Thiazolidinediones and the promise of insulin sensitization in type 2 diabetes

RE Soccio, ER Chen, MA Lazar - Cell metabolism, 2014 - cell.com
Type 2 diabetes is caused by insulin resistance coupled with an inability to produce enough
insulin to control blood glucose, and thiazolidinediones (TZDs) are the only current …

Functional regulation of PPARs through post-translational modifications

R Brunmeir, F Xu - International journal of molecular sciences, 2018 - mdpi.com
Peroxisome proliferator-activated receptors (PPARs) belong to the nuclear receptor
superfamily and they are essential regulators of cell differentiation, tissue development, and …

Transcriptional regulation of adipogenesis

PM de Sá, AJ Richard, H Hang… - Comprehensive …, 2011 - Wiley Online Library
Adipocytes are the defining cell type of adipose tissue. Once considered a passive
participant in energy storage, adipose tissue is now recognized as a dynamic organ that …

PPARγ signaling and emerging opportunities for improved therapeutics

S Wang, EJ Dougherty, RL Danner - Pharmacological Research, 2016 - Elsevier
Peroxisome proliferator-activated receptor gamma (PPARγ) is a ligand-activated nuclear
receptor that regulates glucose and lipid metabolism, endothelial function and inflammation …

The impact of molecular dynamics on drug design: applications for the characterization of ligand–macromolecule complexes

J Mortier, C Rakers, M Bermudez, MS Murgueitio… - Drug discovery today, 2015 - Elsevier
Highlights•Which molecular dynamics (MD) techniques are available for drug design?•How
is MD used to investigate ligand–macromolecule complexes?•How are MD studies applied …

Review of the Structural and Dynamic Mechanisms of PPARγ Partial Agonism

AJ Kroker, JB Bruning - PPAR research, 2015 - Wiley Online Library
PPARγ (peroxisome proliferator activated receptor γ) is a ligand activated transcription factor
of the nuclear receptor superfamily that controls the expression of a variety of genes …

The therapeutic potential of inhibiting PPARγ phosphorylation to treat type 2 diabetes

RL Frkic, K Richter, JB Bruning - Journal of Biological Chemistry, 2021 - ASBMB
A promising approach for treating type 2 diabetes mellitus (T2DM) is to target the
Peroxisome Proliferator-Activated Receptor γ (PPARγ) transcription factor, which regulates …

Obesity-linked PPARγ S273 phosphorylation promotes insulin resistance through growth differentiation factor 3

JA Hall, D Ramachandran, HC Roh, JR DiSpirito… - Cell metabolism, 2020 - cell.com
The thiazolidinediones (TZDs) are ligands of PPARγ that improve insulin sensitivity, but their
use is limited by significant side effects. Recently, we demonstrated a mechanism wherein …

Novel thiazolidin-4-one benzenesulfonamide hybrids as PPARγ agonists: Design, synthesis and in vivo anti-diabetic evaluation

IH Ali, RM Hassan, AM El Kerdawy… - European Journal of …, 2024 - Elsevier
In the current study, two series of novel thiazolidin-4-one benzenesulfonamide arylidene
hybrids 9a-l and 10a-f were designed, synthesized and tested in vitro for their PPARɣ …

Thiazolidinediones and PPAR orchestra as antidiabetic agents: From past to present

S Yasmin, V Jayaprakash - European journal of medicinal chemistry, 2017 - Elsevier
Thiazolidinediones a class of drug, that provided a major breakthrough in the management
of type 2 diabetes since 1990. Following the discovery of PPARs, TZDs were the first class to …