Peroxisome proliferator-activated receptor (PPAR)γ agonists for diabetes

Advances in Protein Chemistry

Volumn 56, Issue , 2001, Pages 181-212

  Moller, David E ^a,b   Greene, Douglas A ^a,b  

^a MERCK RESEARCH LABORATORIES   (United States)

^b UNIVERSITY OF MICHIGAN MEDICAL SCHOOL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; GW 2570; INSULIN; L 764406; L 796449; METFORMIN; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR AGONIST; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PIOGLITAZONE; ROSIGLITAZONE; SB 219994; SULFONYLUREA DERIVATIVE; TROGLITAZONE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; BODY WEIGHT DISORDER; CLINICAL TRIAL; DRUG MECHANISM; DRUG RECEPTOR BINDING; GLUCOSE HOMEOSTASIS; HEMOGLOBINOPATHY; HUMAN; INSULIN RESISTANCE; INSULIN SENSITIVITY; LIVER TOXICITY; META ANALYSIS; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PANCREAS ISLET BETA CELL; PRIORITY JOURNAL; RAT; REVIEW;

ANIMALIA;

EID: 0035056155     PISSN: 00653233     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0065-3233(01)56006-4     Document Type: Review

References (135)

1. The PPAR alpha-leukotriene B4 pathway to inflammation control
2. Modification of metabolism and distribution of lipids by ethylchlorophenoxyisobutyrate
3. Nature of the hepatomegalic effect produced by ethyl-chlorophenoxy-isobutyrate in the rat
4. Peroxisome proliferator-binding Protein: Identification and partial characterization of nafenopin-clofibric acid-, and ciprofibrate-binding proteins from rat liver
5. Hypolipidemic drugs, polyunsaturated fatty acids, and eicosanoids are ligands for peroxisome proliferator-activated receptors alpha and delta
6. Enhancement of adipocyte differentiation by an insulin-sensitizing agent
7. Adipocyte-specific transcription factor ARF6 is a heterodimeric complex of two nuclear hormone receptors, PPAR gamma and RXR alpha
8. Stimulation of adipogenesis in fibroblasts by PPAR gamma 2, a lipid-activated transcription factor
9. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma)
10. Thiazolidinediones produce a conformational change in peroxisomal proliferator-activated receptor-γ: Binding and activation correlate with antidiabetic actions in db/db mice
11. Activation of a member of the steroid hormone receptor superfamily by peroxisome proliferators
12. cDNA cloning, chromosomal mapping, and functional characterization of the human peroxisome proliferator activated receptor
13. Differential expression of peroxisome proliferator-activated receptors (PPARs): Tissue distribution of PPAR-alpha, -beta, and -gamma in the adult rat
14. Chromosomal localisation, inducibility, tissue-specific expression and strain differences in three murine peroxisome-proliferator-activated-receptor genes
15. Control of the peroxisomal beta-oxidation pathway by a novel family of nuclear hormone receptors
16. Cloning of a new member of the peroxisome proliferator-activated receptor gene family from mouse liver
17. cDNA cloning and characterization of the transcriptional activities of the hamster peroxisome proliferator-activated receptor happar gamma
18. Isolation of the human peroxisome proliferator activated receptor gamma cDNA: Expression in hematopoietic cells and chromosomal mapping
19. Structural organization of mouse peroxisome proliferator-activated receptor gamma (mPPARγ) gene: Alternative promoter use and different splicing yield two mPPARγ isoforms
20. Molecular cloning, expression and characterization of human peroxisome proliferator activated receptors gamma 1 and gamma 2
21. Regulation of PPAR gamma gene expression by nutrition and obesity in rodents
22. Identification of a new member of the steroid hormone receptor superfamily that is activated by a peroxisome proliferator and fatty acids
23. The RXR heterodimers and orphan receptors
24. The peroxisome proliferator-activated receptor interacts with the retinoid X receptor in vivo
25. The directly repeated RG(G/T)TCA motifs of the rat and mouse cellular retinol-binding protein II genes are promiscuous binding sites for RAR, RXR, HNF-4, and ARP-1 homo- and heterodimers
26. DNA binding properties of peroxisome proliferator-activated receptor subtypes on various natural peroxisome proliferator response elements. Importance of the 5′-flanking region
27. A signature motif in transcriptional co-activators mediates binding to nuclear receptors
28. The transcriptional co-activator P/CIP binds CBP and mediates nuclear-receptor function
29. Co-activators and co-repressors in the integration of transcriptional responses
30. Nuclear receptors have distinct affinities for coactivators: Characterization by fluorescence resonance energy transfer
31. Cloning and identification of mouse steroid receptor coactivator-1, as a coactivator of peroxisome proliferator-activated receptor gamma
32. Isolation and characterization of PBP, a protein that interacts with peroxisome proliferator-activated receptor
33. A cold-inducible coactivator of nuclear receptors linked to adaptive thermogenesis
34. Inhibition of adipogenesis through MAP kinase-mediated phosphorylation of PPARγ
35. Evolution of the nuclear receptor gene superfamily
36. The nuclear receptor superfamily: The second decade
37. Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-gamma
38. Crystal structure of the ligand binding domain of the human nuclear receptor PPARγ
39. Novel PPARγ and PPARδ ligands produce distinct biological effects
40. Hypoglycemic activity of a series of alpha-alkylthio and alpha-alkoxy carboxylic acids related to ciglitazone
41. L-764406 is a partial agonist of human peroxisome proliferator-activated receptor gamma. The role of Cys313 in ligand binding
42. 15-deoxy-delta 12, 14-prostaglandin J2 is a ligand for the adipocyte determination factor PPAR gamma
43. A prostaglandin J2 metabolite binds peroxisome proliferator-activated receptor gamma and promotes adipocyte differentiation
44. Oxidized LDL regulates macrophage gene expression through ligand activation of PPARγ
45. Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gamma
46. A novel insulin sensitizer acts as a coligand for peroxisome proliferator-activated receptor-alpha (PPAR-alpha) and PPAR-Gamma: Effect of PPAR-alpha activation on abnormal lipid metabolism in liver of zucker fatty rats
47. Peroxisome proliferator-activated receptors alpha and gamma are activated by indomethacin and other non-steroidal anti-inflammatory drugs
48. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones
49. Non thiazolidinedione antihyperglycaemic agents. 1:α-hetero atom substituted β-phenylpropanoic acids
50. Sensitization of diabetic and obese mice to insulin by retinoid X receptor agonists
51. Induction of the fatty acid transport protein 1 and acyl-coa synthase genes by dimer-selective rexinoids suggests that the peroxisome proliferator-activated receptor-retinoid X receptor heterodimer is their molecular target
52. Peroxisome proliferator-activated receptor gene expression in human tissues: Effects of obesity, weight loss, and regulation by insulin and glucocorticoids
53. Tissue distribution and quantification of the expression of mRNAS of peroxisome proliferator-activated receptors and liver X receptor α in humans
54. Skeletal muscle peroxisome proliferator-activated receptor-γ expression in obesity and non-insulin-dependent diabetes mellitus
55. Chromosomal localization and partial genomic structure of the human peroxisome proliferator activated receptor-gamma (hPPARγ) gene
56. A genetic polymorphism of the peroxisome proliferator-activated receptor γ gene influences plasma leptin levels in obese humans
57. Molecular scanning of the human peroxisome proliferator activated receptor γ gene in diabetic caucasians: Identification of a pro12Ala PPARγ2 missense mutation
58. Association of the pro12Ala variant in the peroxisome proliferator-activated receptor γ2 gene with obesity in two caucasian populations
59. Effect of the pro12Ala variant of the human peroxisome proliferator-activated receptor γ2 gene on adiposity, fat distribution, and insulin sensitivity in Japanese men
60. Pro12Ala missense mutation of the peroxisome proliferator activated receptor gamma and diabetes mellitus
61. A pro12Ala substitution in PPARγ2 associated with decreased receptor activity, lower body mass index and improved insulin sensitivity
62. Inhibitory effect of a proline- to-alanine substitution at codon 12 of peroxisome proliferator activated receptor γ2 on thiazolidinedione-induced adipogenesis
63. Obesity associated with a mutation in a genetic regulator of adipocyte differentiation
64. Dominant negative mutations in human PPARγ associated with severe insulin resistance, diabetes mellitus, and hypertension
65. PPARγ is required for differentiation of adipose tissue in vivo and in vitro
66. PPARγ mediates high fat diet-induced adipocyte hypertrophy and insulin resistance
67. The effect of CP 68, 722, a thiazolidinedione derivative, on insulin sensitivity in lean and obese zucker rats
68. Characterization of new oral antidiabetic agent CS-045. Studies in KK and ob/ob mice and zucker fatty rats
69. Repeat treatment of obese mice with BRL 49653, a new and potent insulin sensitizer, enhances insulin action in white adipocytes
70. Pioglitazone increases insulin sensitivity, reduces blood glucose, insulin, and lipid levels, and lowers blood pressure in obese, insulin-resistant rhesus monkeys
71. A New Antidiabetic Agent, BRL 49653, Reduces Lipid Availability and Improves Insulin Action and Glucoregulation in the Rat
72. Role of Skeletal Muscle in Thiazolidinedione Insulin Sensitizer Action
73. Troglitazone Increases the Number of Small Adipocytes Without the Changes of White Adipose Tissue Mass in Obese Zucker Rats
74. Glucose Transport Deficiency in Diabetic Animals Is Corrected by Treatment with the Oral Antihyperglycemic Agent Pioglitazone
75. The Antihyperglycemic Agent Englitazone Prevents the Defect in Glucose Transport in Rats Fed a High-Fat Diet
76. Treatment with the Thiazolidinedione (BRL 49653) Decreases Insulin Resistance in Obese Zucker Hindlimb
77. Effects of Thiazolidinediones on Glucocorticoid-Induced Insulin Resistance and GLUT4 Glucose Transporter Expression in Rat Skeletal Muscle
78. Pioglitazone Improves Insulin Signaling Defects in Skeletal Muscle from Wistar Fatty, (γa/γa) Rats
79. An Antidiabetic Thiazolidinedione Potentiates Insulin Stimulation of Glycogen Synthase in Rat Adipose Tissue
80. Troglitazone Action Is Independent of Adipose Tissue
81. Potentiation Insulin Stimulation of Phosphatidylinositol 3-Kinase by Thiazolidinedione-Derived Antidiabetic Agents in Chinese Hamster Ovary Cells Expressing Human Insulin Receptor and L6 Myotubes
82. Possibility of distinct insulin signaling pathways beyond phosphatidyinositol 3-kinase mediating glucose transport and lipogenesis
83. The New Antidiabetic Drug MCC-555 Acutely Sensitizes Insulin Signaling in Isolated Cardiomyocytes
84. Tumour Necrosis Factor α: A Key Component of the Obesity-Diabetes Link
85. Antidiabetic Thiazolidinediones Block the Inhibitory Effect of Tumor Necrosis Factor-α on Differentiation, Insulin-Stimulated Glucose Uptake, and Gene Expression in 3T3-L1 Cells
86. BRL 49653 Blocks the Lipolytic Actions of Tumor Necrosis Factor-α: A Potential New Insulin Sensitizing Mechanism for Thiazolidinediones
87. TNF-α Induced Insulin Resistance In Vivo and Its Prevention by Troglitazone
88. PPARγ2 Regulates Adipose Expression of the Phosphoenolpyruvate Carboxykinase Gene
89. PPARalpha and PPARgamma Activators Direct a Distinct Tissue-Specific Transcriptional Response via a PPRE in the Lipoprotein Lipase Gene
90. Altered Gene Expression for Tumour Necrosis Factor-A and Its Receptors During Drug and Dietary Modulation of Insulin Resistance
91. Peroxisome Proliferator-Activated Receptors α and γ- Mediate In Vivo Regulation of Uncoupling Protein (UCP1, UCP2, UCP3) gene expression
92. The Peroxisome Proliferator-Activated Receptor-Gamma Is a Negative Regulator of Macrophage Activation
93. PPAR-Gamma Agonists Inhibit Production of Monocyte Inflammatory Cytokines
94. The Peroxisome Proliferator-Activated Receptory as a Regulator of Monocyte/Macrophage Function
95. Activation of Peroxisome Proliferator-Activated Receptor γ Does Not Inhibit IL-6 or TNF-A Responses of Macrophages to LPS In Vitro or In Vivo
96. Macrophages in Human Atheroma Contain PPARγ
97. Expression and Function of PPARγ in Rat and Human Vascular Smooth Muscle Cells
98. Peroxisome Proliferator-Activated Receptor Gamma Activators Inhibit Gene Expression and Migration in Human Vascular Smooth Muscle Cells
99. Modulation of Vascular Inflammation In Vitro and In Vivo by Peroxisome Proliferator-Activated Receptor-γ Activators
100. Differentiation and Reversal of Malignant Changes in Colon Cancer Through Pparγ
101. Aspirin Use and Potential Mechanisms for Colorectal Cancer Prevention
102. Activation of Peroxisome Proliferator Activated Receptor-γ Promotes the Development of Colon Tumors in C57BL/6J-Apcmin/+mice
103. Activation of PPARγ Leads to Inhibition of Anchorage-Independent Growth of Human Colorectal Cells
104. Terminal Differentiation of Human Breast Cancer Through PPAR Gamma
105. Peroxisome Proliferator-Activated Receptor Gamma Ligands Are Potent Inhibitors of Angiogenesis In Vitro and In Vivo
106. Subchronic Toxicity of the Antidiabetic Troglitazone in Wistar Rats
107. Rosiglitazone: A New Therapy for Type 2 Diabetes
108. Prospects for Primary Prevention of Type II or Non-insulin-dependent Diabetes Mellitus
109. Glucose Control and Insulin Resistance in Non-Insulin-Dependent Diabetes Mellitus
110. Thiazolidinediones in The Treatment of Insulin Resistance and Type II Diabetes
111. Pathogenesis of non-insulin-Dependent (type II) diabetes
112. The Deadly Quartet - The Insulin Resistance Syndrome
113. Intensive Blood-Glucose Control with Sulphonylureas or Insulin Compared with Conventional Treatment and Risk of Complications in Patients with Type 2 Diabetes (UKPDS 33)
114. Peroxisome Proliferator-Activated Receptor-γ Agonist, Rosiglitazone, Protects Against Nephropathy and Pancreatic Islet Abnormalities in Zucker Fatty Rrts
115. Thiazolidinediones
116. The Synthesis of BRL 49653 - A Novel and Potent Antihyperglycemic Agent
117. An Antidiabetic Thiazolidinedione Is a High Affinity Ligand for Peroxisome Proliferator-Activated Receptor γ (PPARγ)
118. Rosiglitazone Monotherapy: Improves Glycemic Control in Patients with Type 2 Diabetes: A 12-Week Randomized, Placebo-Controlled Study
119. Troglitazone, an Insulin Action Enhancer, Improves Metabolic Control in NIDDM Patients
120. The Bioavailability of Rosiglitazone Is Unaltered by Food
121. The Rosiglitazone 011 Study Group. Rosiglitazone (BRL 49653) Monotherapy Has Significant Glucose Lowering Effect in Type 2 Diabetic Patients
122. Low Dose Rosiglitazone Provides Additional Glycaemic Control When Combined with Sulfonylureas in Type 2 Diabetes
123. Once Daily Rosiglitazone in Combination with Metformin Effectively Reduces Hyperglycemia in Patients with Type 2 Diabetes
124. Effect of Troglitazone in Insulin-Treated Patients with Type II Diabetes Mellitus
125. Rosiglitazone Improves Glycemic Control in Poorly Controlled, Insulin-Treated Type 2 Diabetes
126. Pioglitazone is Effective in the Treatment of Patients with Type 2 Diabetes
127. The Effect of Pioglitazone on Glucose Control and Lipid Profile in Patients with Type 2 Diabetes
128. The Effect of Combination Therapy with Pioglitazone and Sulfonylurea on the Lipid Profile in Patients with Type 2 Diabetes
129. Combination Therapy with Pioglitazone and Sulfonylurea in Patients with Type 2 Diabetes
130. Adding Pioglitazone to Metformin Therapy Improves Lipid Profile in Patients with Type 2 Diabetes
131. Combination Therapy With Pioglitazone and Metformin in Patients with Type 2 Diabetes
132. Combination Therapy with Pioglitazone and Insulin in Patients with Type 2 Diabetes
133. Analysis of Estrogen Receptor Function in vitro Reveals Three Distinct Classes of Antiestrogens