Therapeutic potential of endothelin receptor antagonists in diabetes

Expert Opinion on Investigational Drugs

Volumn 9, Issue 12, 2000, Pages 2873-2888

  Chakrabarti, S ^a   Cukiernik, M ^a   Mukherjee, S ^a   Chen, S ^a  

^a UNIVERSITY OF WESTERN ONTARIO   (Canada)

Author keywords

Cardiomyopathy; Diabetic complications; Endothelin antagonism; Endothelins; Nephropathy; Neuropathy; Retinopathy

Indexed keywords

2 BUTYL 7 [2 (2 CARBOXYPROPYL ) 4 METHOXYPHENYL] 5 (3,4 METHYLENEDIOXYPHENYL)CYCLOPENTENO[1,2 B]PYRIDINE; 2 PYRIDYLCARBAMIC ACID 2 [[5 (2 METHOXYPHENOXY) 6 [[(4 ISOPROPYLPHENYL)SULFONYL]AMINO] 2 MORPHOLINO 4 PYRIMIDINYL]OXY]ETHYL ESTER; 3 (2 CARBOXYMETHOXY 4 METHOXYPHENYL) 1 (3,4 METHYLENEDIOXYPHENYL) 5 PROPOXY 2 INDANCARBOXYLIC ACID; A 127222; A 182086; ALPHA TOCOPHEROL; ANTIOXIDANT; ASCORBIC ACID; BOSENTAN; BQ 4508; BQ 45082; ENDOTHELIN 1; ENDOTHELIN 2; ENDOTHELIN 3; ENDOTHELIN A RECEPTOR; ENDOTHELIN A RECEPTOR ANTAGONIST; ENDOTHELIN B RECEPTOR; ENDOTHELIN B RECEPTOR ANTAGONIST; ENDOTHELIN RECEPTOR; ENDOTHELIN RECEPTOR ANTAGONIST; ENRASENTAN; GLUCOSE; L 749329; N ACETYL 10,11 DIHYDRO 5H DIBENZO[A,D]CYCLOHEPTEN 5 YLGLYCYLLEUCYLASPARTYLISOLEUCYLISOLEUCYLTRYPTOPHAN; PD 156252; SITAXSENTAN; TAK 044; TARASENTAN; TRANSFORMING GROWTH FACTOR BETA; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; CARDIOMYOPATHY; CELL DIFFERENTIATION; CELL PROLIFERATION; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CORONARY ARTERY ATHEROSCLEROSIS; DIABETES MELLITUS; DIABETIC ANGIOPATHY; DIABETIC NEPHROPATHY; DIABETIC NEUROPATHY; DIABETIC RETINOPATHY; DRUG EFFECT; DRUG RECEPTOR BINDING; GENE INDUCTION; GLYCATION; HUMAN; HYPERTENSION; MAJOR CLINICAL STUDY; MITOGENESIS; NEOVASCULARIZATION (PATHOLOGY); NONHUMAN; OXIDATIVE STRESS; PATHOGENESIS; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; PHASE 3 CLINICAL TRIAL; PROTEIN DETERMINATION; PROTO ONCOGENE; RAT; REVIEW;

EID: 0033663092     PISSN: 13543784     EISSN: None     Source Type: Journal    
DOI: 10.1517/13543784.9.12.2873     Document Type: Review

References (168)

1. Endothelin antagonists and renal protection
2. A novel potent vasoconstrictor peptide produced by vascular endothelial cells
3. The human endothelin family: Three structurally and pharmacologically distinct isopeptides predicted by three separate genes
4. The cellular and molecular mechanisms of diabetic complications
5. Endothelins: Molecular biology, biochemistry, pharmacology, physiology and pathophysiology
6. Endothelins
7. Differential regulation of fos and jun gene expression and AP-1 Cis element activity by endothelin isopeptides: Possible implications for mitogenic signalling by endothelin
8. The human endothelin family: Three structurally and pharmacologically distinct isopeptides predicted by three separate genes
9. Endothelin-1 and endothelin receptor antagonists in cardiovascular remodelling
10. Cellular mechanisms of thrombin on endothelin-1 biosynthesis and release in bovine endothelial cells
11. Transforming growth factor beta stimulates the expression of endothelin mRNA from vascular endothelial cells
12. Transcriptional regulation of the endothelin gene by TNF alpha
13. Pathophysiology of endothelin in the cardiovascular system
14. Cellular mechanism of natriuretic peptides-induced inhibition of endothelin-1 biosynthesis in rat endothelial cells
15. Heparin has an inhibitory effect on endothelin-1 synthesis and release by endothelial cells
16. Regional hemodynamic effects and clearance of endothelin-1 in humans: Renal and peripheral tissue may contribute to the overall disposal of the peptide
17. Molecular characterization of endothelin receptors
18. Endothelin antagonism with bosentan: A review of potential applications
19. Endothelin-1 modulates vascular smooth muscle structure and vasomotion: Implications in cardiovascular pathology
20. Pressor effects of circulating endothelin are limited by its removal in the pulmonary circulation and by the release of prostacyclin and endothelium derived relaxing factor
21. Both ET(A) and ET(B) receptors mediate contraction to endothelin-1 in human blood vessels
22. Clinical development of endothelin receptor antagonists
23. Endothelin receptor antagonists: New perspectives in endothelin research
24. Endothelin: Role in hypertension
25. Structure-activity relationships of the potent combined endothelin-A/ endothelin-B receptor antagonists Ac-DDip16-Leu-Asp-Ile-Trp21:Development of endothelin-B receptor selective antagonists
26. Discovery and synthesis of (S)-3-[2-(3,4-dimethoxy phenyl) ethoxy]-2-(4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU-302872), a novel orally active mixed ETA/ETB receptor antagonist
27. J-104132, a potent, orally active, mixed ETA/ETB receptor antagonist, attenuated salt-sensitive hypertension
28. Antihypertensive effect of the endothelin receptor antagonist SB-209670
29. Agonist-dependent inhibition by peptide and non peptide endothelin receptor antagonists in the rabbit isolated pulmonary artery
30. Endothelin receptor antagonists influence cardiovascular morphology in uremic rats
31. Pharmacological characterization of A-127722: An orally active and highly potent ET (A)-selective receptor antagonist
32. Structure-activity relationships of N2-aryl-3-(isoxazolysulfamoyl)- 2-thiophenecarboxamides as selective endothelin receptor-A antagonists 1
33. Highly selective endothelin antagonists for ETa receptor: Synthesis and structure-activity relationships
34. Comparison of PD-145065 and Ro-46-2005 as antagonists of contractions of guinea-pig airways induced by endothelin-1 or IRL-1620
35. Design of a potent combined pseudopeptide endothelin-A/endothelin-B receptor antagonist, Ac-DBhg16-Leu-Asp-Ile-[NMe]Ile-Trp21 (PD 156252): Examination of its pharmacokinetic and spectral properties
36. Pharmacological profile in vitro of a new endothelin receptor antagonist, TAK-044
37. Endothelin receptor antagonism in patients with chronic heart failure
38. Endothelin receptor blockade attenuates air embolization-induced pulmonary hypertension in sheep
39. An epidemiological model for diabetes mellitus in the United States: Five major complications
40. Diabetic retinopathy: A review
41. Glycosylated hemoglobin predicts the incidence and progression of diabetic retinopathy
42. The effect of intensive treatment of diabetes on the development of long-term complications in insulin-dependent diabetes mellitus
43. Lessons from the diabetes control and complication trial
44. Retinal vascular patterns VI. Mural cells of the retinal capillaries
45. Accelerated death of retinal microvascular pericytes in human and experimental diabetic retinopathy
46. Comparison of retinal lesions in alloxan-diabetic rats and galactose-fed rats
47. Endothelium: The main actor in the remodelling of the retinal microvasculature in diabetes
48. Coagulation activation in diabetes mellitus: The role of hyperglycemia and therapeutic prospects
49. Decreased antithrombin III activity in diabetes may be due to non-enzymatic glycosylation. A preliminary report
50. Protein kinase C (PKC) activation is a causal factor for the alteration of retinal blood flow in diabetes of short duration
51. 3H-Desmethylimiprimine) microspheres
52. Glucose-induced metabolic imbalances in the pathogenesis of diabetic vascular disease
53. Inhibition of sorbitol dehydrogenase. Effects on vascular and neural dysfunction in streptozocin-induced diabetic rats
54. Prevention of diabetic vascular dysfunction by guanidines. Inhibition of nitric oxide synthase versus advanced glycation end-product formation
55. Prevention of hemodynamic and vascular albumin filtration changes in diabetic rats by aldose reductase inhibitors
56. Glucose-induced increases in ocular blood flow are prevented by aminoguanidine and L-NMMA, inhibitors of nitric oxide synthase
57. Endoneurial blood flow changes in diabetic rats
58. Vitamin E prevents diabetes-induced abnormal retinal blood flow via the diacylglycerol-protein kinase C pathway
59. Normalization of retinal blood flow in diabetic rats with primary intervention using insulin pumps
60. Amelioration of vascular dysfunctions in diabetic rats by an oral PKC beta inhibitor
61. Vascular endothelial growth factor-induced retinal permeability is mediated by protein kinase C in vivo and suppressed by an orally effective beta-isoform-selective inhibitor
62. Effect of propionyl-L-carnitine on oscillatory potentials in electroretinogram in streptozotocin-diabetic rats
63. Effect of an aldose reductase inhibitor on abnormalities of electroretinogram and vascular factors in diabetic rats
64. The development of electroretinogram abnormalities and possible roles of polyol pathway activity in diabetic hyperglycemia and galactosemia
65. Treatment with an aldose reductase inhibitor or with myo-inositol arrests deterioration of electroretinogram of diabetic rats
66. United States Renal Data System 1990 annual report
67. Diabetic neuropathy in Type I (insulin-dependent) diabetes: An epidemiological study
68. Predictors of the progression of renal insufficiency in patients with insulin-dependent diabetes and overt diabetic nephropathy
69. The stages in diabetic renal disease. With emphasis in the stage of incipient diabetic neuropathy
70. The Kidney
71. Glomerular and mesangial cell number in insulin dependent diabetes mellitus (IDDM)
72. Pathophysiology of Progressive nephropathies
73. United Kingdom prospective diabetic study
74. Effect of intensive therapy
75. Anti-TGF-β antibody attenuates hypertrophy and extracellular matrix gene expression
76. Diabetic neuropathy: Models, mechanisms and mayhem
77. Pathogenesis of diabetic neuropathy
78. Diabetes mellitus and hypertension
79. Relation between insulin resistance and carotid intima-media thickness and stenosis in non-diabetic subjects. Results from a cross-sectional study in Malmo, Sweden
80. Acute myocardial infarction in diabetes mellitus and significance of congestive heart failure as a prognostic factor
81. Cardiac consequences of diabetes mellitus
82. Diabetic cardiomyopathy: An overview
83. Diabetic autonomic neuropathy in BB rats and effect of ARI treatment on heart rate variability and vagus structure
84. Perspectives in diabetes. Hyperglycemic pseudohypoxia and diabetic complications
85. The sorbitol-osmotic and sorbitol-redox hypotheses
86. Protein kinase C activation and the development of diabetic complications
87. Downregulation of the human taurine transporter by glucose in cultured retinal pigment epithelial cells
88. Abnormalities of retinal metabolism in diabetes or galactosemia: ATPases and glutathione
89. Abnormalities of retinal metabolism in diabetes or experimental galactosemia. IV. Antioxidant defense system
90. Glucose dependence of glycolysis, hexose monophosphate shunt activity, energy status and the polyol pathway in retinas isolated from normal (non diabetic) rats
91. Evaluation of β1-adrenoceptor antagonist and antioxidant therapy on diabetes-induced changes in retinal NAD(P)-Redox status: Evidence against pseudohypoxia?
92. Free radicals, nitric oxide and diabetic complications
93. The autoxidation of glyceraldehyde and other simple monosaccharides
94. Hydroxyl radical production and autoxidative glycosylation. Glucose autoxidation as the cause of protein damage in the experimental glycation model of diabetes mellitus and ageing
95. Hydrogen peroxide production during experimental protein glycation
96. The oxidation of oxyhaemoglobin by glyceraldehyde and other simple monosaccharides
97. Effect of insulin on impaired antioxidant activities in aortic endothelial cells from diabetic rabbits
98. Glycation and inactivation of human Cu-Zn-superoxide dismutase. Identification of the in vitro glycated site
99. Normalizing mitochondrial superoxide production blocks three pathways of hyperglycaemic damage
100. Regulation of protein kinase C
101. PKC is a novel, atypical member of the protein kinase C family
102. Protein kinase C isotypes controlled by phosphoinositide 3 kinase through the protein kinase PDK1
103. Correlation of diacylglycerol level and protein kinase C activity in rat retina to retinal circulation
104. Characterization of the mechanism for the chronic activation of DAG-PKC pathway in diabetes and hypergalactosemia
105. Abnormalities of retinal metabolism in diabetes or experimental galactosemia. III. Effects of antioxidants
106. Increased endothelial albumin permeability mediated by protein kinase C activation
107. Enhanced expression of inducible nitric oxide synthase in murine macrophages and glomerular mesangial cells by elevated glucose levels: Possible mediation via protein kinase C
108. The role of growth factors in the pathogenesis of diabetic vascular complications
109. Recent progress in advanced glycation end products and diabetic complications
110. Significance of fructose-induced protein oxidation and formation of advanced glycation end product
111. Mechanism of protein modification by glyoxal and glycolaldehyde, reactive intermediates of the Maillard reaction
112. Advanced glycation end products (AGEs) co-localize with AGE receptors in the retinal vasculature of diabetic and of AGE-infused rats
113. Characterization of the advanced glycation end-product receptor complex in human vascular endothelial cells
114. The role of oxidative stress and NF-kappaB activation in late diabetic complications
115. Endothelial receptor mediated binding of glucose modified albumin is associated with increased monolayer permeability and modulation of cell surface coagulant properties
116. Advanced glycation end products-driven angiogenesis in vitro. Induction of the growth and tube formation of human microvascular endothelial cells through autocrine vascular endothelial growth factor
117. Altered cellular interaction between endothelial cells and non-enzymatically glucosylated laminin/type IV collagen
118. Advanced glycosylation products quench nitric oxide and mediate defective endothelium-dependent vasodilation in experimental diabetes
119. BCL-2-expression or antoxidants prevent hyperglycemia-induced formation of intracellular advanced glycation end products in bovine endothelial cells
120. Endothelin: Emerging role in diabetic vascular complications
121. Enhanced secretion of endothelin_1 by elevated glucose levels from cultured bovine aortic endothelial cells
122. Interaction of endothelin-1 with vasoactive factors in mediating glucose-induced increased permeability in endothelial cells
123. Insulin stimulates production and secretion of endothelin from bovine endothelial cells
124. Targeted overexpression of protein kinase C2 isoform in myocardium causes cardiomyopathy
125. Endothelin-1. A matter of life and breath
126. Vascular endothelial growth factor increases endothelin-converting enzyme expression in vascular endothelial cells
127. Vasoactive peptides modulate vascular endothelial cell growth factor production and endothelial cell proliferation and invasion
128. Endothelin 1 transcription is controlled by nuclear factor-κB in AGE-stimulated cultured endothelial cells
129. Endothelin-1 and Endothelin-3 like immunoreactivity in the eyes of diabetic and non-diabetic BB/W rats
130. Immunoreactive endothelin distribution in ocular tissue
131. Augmented retinal endothelin-1, endothelin-3, Endothelin(A) and Endothelin(B) gene expression in chronic diabetes
132. Regulation of retinal hemodynamics in diabetic rats by increased expression and action of endothelin-1
133. Diabetes induced dysfunction in the retina: Role of endothelins
134. Endothelins, their receptors and retinal vascular dysfunction in galactose-fed rats
135. Endothelin receptor blockade prevents augmented extracellular matrix component mRNA expression and capillary basement membrane thickening in the retina of diabetic and galactose fed rats
136. Increased plasma endothelin in NIDDM patients with retinopathy
137. Immunoreactive endothelin levels in the vitreous fluid are decreased in diabetic patients with proliferative retinopathy
138. Endothelins: Multifunctional renal peptides
139. Elevated renal endothelin-1 clearance and mRNA levels associated with albuminuria and nephropathy in non-insulin dependent diabetes mellitus studies in obese fa/fa Zucker rats
140. Time-dependent up-regulation of endothelin-A receptors and down-regulation of endothelin-B receptors and nitric oxide synthase binding sites in the renal medulla of a rabbit model of partial bladder outlet obstruction: Potential clinical relevance
141. Effect of a specific endothelin-A receptor antagonist on mRNA levels for extracellular matrix components and growth factors in diabetic glomeruli
142. Regulation of mRNA expression for ECM by cultured rat mesangial cells
143. Endothelin-1 is produced and secreted by neonatal rat cardiac myocytes in vitro
144. Regulation of endothelin-1 mRNA by angiotensin II in rat heart endothelial cells
145. Expression of endothelin-1 and endothelin-converting enzyme-1 mRNAs and proteins in failing human hearts
146. Endothelin has potent inotropic effects in rat atria
147. Positive chronotropic effects of endothelin, a novel endothelium-derived vasoconstrictor peptide
148. The role of endothelins in cardiac function in health and disease
149. Expression of preproEndothelin-1 mRNA in streptozotocin-induced diabetic rats
150. Cardiac and renal endothelin-1 binding sites in streptozotocin-induced diabetic rats
151. Changes in the responsiveness to endothelin-1 in isolated atria from diabetic rats
152. Diabetes-induced myocardial structural changes: Role of endothelin-1 and its receptors
153. Endothelin in hypertension and diabetes mellitus
154. Vascular damage and not hypertension per se influences endothelin-1 plasma levels in patients with non insulin dependent diabetes mellitus
155. Experimental diabetic neuropathy: An update
156. 1,2-diacylglycerol content and its arachidonyl-containing molecular species are reduced in sciatic nerve from streptozotocin-induced diabetic rats
157. +-ATPase activity in sciatic nerve of diabetic mice by administration of H7 or callphostin C, inhibitors of protein kinase C
158. The potential contribution of endothelin-1 to neurovascular abnormalities in streptozotocin diabetic rats
159. Effects of endothelin receptor antagonism with bosentan on peripheral nerve function in experimental diabetes
160. Endothelin-1 and its receptors in the pathogenesis of neuronal and retinal functional abnormalities in the diabetic rats
161. Contribution of protein kinase C to ET-1-induced proliferation in human myometrial cells
162. Endothelin-stimulated phosphoinositide turnover and protein kinase C translocation in rat synaptosomes
163. +, K(+)-ATPase and Na(+)-K(+)-C1-cotransport through ETA receptors and protein kinase C-dependent pathway in cerebral capillary endothelium
164. Endothelial relaxation is disturbed by oxidative stress in the diabetic rat heart: Influence of tocopherol as antioxidant
165. Differential regulation of nitric oxide synthase-II mRNA by growth factors in rat, bovine and human retinal pigmented epithelial cells
166. Insulin and IGF-I attenuate the coronary vasoconstrictor effects of endothelin-1 but not of sarafotoxin 6c
167. Suppression of hypoxia-associated vascular endothelial growth factor gene expression by nitric oxide via cGMP