Discovery and development of selective PPARγ modulators as safe and effective antidiabetic agents

PAR-1622 is a selective peroxisome proliferator-activated receptor γ partial activator with preserved antidiabetic efficacy and broader safety profile for fluid retention

(2009) Mi-Kyung Kim et al.   ARCHIVES OF PHARMACAL RESEARCH

PPAR γ partial agonist, KR-62776, inhibits adipocyte differentiation via activation of ERK

(2009) J. Kim et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

A comparison of glycemic control, water retention, and musculoskeletal effects of balaglitazone and pioglitazone in diet-induced obese rats

(2009) Kim Henriksen et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

How safe is the use of thiazolidinediones in clinical practice?

(2009) CV Rizos et al.   Expert Opinion On Drug Safety

Discovery of a Peroxisome Proliferator Activated Receptor γ (PPARγ) Modulator with Balanced PPARα Activity for the Treatment of Type 2 Diabetes and Dyslipidemia

(2009) Weiguo Liu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic Acid (MK-0533): A Novel Selective Peroxisome Proliferator-Activated Receptor γ Modulator for the Treatment of Type 2 Diabetes Mellitus with a Reduced Potential to Increase Plasma and Extracellular Fluid Volume

(2009) John J. Acton et al.   JOURNAL OF MEDICINAL CHEMISTRY

INT131: A Selective Modulator of PPARγ

(2009) Alykhan Motani et al.   JOURNAL OF MOLECULAR BIOLOGY

Rosiglitazone evaluated for cardiovascular outcomes in oral agent combination therapy for type 2 diabetes (RECORD): a multicentre, randomised, open-label trial

(2009) Philip D Home et al.   LANCET

Nuclear Receptor-Coregulator Interaction Profiling Identifies TRIP3 as a Novel Peroxisome Proliferator-activated Receptor γ Cofactor

(2009) Arjen Koppen et al.   MOLECULAR & CELLULAR PROTEOMICS

MBX-102/JNJ39659100, a Novel Peroxisome Proliferator-Activated Receptor-Ligand with Weak Transactivation Activity Retains Antidiabetic Properties in the Absence of Weight Gain and Edema

(2009) Francine M. Gregoire et al.   MOLECULAR ENDOCRINOLOGY

MBX-102/JNJ39659100, a Novel Non-TZD Selective Partial PPAR- Agonist Lowers Triglyceride Independently of PPAR- Activation

(2009) Apurva Chandalia et al.   PPAR Research

Discovery of a novel class of PPARδ partial agonists

(2008) Barry G. Shearer et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Long-term use of thiazolidinediones and fractures in type 2 diabetes: a meta-analysis

(2008) Y. K. Loke et al.   CANADIAN MEDICAL ASSOCIATION JOURNAL

Peroxisome Proliferator-Activated Receptor γ Agonists as Insulin Sensitizers: From the Discovery to Recent Progress

(2008) Nobuo Cho et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

PPAR Modulators and PPAR Pan Agonists for Metabolic Diseases: The Next Generation of Drugs Targeting Peroxisome Proliferator-Activated Receptors?

(2008) P. Feldman et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Rosiglitazone and Risk of Cancer: A meta-analysis of randomized clinical trials

(2008) M. Monami et al.   DIABETES CARE

Rosiglitazone-Associated Fractures in Type 2 Diabetes: An analysis from A Diabetes Outcome Progression Trial (ADOPT)

(2008) S. E. Kahn et al.   DIABETES CARE

Dissociation of antihyperglycaemic and adverse effects of partial perioxisome proliferator-activated receptor (PPAR-γ) agonist balaglitazone

(2008) Philip J. Larsen et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

A novel selective peroxisome proliferator-activator receptor-γ modulator—SPPARγM5 improves insulin sensitivity with diminished adverse cardiovascular effects

(2008) Ching H. Chang et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

T2384, a Novel Antidiabetic Agent with Unique Peroxisome Proliferator-activated Receptor γ Binding Properties

(2008) Yang Li et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

In Vivo Imaging Reveals Selective Peroxisome Proliferator Activated Receptor Modulator Activity of the Synthetic Ligand 3-(1-(4-Chlorobenzyl)-3-t-butylthio-5-isopropylindol-2-yl)-2,2-dimethylpropanoic acid (MK-886)

(2008) A. Biserni et al.   MOLECULAR PHARMACOLOGY

Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent

(2008) D. R. Artis et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The genetic ablation of SRC-3 protects against obesity and improves insulin sensitivity by reducing the acetylation of PGC-1 

(2008) A. Coste et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Development of INT131 as a Selective PPAR Modulator: Approach to a Safer Insulin Sensitizer

(2008) Linda S. Higgins et al.   PPAR Research