, 1, 696-709.
15. Tonks, N. K., PTP-1B: From the sidelines to the front lines. FEBS Lett., 2003, 546, 140-148.
16. Pei, Z. et al., Discovery and SAR of novel, potent and selective protein tyrosine phosphatase-1B inhibitors. Bioorg. Med. Chem. Lett., 2003, 13, 3129-3132.
17. Huijsduijnen, V. R. H., Bombrun, A. and Swinnen, D., Selecting protein tyrosine phosphatases as drug targets. Drug Discovery Today, 2002, 7, 1013-1019.
18. Ahn, J. H. et al., Synthesis and PTP-1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents. Bioorg. Med. Chem. Lett., 2002, 12, 1941-1946.
19. Liljebris, C. et al., Synthesis and biological activity of a novel class of pyridazine analogues as non-competitive reversible inhibitors of protein tyrosine phosphatase-1B (PTP-1B). Bioorg. Med. Chem., 2002, 10, 3197-3212.
20. Hum, G., Lee, J. and Taylor, S. D., Synthesis of [difluoro-(3- alkenylphenyl)-methyl]-phosphonic acids on non-crosslinked polystyrene and their evaluation as inhibitors of PTP-1B. Bioorg. Med. Chem. Lett., 2002, 12, 3471-3474.
21. Shim, Y. S., Kim, K. C., Chi, D. Y., Lee, K. H. and Cho, H., Formylchromone derivatives as a novel class of protein tyrosine phosphatase-1B inhibitors. Bioorg. Med. Chem. Lett., 2003, 13, 2561-2563.
22. Xin, Z. et al., Potent, selective inhibitors of protein tyrosine phosphatase-1B. Bioorg. Med. Chem. Lett., 2003, 13, 1887-1890.
23. Gao, Y. et al., Utilization of a peptide lead for the discovery of a novel PTP-1B binding motif. J. Med. Chem., 2001, 44, 2869-2878.
24. Leung, C. et al., The difluoromethylenesulfonic acid group as a monoanionic phosphate surrogate for obtaining PTP-1B inhibitors. Bioorg. Med. Chem., 2002, 10, 2309-2323.
25. Burke, J. et al., Enantioselective synthesis of nonphosphorus-containing phosphotyrosyl mimetics and their use in the preparation of tyrosine phosphatase inhibitory peptides. Tetrahedron, 1998, 54, 9981-9994.
26. Gao, Y., Wu, L., Luo, J. H., Guo, R., Yang, D., Zhang, Z. Y. and Burke Jr., T. R., Examination of novel non-phosphorus containing phosphotyrosyl mimetics against protein-tyrosine phosphatase-1B and demonstration of differential affinities toward Grb2 SH2 domains. Bioorg. Med. Chem. Lett., 2000, 10, 923-927.
27. Larsen, S. D. et al., Modification of the N-terminus of peptidomimetic protein tyrosine phosphatase-1B (PTP-1B) inhibitors: identification of analogues with cellular activity. Bioorg. Med. Chem. Lett., 2003, 13, 971-975.
28. Chen, Y. T., Xie, J. and Seto, C. T., Peptidic alpha-ketocarboxylic acids and sulfonamides as inhibitors of protein tyrosine phosphatases. J. Org. Chem., 2003, 68, 4123-4125.
29. Arabaci, G., Yi, T., Fu, H., Porter, M. E., Beebe, K. D. and Pei, D., Alpha-bromoacetophenone derivatives as neutral protein tyrosine phosphatase inhibitors: Structure-activity relationship. Bioorg. Med. Chem. Lett., 2002, 12, 3047-3050.
30. Finkelman, H. E., Glycogen synthase kinase-3: An emerging therapeutic target. Trends Mol. Med., 2002, 8, 126-129.
31. Frame, S. and Cohen, P., GSK-3 takes centre stage more than 20 years after its discovery. Biochem. J., 2001, 359, 1-16.
32. Ali, A., Hoeflich, K. P. and Woodgett, J. R., Glycogen synthase kinase-3: Properties, functions and regulation. Chem. Rev., 2001, 101, 2527-2540.
33. Jope, R. S. and Johnson, G. V. W., The glamour and gloom of glycogen synthase kinase 3. Trends Biochem. Sci., 2004, 29, 95-102.
34. Darren, A. E., Cross, D. R., Cohen, P., Andjelkovich, M. and Brian, A. H., Inhibition of glycogen synthase kinase-3 by insulin mediated by protein kinase B. Nature, 1995, 378, 785-789.
35. Svetlana, E., Nikoulina, T. P., Mudaliar, S., Mohideen, P., Carter, L. and Henry, R. R., Potential role of glycogen synthase kinase-3 in skeletal muscle insulin resistance of type 2 diabetes. Diabetes, 2000, 49, 263-271.
36. Grimes, C. A. and Jope, R. S., The multifaceted roles of glycogen synthase kinase-3b in cellular signaling. Prog. Neurobiol., 2001, 65, 391-426.
37. Ciarald, T. P., Nikoulina, S. E. and Henry, R. R., Role of glycogen synthase kinase-3 in skeletal muscle insulin resistance in type-2 diabetes. J. Diabetes Complication, 2002, 16, 69-71.
38. Zhang, B. B., Insulin signaling and action: Glucose, lipids, protein. 2002, www.endotext.com
39. Plotkin, B., Insulin mimetic action of synthetic phosphorylated peptide inhibitors of glycogen synthase kinase-3. J. Pharmacol. Exp. Ther., 2003, 305, 974-980.
40. Ring, D. B., Johnson, K. W., Henriksen, E. J., Nuss, J. M., Goff, D., Kinnick, T. R. and Harrison, S. D., Selective glycogen synthase kinase-3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes, 2003, 52, 588-595.
41. Svetlana, E., Nicoulina, T. P. C., Mudaliar, S., Carter, L., Johnson, K. and Henry, R. R., Inhibition of glycogen synthase kinase-3 improves insulin action and glucose metabolism in human skeletal muscle. Diabetes, 2002, 51, 2190-2198.
42. Wauwe, J. V. and Haefner, B., Glycogen synthase kinase-3 as drug target: From wallflower to center of attention. Drug News Perspect., 2003, 16, 557-565.
43. Ryves, W. J. and Harwood, A. J., Lithium inhibits glycogen synthase kinase-3 by competition for magnesium. Biochem. Biophys. Res. Commun., 2001, 280, 720-725.
44. Zhang, F., Christopher, J. P., Laura, S., Nadia, G. and Klein, P. S., Inhibitory phosphorylation of glycogen synthase kinase-3 (GSK-3) in response to lithium. J. Biol. Chem., 2003, 278, 33067-33077.
45. Kunick, C., Lauenroth, C., Wieking, K., Schultz, C., Lemcke, T. and Flemming, S. J., Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5 and GSK-3 inhibition by paullones. J. Med. Chem., 2004, 47, 22-36.
46. Kunick, C., Lauenroth, C., Leost, M., Meijer, L. and Lemcke, T., 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3β. Bioorg. Med. Chem. Lett., 2004, 14, 413-416.
47. Meijer, L., Skaltsounis, A., Magiatis, P. and Knockaert, M., GSK-3 selective inhibitors derived from tyrian purple indirubins. Chem. Biol., 2003, 10, 1255-1266.
48. Smith, D. G., Buffet, M., Ashley, E. F., Haigh, D., Ife, R. J. and Ward, R. W., Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3. Bioorg. Med. Chem. Lett., 2003, 13, 3049-3053.
49. Smith, D. G., Buffet, M., Ashley, E. F., Haigh, D., Ife, R. J. and Ward, R. W., 3-Anilino-4-arylmaleimides: Potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3). Bioorg. Med. Chem. Lett., 2001, 11, 635-639.
50. Gee-Hong, K., Prouty, C., Angelis, A. D., Shen, L., ONeill, D. J., Shah, C. and Jolliffe, L., Synthesis and discovery of macrocyclic polyoxygenatebis-7- azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3β inhibitors. J. Med. Chem., 2003, 46, 4021-4031.
51. Shen, L., Prouty, C., Conway, B. R., Jun, Z. X. and Gee-Hong, K., Synthesis and biological evaluation of novel macrocyclic bis-7- azaindolylmaleimides as potent and highly selective glycogen synthase kinase-3β (GSK-3β) inhibitors. Bioorg. Med. Chem., 2004, 12, 1-17.
52. Zhang, H. C., Ye, H., Conway, B. R., Derian, C. K. and Maryanoff, B. C., 3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3. Bioorg. Med. Chem. Lett., 2004, 14, 3245-3250.
53. Witherington, J., Bordas, V., Garland, S. L., Deirdre, M. B. and Smith, D. J., 5-Aryl-pyrazolo[3,4-b]pyridines: Potent inhibitors of glycogen synthase kinase-3 (GSK-3). Bioorg. Med. Chem. Lett., 2003, 13, 1577-1580.
54. Witherington, J., Bordas, V., Garland, S. L., Deirdre, M. B. and Smith, D. J., 5-Aryl-pyrazolo[3,4-b]pyridazines: Potent inhibitors of glycogen synthase kinase-3 (GSK-3). Bioorg. Med. Chem. Lett., 2003, 13, 1581-1584.
55. Witherington, J., Bordas, V., Garland, S. L., Deirdre, M. B. and Smith, D. J., 6-Aryl-pyrazolo[3,4-b]pyridines: Potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3). Bioorg. Med. Chem. Lett., 2003, 13, 3055-3057.
56. Witherington, J., Bordas, V., Garland, S. L., Deirdre, M. B. and Smith, D. J., 6-Heteroaryl-pyrazolo[3,4-b]pyridines: Potent and selective inhibitors of glycogen synthase kinase (GSK-3). Bioorg. Med. Chem. Lett., 2003, 13, 3059-3062.
57. Smith, D. G. and Ward, R. W., Diamino-1,2,4-triazole-carboxylic acid and derivatives as GSK-3 inhibitors. 2001, WO 01/009106.
58. Saady, M. Y. P., Lochead, A. and Marguerie, S., 1-(Alkyl),1-(hetroaryl) alkyl and 1-(arylalkyl)-7 pyridine-4yl-imidazole(1,2a) pyrimidine-5(1H)-one derivatives. 2002, WO 02/018385.
59. Li, A. T., Nedelec, A. and Gallet, T., 2-Pyridinyl-6,7,8,9- tetrahydropyrimido[1,2-a]pyrimidine-4-one and 7-pyridinyl-2,3 dihydro imidazolo[1,2-a]pyrimidine-5(1H)-one derivatives. 2002, WO 02/018386.
60. Peat, A. J. et al., Novel pyrazolopyrimidine derivatives as GSK-3 inhibitors. Bioorg. Med. Chem. Lett., 2004, 14, 2121-2125.
61. Peat, A. J. et al. Novel GSK-3 inhibitors with improved cellular activity. Bioorg. Med. Chem. Lett., 2004, 14, 2127-2130.
62. Bowler, A. N., Kilburn, J. P., Engelhardt, S., Danielsen, G. M. and Kurthzals, P., Oxadiazepines with glucose lowering properties. 16th Int. Symp. Med. Chem., 2000, www.google.com
63. Olesen, P., Kurthzhals, P., Worsaee, H., Hansen, B. F., Sorensen A. I. and Bowler, A. N., Synthesis and in vitro characterization of 1-(4-aminofurazan-3-yl)-5-dialkylamino methyl-1H-[1,2,3]triazole-4-carboxylic acid derivatives. J. Med. Chem., 2003, 46, 3333-3341.
64. Olesen, P., Kurthzhals, P., Worsaee, H., Hansen, B. F., Sorensen, A. I. and Bowler, A. N., Furazanyl-triazole derivatives for the treatment of diseases. 2002, WO 02/032896.
65. Sorensen, A. R., Worsaae, H., Hansen, B. F., Kurthzhals, P., Bowler, A. N. and Olesen P. H., 2,4-Diaminothizole derivatives and their use as glycogen synthase kinase-3 (GSK-3) inhibitors. 2001, WO 01/056567.
66. Bowler, A. N. and Hansen, B. F., 2,4-Diaminothiazole derivatives and their use as glycogen synthase kinase-3 (GSK-3) inhibitors. 2003, WO 03/011843.
67. Cochran, J., Nanthakumar, J., Harrigton, E. and Wang, J., Thiazole derivatives useful as inhibitors of protein kinases. 2002, WO 02/096905.
68. Moon, Y. C., Green, J., Davies, R., Choquette, D., Pierce, A. and Ledeboer, M., 5-(2-aminopyrimidine-4-yl) benzisoxazoles as protein kinase inhibitors. 2002, WO 02/102800.
69. Green, J., Arnost, M. J. and Pierce, A., Pyrazolone derivatives as inhibitors of GSK-3. 2003, WO 03/011287.
70. Savithri, R. and Nuss, J., Pyrazine based inhibitors of glycogen synthase kinase-3. 2001, WO 01/044206.
71. Desai, M., Ramurthy, S., Nuss, J. M. and Boyce, R., Pyrimidine based inhibitors of GSK-3. 2002, WO 02/020495.
72. Ramurthy, S., Goff, D. and Nuss, J. M., Inhibitors of glycogen synthase kinase-3. 1999, WO 99/065897.
73. Cline, G. W. et al., Effects of novel glycogen synthase kinase-3 inhibitors on insulin stimulated glucose metabolism in zucker diabetic fatty(fa/fa) rats. Diabetes, 2002, 51, 2903-2910.
74. UK Prospective Diabetes Study Group, Intensive blood glucose control with sulphonyl ureas or insulin compared with conventional treatment and risk complications in patients with type 2 diabetes. Lancet, 1998, 352, 837-853.
75. Burge, M. R., Sood, V., Sobhy, T. A., Rassam, A. G. and Schade, D. S., Sulphonyl urea induced hypoglycemia in type 2 diabetes mellitus. Diabetes Obesity Metab., 1999, 1, 199-206.
76. Amos, A. F., McCarty, D. J. and Zimmet, P., The rising global burden of diabetes and its complications: estimates and projections to the year 2010. Diabetes Med. (Suppl.), 1997, 14, S1-85.