Glycogen phosphorylase inhibitors for treatment of type 2 diabetes mellitus

Expert Opinion on Investigational Drugs

Volumn 10, Issue 3, 2001, Pages 439-454

  Treadway, J L ^a   Mendys, P ^a   Hoover, D J ^a  

^a PFIZER INC   (United States)

Author keywords

Antihyperglycaemic; Blood glucose; Diabetic animal models; Diabetic complications; Drug discovery; Enzyme; Gluconeogenesis; Glycogen phosphorylase inhibitor; Glycogenolysis; Hepatic glucose production; Indole inhibitor site; Myocardial infarction; Obesity; Oral hypoglycaemic agents; Stroke; Type 2 diabetes mellitus therapy

Indexed keywords

1,4 DIDEOXY 1,4 IMINOARABINITOL; 2 HYDROXYMETHYL 3,4 PYRROLIDINEDIOL; ADENOSINE PHOSPHATE; ALPHA GLUCOSIDASE; ANTIDIABETIC AGENT; BAY W 1807; BAYR 3401; CAFFEINE; CP 320626; CP 403700; CP 526423; CP 91 149; FLAVINE MONONUCLEOTIDE; FLAVOPIRIDOL; GLUCOSE; GLUCOSE 6 PHOSPHATASE; GLYCOGEN; GLYCOGEN PHOSPHORYLASE; GLYCOGEN PHOSPHORYLASE INHIBITOR; GLYCOGEN SYNTHASE; INSULIN; ISOFAGOMINE; LACTIC ACID; METFORMIN; PIOGLITAZONE; PURINE NUCLEOSIDE; ROSIGLITAZONE; SPIROHYDANTOIN; TROGLITAZONE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; CATALYSIS; CONTROLLED STUDY; DOSE RESPONSE; DRUG MECHANISM; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG TARGETING; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME BINDING; ENZYME INHIBITION; GLUCONEOGENESIS; GLUCOSE BLOOD LEVEL; GLYCOGENOLYSIS; HEART PROTECTION; HUMAN; HYPOGLYCEMIA; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PROTEIN PHOSPHORYLATION; RAT; REVIEW; STRUCTURE ACTIVITY RELATION;

ANIMALS; DIABETES MELLITUS, TYPE 2; ENZYME INHIBITORS; HUMANS; PHOSPHORYLASES;

EID: 0035110957     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543784.10.3.439     Document Type: Review

References (84)

1. Reducing the burden of diabetes: Managing cardiovascular disease
2. Cardiovascular risk profile in individuals with borderline glycemia: The effect of the 1997 American Diabetes Association diagnostic criteria and the 1998 World Health Organization Provisional Report
3. The effect of glycemic control on the incidence of macrovascular complications of Type 2 diabetes
4. Glycemic control and cardiovascular disease in type 2 diabetes: A review
5. Promoting early diagnosis and treatment of type 2 diabetes: The National Diabetes Education Program
6. Economic consequences of diabetes mellitus in the US in 1997
7. Pharmacologic therapy for type 2 diabetes mellitus
8. Prevalence of diabetes, impaired fasting glucose and impaired glucose tolerance in US adults
9. Global burden of diabetes, 1995-2025: Prevalence, numerical estimates and projections
10. Diabetes. Exploding Type II
11. The rising global burden of diabetes and its complications: Estimates and projections by 2010
12. Mortality from coronary heart disease in subjects with type 2 diabetes and in nondiabetic subjects with and without prior myocardial infarction
13. FDA approach to the regulation of drugs for diabetes
14. Surrogate end points, health outcomes and the drug-approval process for the treatment of risk factors for cardiovascular disease
15. Pathogenesis of NIDDM. A balanced overview
16. Perspective: The insulin signaling system - A common link in the pathogenesis of type 2 diabetes
17. Role of liver in pathophysiology of NIDDM
18. Type II diabetes mellitus
19. On the pathophysiology of late onset non-insulin dependent diabetes mellitus. Current controversies and new insights
20. Glucose metabolism and the postprandial state
21. Regulation of hepatic glucose production in healthy subjects and patients with non-insulin-dependent diabetes mellitus
22. The role of splanchnic glucose appearance in determining carbohydrate tolerance
23. Contributions by kidney and liver to glucose production in the postabsorptive state and after 60 h of fasting
24. A critical evaluation of mass isotopomer distribution analysis of gluconeogenesis in vivo
25. Limitations of the mass isotopomer distribution analysis of glucose to study gluconeogenesis. Heterogeneity of glucose labeling in incubated hepatocytes
26. Measurement of gluconeogenesis and mass isotopomer analysis based on [U-(13)C]glucose
27. Estimating gluconeogenesis with [U-13C]glucose: Molecular condensation requires a molecular approach
28. NMR and stable isotope techniques for studies of liver metabolism in man
29. Metabolic investigations in humans by in vivo nuclear magnetic resonance
30. Hepatic glucose metabolism and insulin resistance in NIDDM and obesity
31. Influence of obesity and type 2 diabetes on gluconeogenesis and glucose output in humans: A quantitative study
32. Contributions of gluconeogenesis to glucose production in the fasted state
33. 13C NMR
34. 13C nuclear magnetic resonance study
35. Hepatic gluconeogenic fluxes and glycogen turnover during fasting in humans. A stable isotope study
36. Glycogen: Its mode of formation and contribution to hepatic glucose output in postabsorptive humans
37. Glucose production, recycling and gluconeogenesis in normals and diabetics: A mass isotopomer [U-13C]glucose study
38. Non-invasive tracing of liver intermediary metabolism in normal subjects and in moderately hyperglycaemic NIDDM subjects. Evidence against increased gluconeogenesis and hepatic fatty acid oxidation in NIDDM
39. The role of the liver in metabolic homeostasis: Implications for inborn errors of metabolism
40. The family of glycogen phosphorylases: Structure and function
41. Catalytic site of glycogen phosphorylase: Structure of the T state and specificity for α-D-glucose
42. Glucose analog inhibitors of glycogen phosphorylase: The design of potential drugs for diabetes
43. Design of Inhibitors of Glycogen Phosphorylase: A Study of α-and β-C-Glucosides and 1-Thio-β-D-glucose compounds
44. Glucose analog inhibitors of glycogen phosphorylase: From crystallographic analysis to drug prediction using GRID force-field and GOLPE variable selection
45. The structure of a glycogen phosphorylase glucopyranose spirohydantoin complex at 1.8.ANG. Resolution and 100 K: The role of the water structure and its contribution to binding
46. Efficient inhibition of muscle and liver glycogen phosphorylases by a new glucopyranosylidene-spirothiohydantoin
47. Ternary complex crystal structures of glycogen phosphorylase with the transition state analog nojirimycin tetrazole and phosphate in the T and R states
48. Sugarmimic glycosidase inhibitors: Natural occurrence, biological activity and prospects for therapeutic application
49. The effects of isofagomine, a potent glycogen phosphorylase inhibitor, on glycogen metabolism in cultured mouse cortical astrocytes
50. NN 42-1007 is a novel potent inhibitor of hepatic glycogen phosphorylase and of hepatocyte glycogenolysis
51. Kinetic and functional characterization of 1,4-dideoxy-1,4-imino-d-arabinitol: A potent inhibitor of glycogen phosphorylase with anti-hyperglycaemic effect in ob/ob mice
52. Inhibition of glycogenolysis enhances gluconeogenic precursor uptake by the liver of conscious dogs
53. Molecular mode of inhibition of glycogenolysis in rat liver by the dihydropyridine derivative, BAY R3401; Inhibition and inactivation of glycogen phosphorylase by an activated metabolite
54. The structure of glycogen phosphorylase b with an alkyl-dihydropyridine-dicarboxylic acid compound, a novel and potent inhibitor
55. Allosteric inhibition of glycogen phosphorylase a by the potential antidiabetic drug 3-isopropyl 4-(2-chlorophenyl)-1,4-dihydro-1-ethyl-2 -methyl-pyridine-3,5,6-tricarboxylate
56. Flavopiridol inhibits glycogen phosphorylase by binding at the inhibitor site
57. Analysis of an allosteric binding site: The nucleoside inhibitor site of phosphorylase alpha
58. Specificity of inhibition of muscle glycogen phosphorylase β by flavins
59. Synergistic regulation of phosphorylase a by glucose and caffeine
60. The effect of caffeine and caffeine analogs on rat liver phosphorylase a activity
61. Uric acid inhibits liver phosphorylase a activity under simulated in vivo conditions
62. Discovery of a human liver glycogen phosphorylase inhibitor that lowers blood glucose in vivo
63. Indole-2-carboxamide inhibitors of human liver glycogen phosphorylase
64. A new allosteric site in glycogen phosphorylase b as a target for drug interactions
65. Human liver glycogen phosphorylase inhibitors bind at a new allosteric site
66. Evaluation of Isofagomine and its derivatives as potent Glycosidase inhibitors
67. Inhibition of glycogenolysis in primary rat hepatocytes by 1,4-dideoxy-1,4-imino-D-arabinitol
68. Effects of C-1-substituted glucose analog on the activation states of glycogen synthase and glycogen phosphorylase in rat hepatocytes
69. Demonstration of a glycogen/glucose 1-phosphate cycle in hepatocytes from fasted rats. Selective inactivation of phosphorylase by 2-deoxy-2-fluoro-alpha-D-glucopyranosyl fluoride
70. Gram-scale synthesis of a glucopyranosylidene-spirothiohydantoin and its effect on hepatic glycogen metabolism studied in vitro and in vivo
71. Regulation of the dephosphorylation of glycogen phosphorylase a and synthase b by glucose and caffeine in isolated hepatocytes
72. Identification of the separate domains in the hepatic glycogen-targeting subunit of protein phosphatase 1 that interact with phosphorylase a, glycogen and protein phosphatase 1
73. Specific featurés of glycogen metabolism in the liver
74. Inhibition of gluconeogenesis and glycogenolysis by 2,5-anhydro-D-mannitol
75. The human liver glycogen phosphorylase inhibitor CP-320,626 shows sustained glucose lowering on multiple dosing in diabetic ob/ob mice
76. Glucose and glycogen utilisation in myocardial ischemia - Changes in metabolism and consequences for the myocyte
77. Cardio-protective effect of the glycogen phosphorylase inhibitor CP-380867
78. Crucial role of intracellular effectors on glycogenolysis in the isolated rat heart: Potential consequences on the myocardial tolerance to ischemia
79. A novel anti-diabetic drug, miglitol, markedly reduces myocardial infarct size in rabbits
80. Ribbons 2.0
81. Activation of human liver glycogen phosphorylase by alteration of the secondary structure and packing of the catalytic core