GLP-1 derivatives as novel compounds for the treatment of type 2 diabetes: Selection of NN2211 for clinical development

Drugs of the Future

Volumn 26, Issue 7, 2001, Pages 677-685

  Knudsen, B L ^a   Agerso, H ^a   Bjenning, C ^a   Bregenholt, S ^a   Carr, R D ^a   Godtfredsen, C ^a   Holst, J J ^a   Huusfeldt, P O ^a   Larsen, M O ^a   Larsen, P J ^a   Nielsen, P F ^a   Ribel, U ^a   Rolin, B ^a   Romer, J ^a   Sturis, J ^a   Wilken, M ^a   Kristensen, P ^a  

^a NOVO NORDISK A S   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

GLUCAGON LIKE PEPTIDE 1; GLUCAGON LIKE PEPTIDE 1 [7-36] AMIDE; GLUCAGON LIKE PEPTIDE 1 [7-37] AMIDE; GLUCAGON LIKE PEPTIDE 1 [7-38] AMIDE; GLUCOSE; LIRAGLUTIDE; UNCLASSIFIED DRUG;

ACYLATION; AMINO ACID SEQUENCE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; CONTROLLED STUDY; DERIVATIZATION; DOSE RESPONSE; DRUG POTENCY; GLUCOSE BLOOD LEVEL; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PHARMACODYNAMICS; RAT; REVIEW;

EID: 0034781256     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.2001.026.07.628723     Document Type: Review

References (92)

1. Clinical practice recommendations 2001
2. Hamster preproglucagon contains the sequence of glucagon and two related peptides
3. Exon duplication and divergence in the human preproglucagon gene
4. Pathogenesis of NIDDM. A balanced overview
5. The essential role of glucagon in the pathogenesis of diabetes mellitus
6. Degradation of glucagon-like peptide-1 by human plasma in vitro yields an N-terminally truncated peptide that is a major endogenous metabolite in vivo
7. Degradation of GIP and truncated GLP-1 in vitro and in vivo by dipeptidyl peptidase IV
8. GLP-1(9-36)amide is major metabolite of GLP-1(7-36)amide after in vivo administration to dogs, and it acts as an antagonist on the pancreatic receptor
9. Subcutaneous injection of the incretin hormone GLP-1 abolishes postprandial glycemia in NIDDM
10. Effects of subcutaneous GLP-1(7-36)amide in patients with NIDDM
11. Preserved incretin activity of GLP-1(7-36amide) but not of synthetic human GIP in patients with type 2-diabetes mellitus
12. Insulinotropic action of GLP-1-(7-37) in diabetic and non-diabetic subjects
13. Normalization of fasting hyperglycemia by exogenous GLP-1(7-36amide) in type 2 diabetic patients
14. GLP-1(7-36): A physiological incretin in man
15. Expression cloning of the pancreatic β-cell receptor for the gluco-incretin hormone glucagon-like peptide 1
16. Insulinotropic glucagon-like peptide-1 receptor expression in glucagon-producing α-cells of the rat endocrine pancreas
17. The metabolic rate and the biological effects of GLP-1(7-36amide) and GLP-1(7-37) in healthy volunteers are identical
18. Differential effects of subcutaneous GLP-1 on gastric emptying, antroduodenal motility and pancreatic function in men
19. Gastric emptying, glucose responses, and insulin secretion after a liquid test meal: Effects of exogenous GLP-1(7-36)amide in type 2 (noninsulin-dependent) diabetic patients
20. Pharmacokinetic, insulinotropic, and glucagonostatic properties of GLP-1(7-36amide) after subcutaneous injection in healthy volunteers. Dose-response relationships
21. Effect of glucagon-like peptide-1 (proglucagon 78-107amide) on hepatic glucose production in healthy men
22. Glucagon-like peptide-1 inhibition of gastric-emptying outweighs its insulinotropic effects in healthy humans
23. Antidiabetogenic effect of glucagon-like peptide-1 (7-36)amide in normal subjects and patients with diabetes mellitus
24. Glucagonostatic actions and reduction of fasting hyperglycemia by exogenous glucagon-like peptide-1(7-36amide) in type I diabetic patients
25. Near-normalization of diurnal glucose concentrations by continous administration of GLP-1 in subjects with NIDDM
26. Glucagon-like peptide-1 infusion must be maintained for 24 h/day to obtain acceptable glycemia in type 2 diabetic patients who are poorly controlled on treatment with sulphonylurea
27. GLP-1 for six weeks reduces weight and improves insulin sensitivity and glycemic control in patients with type 2 diabetes
28. Insulinotropic actions of intravenous glucagon-like peptide-1[7-36amide] in the fasting state in healthy subjects
29. Cellular regulation of islet hormone secretion by the incretin hormone GLP- 1
30. Subcutaneous glucagon-like peptide-1(7-36)amide is insulinotropic and can cause hypoglycaemia in fasted healthy subjects
31. Exaggerated secretion of GLP-1 could cause reactive hypoglycaemia
32. Insulinotropic hormone GLP-1(7-37) stimulation of proinsulin gene expression and proinsulin biosynthesis in insulinoma βTC1-cells
33. GLP-1 affects gene transcription and mRNA stability of components of the insulin secretory system in RIN 1046-38 cells
34. GLP-1 can reverse the age-related decline in glucose tolerance in rats
35. The effects of GLP-1 on insulin release in young and old rats in the fasting state and during an intravenous glucose tolerance test
36. GLP-1 confers glucose sensitivity to previously glucose-incompetent β-cells in diabetic rats: In vivo and in vitro studies
37. Glucagon-like peptide-1 improves the ability of the β-cell to sense and respond to glucose in subjects with impaired glucose-tolerance
38. Initiation of increased pancreatic islet growth in young normoglycaemic mice (Umeå +/?)
39. GLP-1 promotes DNA synthesis, activates phosphatidylinasitol-3-kinase and increases transcription factor pancreatic and duodenal homeobox gene 1 (PDX- 1) DNA binding activity in (INS-1)-cells
40. Exendin-4 stimulates both β-cell replication and neogenesis, resulting in increased β-cell mass and improved glucose tolerance in diabetic rats
41. The GLP-1 derivative NN2211 inhibits cytokine-induced apoptosis in primary rat β-cells
42. Glucagon-like peptide-1 and exendin-4 convert pancreatic ARJ42 cells into glucagon and insulin producing cells
43. In vitro insulinomimetic effects of GLP-1 in liver, muscle and fat
44. Glucagon-like peptide 1 enhances glucose tolerance both by stimulation of insulin release and by increasing insulin-independent glucose disposal
45. Effect of glucagon-like peptide 1(7-36) amide on initial splanchnic glucose uptake and insulin action in humans with type 1 diabetes
46. GLP-1 does not acutely affect insulin sensitivity in healthy man
47. Effect of glucagon-like peptide 1(7-36) amide on glucose effectiveness and insulin action in people with type 2 diabetes
48. GLP-1 promotes satiety and suppresses energy intake in humans
49. GLP-1 increases the period of postprandial satiety and slows gastric emptying in obese humans
50. Glucagon-like peptide-1:A potent regulator of food intake in humans
51. Attenuated GLP-1 secretion in obesity: Cause or consequence
52. Systemic administration of the long-acting GLP-1 derivative NN2211 induces lasting and reversible loss of body adiposity
53. Glucagon-like peptide-1- a novel brain peptide involved in feeding regulation
54. Brain GLP-1(7-36) amide receptors play a major role in regulation of food and water intake
55. A role for glucagon-like peptide-1 in the regulation of feeding
56. Distribution of glucagon-like peptide-1 (GLP-1), glucagon, and glicentin in the rat brain: An immunocytochemical study
57. Distribution of glucagon-like peptide-1 (GLP-1) and other preproglucagon derived peptides in the rat hypothalamus and brain stem
58. GLP-1 receptors in the subfornical organ and the area postrema are accessible to circulating glucagon-like peptide-1
59. GLP-1 (glucagon-like peptide-1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in man
60. Truncated GLP-1 (proglucagon 72-107amide) inhibits gastric and pancreatic functions in man
61. The inhibitory effect of glucagon-like peptide-1 (7-36amide) on gastric acid secretion in man depends on an intact vagal innervation
62. Glucagon-like peptide-1 inhibits gastric emptying via vagal afferent-mediated central mechanisms
63. Small bowel gut hormones: Correlation to fasting antroduodenal motility and gastric emptying
64. GLP-1 in the pathogenesis of obesity
65. Reduced post-prandial concentrations of intact biologically active glucagon-like peptide 1 in type 2 diabetic patients
66. GLP-1 inhibits gastric emptying of water but does not influence plasma vasopressin, sodium, or osmolality
67. The glucagon-like peptides
68. Potential therapeutic levels of GLP-1 achieved in humans by a buccal tablet
69. Dipeptidyl peptidase IV resistant analogues of GLP-1 which have extended metabolic stability and improved biological activity
70. LY315902: An analog of GLP-1 with enhanced activity and time action in vivo
71. The GLP-1 analogue LY307161 is resistant to degradation by DPP-IV and is fully active in vitro
72. Glucose-lowering and insulin-sensitizing actions of exendin-4: Studies in obese diabetic (ob/ob, db/db) mice, diabetic fatty Zucker rats, and diabetic rhesus monkeys (Macaca mulatta)
73. LY307161: A protease-protected analogue of GLP-1, with enhanced activity and time action in vivo
74. Albumin-binding of insulins acylated with fatty-acids: Characterization of the ligand protein-interaction and correlation between binding-affinity and timing of the insulin effect in vivo
75. Soluble, fatty-acid acylated insulins bind to albumin and show protracted action in pigs
76. Albumin-binding and time action of acylated insulins in various species
77. Acylation of human insulin with palmitic acid extends the time action of human insulin in diabetic dogs
78. Potent derivatives of GLP- 1 with pharmacokinetic properties suitable for once daily administration
79. Structure activity studies of GLP-1
80. Derivatives of glucagon-like peptide-1 suitable for once daily administration
81. Pharmacokinetic profile of the long-acting derivative NN2211 in healthy male subjects
82. Evidence of a substantial reduction in fasting and postprandial glycemia in type 2 diabetes after bedtime administration of a long-acting GLP-1 derivative, NN2211
83. Glucose lowering effect of the protracted GLP-1 derivative, NN2211, in the β-cell reduced minipig
84. Effect of the protracted GLP-1 derivative NN2211 in β-cell reduced minipig
85. NN2211, a protracted GLP-1 derivative, potently reduces consumption of high-carbohydrate and high-fat diets in the rat
86. Efficacy of the long-acting GLP-1 derivative NN2211 in diabetic ob/ob mice
87. NN2211, a long-acting derivative of GLP-1, lowers blood glucose in diabetic ob/ob and db/db mice
88. NN2211, a GLP-1 Derivative, has a long lasting blood glucose lowering effect in db/db mice: A comparison with exendin-4
89. Effects of NN2211, a long-acting derivative of GLP-1, on β-cell proliferation and β-cell mass in db/db mice
90. The long-acting GLP-1 derivative NN2211 markedly slows diabetes development in the male Zucker diabetic fatty rat