Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone.
paper
Cited
Public
Unavailable
- Authors
- Sakamoto, J; Kimura, H; Moriyama, S; Odaka, H; Momose, Y; Sugiyama, Y; Sawada, H
- Year
- 2000
- Journal
- Biochemical and biophysical research communications
- PMID
- 11095972
- DOI
- 10.1006/bbrc.2000.3868
Pioglitazone, a thiazolidinedione (TZD) derivative, is an antidiabetic agent that improves hyperglycaemia and hyperlipidaemia in obese and diabetic animals via a reduction in hepatic and peripheral insulin resistance. The TZDs including pioglitazone have been identified as high affinity ligands for peroxisome proliferator-activated receptor (PPAR) gamma. The selectivity of pioglitazone for the human PPAR subtypes has not been reported, thus, we investigated the effect of pioglitazone on the human PPAR subtypes. Transient transactivation assay showed that pioglitazone is a selective hPPARgamma1 activator and a weak hPPARalpha activator. Binding assay indicated that the transactivation of hPPARgamma1 or hPPARalpha by pioglitazone is due to direct binding of pioglitazone to each subtype. Furthermore, pioglitazone significantly increased the apoA-I secretion from the human hepatoma cell line HepG2.
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| Changes in adiponectin receptor expression in muscle and adipose tissue of type 2 diabetic patients during rosiglitazone therapy. | Tan GD et al. | β | 2005 | β |
| Effects of the PPARgamma agonist pioglitazone on lipoprotein metabolism in patients with type 2 diabetes mellitus. | Nagashima K et al. | β | 2005 | β |
| Expression of PPAR, RXR isoforms and fatty acid transporting proteins in the rat and human gastrointestinal tracts. | Wang Q et al. | β | 2005 | β |
| Pioglitazone increases the fractional catabolic and production rates of high-density lipoproteins apo AI in the New Zealand White Rabbit. | CarreΓ³n-Torres E et al. | β | 2005 | β |
| Pioglitazone induces mitochondrial biogenesis in human subcutaneous adipose tissue in vivo. | Bogacka I et al. | β | 2005 | β |
| PPARalpha, but not PPARgamma, activators decrease macrophage-laden atherosclerotic lesions in a nondiabetic mouse model of mixed dyslipidemia. | Hennuyer N et al. | β | 2005 | β |
| PPAR-gamma activation fails to provide myocardial protection in ischemia and reperfusion in pigs. | Xu Y et al. | β | 2005 | β |
| Rosiglitazone and lipid metabolism. | Ferrannini E | β | 2005 | β |
| Subchronic exposure to high-dose ACE-inhibitor moexipril induces catalase activity in rat liver. | Adeghate E et al. | β | 2005 | β |
| The dual PPARalpha/gamma agonist, ragaglitazar, improves insulin sensitivity and metabolic profile equally with pioglitazone in diabetic and dietary obese ZDF rats. | Pickavance LC et al. | β | 2005 | β |
| The effects of rosiglitazone on fatty acid and triglyceride metabolism in type 2 diabetes. | Tan GD et al. | β | 2005 | β |
| The nonthiazolidinedione tyrosine-based peroxisome proliferator-activated receptor gamma ligand GW7845 induces apoptosis and limits migration and invasion of rat and human glioma cells. | Grommes C et al. | β | 2005 | β |
| The PPARdelta agonist GW0742X reduces atherosclerosis in LDLR(-/-) mice. | Graham TL et al. | β | 2005 | β |
| The PPAR genes, cardiovascular disease and the emergence of PPAR pharmacogenetics. | Cresci S | β | 2005 | β |
| Troglitazone, the peroxisome proliferator-activated receptor-gamma agonist, induces antiproliferation and redifferentiation in human thyroid cancer cell lines. | Park JW et al. | β | 2005 | β |
| A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes. | Sakamoto J et al. | β | 2004 | β |
| Beneficial effects of troglitazone on neutrophil dysfunction in multiple low-dose streptozotocin-induced diabetic mice. | Kannan Y et al. | β | 2004 | β |
| Comparison of the effects of pioglitazone and rosiglitazone on macrophage foam cell formation. | Hirakata M et al. | β | 2004 | β |
| Economic benefits of pioglitazone for treating patients with Type 2 diabetes. | Grossman LD et al. | β | 2004 | β |
| Effect of pioglitazone on endotoxin-induced decreases in hepatic drug-metabolizing enzyme activity and expression of CYP3A2 and CYP2C11. | Ueyama J et al. | β | 2004 | β |
| Effect of PPAR-gamma activation and inhibition on glucose-stimulated insulin release in INS-1e cells. | Santini E et al. | β | 2004 | β |
| Growth arrest by troglitazone is mediated by p27Kip1 accumulation, which results from dual inhibition of proteasome activity and Skp2 expression in human hepatocellular carcinoma cells. | Motomura W et al. | β | 2004 | β |
| Insulin resistance and cardiovascular disease: the role of PPARgamma activators beyond their anti-diabetic action. | Walcher D et al. | β | 2004 | β |
| Pharmacologic treatment of type 2 diabetic dyslipidemia. | Moon YS et al. | β | 2004 | β |
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| Pioglitazone prevents hepatic steatosis, fibrosis, and enzyme-altered lesions in rat liver cirrhosis induced by a choline-deficient L-amino acid-defined diet. | Kawaguchi K et al. | β | 2004 | β |
| Redifferentiation therapy for thyroid cancer. | Park JW et al. | β | 2004 | β |
| The possible role of peroxisome proliferator-activated receptor gamma in heart failure. | Ehara N et al. | β | 2004 | β |
| Thiazolidinediones. | Yki-JΓ€rvinen H | β | 2004 | β |
| Thiazolidinediones: comparison of long-term effects on glycemic control and cardiovascular risk factors. | Gegick CG et al. | β | 2004 | β |
| Thiazolidinediones increase arachidonic acid release and subsequent prostanoid production in a peroxisome proliferator-activated receptor gamma-independent manner. | Tsukamoto H et al. | β | 2004 | β |
| Transcriptional control of apolipoprotein A-I gene expression in diabetes. | Mooradian AD et al. | β | 2004 | β |
| A PPAR agonist improves TNF-alpha-induced insulin resistance of adipose tissue in mice. | Shibasaki M et al. | β | 2003 | β |
| Dose-dependent suppression of hyperlipidemia and intestinal polyp formation in Min mice by pioglitazone, a PPAR gamma ligand. | Niho N et al. | β | 2003 | β |
| Inhibition of MMP-9 expression by PPARgamma activators in human bronchial epithelial cells. | Hetzel M et al. | β | 2003 | β |
| Insulin sensitisation in the treatment of Type 2 diabetes. | Tadayyon M et al. | β | 2003 | β |
| Insulin sensitizers. | Zangeneh F et al. | β | 2003 | β |
| Peroxisome proliferator-activated receptor gamma activation counters the detrimental effect of Helicobacter pylori lipopolysaccharide on gastric mucin synthesis. | Slomiany BL et al. | β | 2003 | β |
| Pioglitazone, a peroxisome proliferator-activated receptor-gamma agonist, attenuates myocardial ischemia/reperfusion injury in a rat model. | Ito H et al. | β | 2003 | β |
| Pioglitazone reduces atherogenic dense LDL particles in nondiabetic patients with arterial hypertension: a double-blind, placebo-controlled study. | Winkler K et al. | β | 2003 | β |
| Ragaglitazar: the pharmacokinetics, pharmacodynamics, and tolerability of a novel dual PPAR alpha and gamma agonist in healthy subjects and patients with type 2 diabetes. | Skrumsager BK et al. | β | 2003 | β |
| Troglitazone stimulates IGF-binding protein-1 by a PPAR gamma-independent mechanism. | Hilding A et al. | β | 2003 | β |
| Apolipoprotein A-I expression in rats is not altered by troglitazone. | Mooradian AD et al. | β | 2002 | β |
| A prospective, randomized comparison of the metabolic effects of pioglitazone or rosiglitazone in patients with type 2 diabetes who were previously treated with troglitazone. | Khan MA et al. | β | 2002 | β |
| Differences in lipid profiles of patients given rosiglitazone followed by pioglitazone. | LaCivita KA et al. | β | 2002 | β |
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| Effects of gemfibrozil on insulin resistance to fat metabolism in subjects with type 2 diabetes and hypertriglyceridaemia. | Whitelaw DC et al. | β | 2002 | β |
| Insulin resistance, diabetes, and atherosclerosis: thiazolidinediones as therapeutic interventions. | Raji A et al. | β | 2002 | β |
| New solutions for type 2 diabetes mellitus: the role of pioglitazone. | Grossman LD | β | 2002 | β |
| Novel 5-substituted-1H-tetrazole derivatives as potent glucose and lipid lowering agents. | Momose Y et al. | β | 2002 | β |
| Novel 5-substituted 2,4-thiazolidinedione and 2,4-oxazolidinedione derivatives as insulin sensitizers with antidiabetic activities. | Momose Y et al. | β | 2002 | β |
| Peroxisome proliferator-activated receptor gamma agonist ligands stimulate a Th2 cytokine response and prevent acute colitis. | Saubermann LJ et al. | β | 2002 | β |
| PPAR activators as antiinflammatory mediators in human T lymphocytes: implications for atherosclerosis and transplantation-associated arteriosclerosis. | Marx N et al. | β | 2002 | β |
| Roles of peroxisome proliferator-activated receptor gamma in cardiovascular disease. | Takano H et al. | β | 2002 | β |
| Toxicological consequences of altered peroxisome proliferator-activated receptor gamma (PPARgamma) expression in the liver: insights from models of obesity and type 2 diabetes. | Boelsterli UA et al. | β | 2002 | β |
| Troglitazone: a possible modulator of ovarian steroidogenesis. | Mitwally MF et al. | β | 2002 | β |
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