(Q36512559)

14 August 2017

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title

Investigational PPAR-gamma agonists for the treatment of Type 2 diabetes (English)

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14 August 2017

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Rajesh S Savkur

1

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14 August 2017

Anne R Miller

series ordinal

2

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14 August 2017

language of work or name

English

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publication date

1 July 2006

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Expert Opinion on Investigational Drugs

14 August 2017

published in

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14 August 2017

volume

15

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14 August 2017

issue

7

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14 August 2017

page(s)

763-778

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Global prevalence of diabetes: estimates for the year 2000 and projections for 2030

14 August 2017

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PPARs as targets for metabolic and cardiovascular diseases

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The PPARs: from orphan receptors to drug discovery

21 January 2018

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PPARs: therapeutic targets for metabolic disease

21 January 2018

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Therapeutic roles of peroxisome proliferator-activated receptor agonists

21 January 2018

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An adipogenic cofactor bound by the differentiation domain of PPARgamma

21 January 2018

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The mechanisms of action of PPARs

21 January 2018

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Convergence of 9-cis retinoic acid and peroxisome proliferator signalling pathways through heterodimer formation of their receptors

21 January 2018

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The RXR heterodimers and orphan receptors

21 January 2018

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cDNA cloning, chromosomal mapping, and functional characterization of the human peroxisome proliferator activated receptor

21 January 2018

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Fatty acids activate a chimera of the clofibric acid-activated receptor and the glucocorticoid receptor

21 January 2018

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Activation of proliferator-activated receptors alpha and gamma induces apoptosis of human monocyte-derived macrophages

21 January 2018

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Differential expression of peroxisome proliferator-activated receptors (PPARs): tissue distribution of PPAR-alpha, -beta, and -gamma in the adult rat

21 January 2018

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Tissue distribution and quantification of the expression of mRNAs of peroxisome proliferator-activated receptors and liver X receptor-alpha in humans: no alteration in adipose tissue of obese and NIDDM patients

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Expression of peroxisome proliferator-activated receptor alpha (PPAR alpha) in primary cultures of human vascular endothelial cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Activation of human aortic smooth-muscle cells is inhibited by PPARalpha but not by PPARgamma activators

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Differential gene regulation in human versus rodent hepatocytes by peroxisome proliferator-activated receptor (PPAR) alpha. PPAR alpha fails to induce peroxisome proliferation-associated genes in human cells independently of the level of receptor ex

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

PPAR-alpha and PPAR-gamma activators induce cholesterol removal from human macrophage foam cells through stimulation of the ABCA1 pathway

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Coordinate regulation of the expression of the fatty acid transport protein and acyl-CoA synthetase genes by PPARalpha and PPARgamma activators

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Expression of putative fatty acid transporter genes are regulated by peroxisome proliferator-activated receptor alpha and gamma activators in a tissue- and inducer-specific manner

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Co-ordinate induction of hepatic mitochondrial and peroxisomal carnitine acyltransferase synthesis by diet and drugs

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Control of human muscle-type carnitine palmitoyltransferase I gene transcription by peroxisome proliferator-activated receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

A critical role for the peroxisome proliferator-activated receptor alpha (PPARalpha) in the cellular fasting response: the PPARalpha-null mouse as a model of fatty acid oxidation disorders

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Peroxisome proliferator-activated receptor alpha mediates the adaptive response to fasting

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Targeted disruption of the alpha isoform of the peroxisome proliferator-activated receptor gene in mice results in abolishment of the pleiotropic effects of peroxisome proliferators

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Alterations in lipoprotein metabolism in peroxisome proliferator-activated receptor alpha-deficient mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Altered constitutive expression of fatty acid-metabolizing enzymes in mice lacking the peroxisome proliferator-activated receptor alpha (PPARalpha)

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Fibrates, dyslipoproteinaemia and cardiovascular disease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Acute (24 h) activation of peroxisome proliferator-activated receptor-alpha (PPARalpha) reverses high-fat feeding-induced insulin hypersecretion in vivo and in perifused pancreatic islets

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Potential role of peroxisome proliferator-activated receptor-alpha in the modulation of glucose-stimulated insulin secretion

21 January 2018

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Peroxisome proliferator-activated receptor (PPAR)-alpha activation lowers muscle lipids and improves insulin sensitivity in high fat-fed rats: comparison with PPAR-gamma activation

21 January 2018

1 reference

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Peroxisome proliferator-activated receptor-alpha agonist treatment in a transgenic model of type 2 diabetes reverses the lipotoxic state and improves glucose homeostasis.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

WY14,643, a peroxisome proliferator-activated receptor alpha (PPARalpha ) agonist, improves hepatic and muscle steatosis and reverses insulin resistance in lipoatrophic A-ZIP/F-1 mice.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Human and rat peroxisome proliferator activated receptors (PPARs) demonstrate similar tissue distribution but different responsiveness to PPAR activators

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Cloning of a protein that mediates transcriptional effects of fatty acids in preadipocytes. Homology to peroxisome proliferator-activated receptors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Activation of PPARdelta alters lipid metabolism in db/db mice.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Peroxisome-Proliferator-Activated Receptor δ Activates Fat Metabolism to Prevent Obesity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Activation of peroxisome proliferator-activated receptor delta induces fatty acid beta-oxidation in skeletal muscle and attenuates metabolic syndrome

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

The peroxisome proliferator-activated receptor beta/delta agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Direct activation of glucose transport in primary human myotubes after activation of peroxisome proliferator-activated receptor delta

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

cDNA cloning and characterization of the transcriptional activities of the hamster peroxisome proliferator-activated receptor haPPAR gamma

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Molecular cloning, expression and characterization of human peroxisome proliferator activated receptors gamma 1 and gamma 2

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

The organization, promoter analysis, and expression of the human PPARgamma gene

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

PPARgamma3 mRNA: a distinct PPARgamma mRNA subtype transcribed from an independent promoter

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Expression of the peroxisome proliferator-activated receptor gamma (PPARgamma) in human atherosclerosis and regulation in macrophages by colony stimulating factors and oxidized low density lipoprotein

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Adipocyte-specific transcription factor ARF6 is a heterodimeric complex of two nuclear hormone receptors, PPAR gamma and RXR alpha

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Stimulation of adipogenesis in fibroblasts by PPAR gamma 2, a lipid-activated transcription factor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Induction of the acyl-coenzyme A synthetase gene by fibrates and fatty acids is mediated by a peroxisome proliferator response element in the C promoter

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Troglitazone inhibits formation of early atherosclerotic lesions in diabetic and nondiabetic low density lipoprotein receptor-deficient mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Peroxisome proliferator-activated receptor gamma ligands inhibit development of atherosclerosis in LDL receptor-deficient mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

The selective peroxisomal proliferator-activated receptor-gamma agonist has an additive effect on plaque regression in combination with simvastatin in experimental atherosclerosis: in vivo study by high-resolution magnetic resonance imaging

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

TNF-alpha-induced insulin resistance in vivo and its prevention by troglitazone

21 January 2018

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The hormone resistin links obesity to diabetes

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

The effect of thiazolidinediones on plasma adiponectin levels in normal, obese, and type 2 diabetic subjects

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

PPARgamma ligands increase expression and plasma concentrations of adiponectin, an adipose-derived protein

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Role of skeletal muscle in thiazolidinedione insulin sensitizer (PPARgamma agonist) action

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Troglitazone induces GLUT4 translocation in L6 myotubes.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Enhanced insulin-stimulated glycogen synthesis in response to insulin, metformin or rosiglitazone is associated with increased mRNA expression of GLUT4 and peroxisomal proliferator activator receptor gamma co-activator 1.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Peroxisome proliferator-activated receptor γ in diabetes and metabolism

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Peroxisome proliferator-activated receptor gamma and metabolic disease.

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

PPARgamma activators improve glucose homeostasis by stimulating fatty acid uptake in the adipocytes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

PPAR(gamma) and glucose homeostasis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Differential effects of rosiglitazone on skeletal muscle and liver insulin resistance in A-ZIP/F-1 fatless mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Adipose tissue is required for the antidiabetic, but not for the hypolipidemic, effect of thiazolidinediones

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Thiazolidinediones: a review of their mechanisms of insulin sensitization, therapeutic potential, clinical efficacy, and tolerability

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Thiazolidinediones in type 2 diabetes mellitus: current clinical evidence

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Lessons from the glitazones: a story of drug development

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Pioglitazone hydrochloride monotherapy improves glycemic control in the treatment of patients with type 2 diabetes: a 6-month randomized placebo-controlled dose-response study. The Pioglitazone 001 Study Group.

21 January 2018

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The impact of pioglitazone on glycemic control and atherogenic dyslipidemia in patients with type 2 diabetes mellitus

21 January 2018

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Rosiglitazone: a review of its use in the management of type 2 diabetes mellitus

21 January 2018

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Once- and twice-daily dosing with rosiglitazone improves glycemic control in patients with type 2 diabetes

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Nonhypoglycemic effects of thiazolidinediones

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Effect of rosiglitazone treatment on nontraditional markers of cardiovascular disease in patients with type 2 diabetes mellitus

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

A comparison of lipid and glycemic effects of pioglitazone and rosiglitazone in patients with type 2 diabetes and dyslipidemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Thiazolidinedione use, fluid retention, and congestive heart failure: a consensus statement from the American Heart Association and American Diabetes Association

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Thiazolidinediones, Peripheral Edema, and Type 2 Diabetes: Incidence, Pathophysiology, and Clinical Implications

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Possible heart failure exacerbation associated with rosiglitazone: case report and literature review

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Leukopenia and thrombocytopenia caused by thiazolidinediones

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Effect of thiazolidinediones on body weight in patients with diabetes mellitus

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Thiazolidinedione-induced congestive heart failure

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Vision loss due to macular edema induced by rosiglitazone treatment of diabetes mellitus

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Thiazolidinedione derivative improves fat distribution and multiple risk factors in subjects with visceral fat accumulation--double-blind placebo-controlled trial

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Effect of pioglitazone on abdominal fat distribution and insulin sensitivity in type 2 diabetic patients

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Collecting duct-specific deletion of peroxisome proliferator-activated receptor gamma blocks thiazolidinedione-induced fluid retention

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Thiazolidinediones expand body fluid volume through PPARgamma stimulation of ENaC-mediated renal salt absorption

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Pharmacological profile of a novel, non-TZD PPARgamma agonist

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Combination therapy with PPARgamma and PPARalpha agonists increases glucose-stimulated insulin secretion in db/db mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Fenofibrate prevents Rosiglitazone-induced body weight gain in ob/ob mice.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

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

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious gluco

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Muraglitazar, a dual (alpha/gamma) PPAR activator: a randomized, double-blind, placebo-controlled, 24-week monotherapy trial in adult patients with type 2 diabetes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Effect of muraglitazar on death and major adverse cardiovascular events in patients with type 2 diabetes mellitus

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

AZ 242, a novel PPARalpha/gamma agonist with beneficial effects on insulin resistance and carbohydrate and lipid metabolism in ob/ob mice and obese Zucker rats

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Structure of the PPARalpha and -gamma ligand binding domain in complex with AZ 242; ligand selectivity and agonist activation in the PPAR family

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Tesaglitazar, a dual PPAR{alpha}/{gamma} agonist, ameliorates glucose and lipid intolerance in obese Zucker rats

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Tesaglitazar, a novel dual peroxisome proliferator-activated receptor alpha/gamma agonist, dose-dependently improves the metabolic abnormalities associated with insulin resistance in a non-diabetic population

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Redox paradox: insulin action is facilitated by insulin-stimulated reactive oxygen species with multiple potential signaling targets

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

A peroxisome proliferator-activated receptor alpha/gamma dual agonist with a unique in vitro profile and potent glucose and lipid effects in rodent models of type 2 diabetes and dyslipidemia

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Reduction in glucagon receptor expression by an antisense oligonucleotide ameliorates diabetic syndrome in db/db mice

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Substituted indanylacetic acids as PPAR-alpha-gamma activators

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Antidiabetic and hypolipidemic potential of DRF 2519--a dual activator of PPAR-alpha and PPAR-gamma

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Identification of a series of PPAR gamma/delta dual agonists via solid-phase parallel synthesis

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Improved metabolic status and insulin sensitivity in obese fatty (fa/fa) Zucker rats and Zucker Diabetic Fatty (ZDF) rats treated with the thiazolidinedione, MCC-555.

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

A tailored therapy for the metabolic syndrome: the dual peroxisome proliferator-activated receptor-alpha/gamma agonist LY465608 ameliorates insulin resistance and diabetic hyperglycemia while improving cardiovascular risk factors in preclinical mode

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

PPAR ligands for metabolic disorders

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Molecular determinants for the tissue specificity of SERMs

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Coregulator function: a key to understanding tissue specificity of selective receptor modulators

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Ligand control of coregulator recruitment to nuclear receptors

21 January 2018

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https://api.crossref.org/works/10.1517%2F13543784.15.7.763

A unique PPARgamma ligand with potent insulin-sensitizing yet weak adipogenic activity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Studies on non-thiazolidinedione antidiabetic agents. 1. Discovery of novel oxyiminoacetic acid derivatives

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Distinct properties and advantages of a novel peroxisome proliferator-activated protein [gamma] selective modulator

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Selective PPARgamma modulators with improved pharmacological profiles

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

A new selective peroxisome proliferator-activated receptor gamma antagonist with antiobesity and antidiabetic activity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Gaining weight: the Keystone Symposium on PPAR and LXR.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Genetic modulation of PPARgamma phosphorylation regulates insulin sensitivity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

Peroxisome Proliferator-activated Receptor α Activators Improve Insulin Sensitivity and Reduce Adiposity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F13543784.15.7.763

10.1517/13543784.15.7.763

21 January 2018

Identifiers

DOI

1 reference

14 August 2017

1 reference