Type 2 diabetes is one of the most significant global health concerns: around 400 million people are affected and 5.1 million people died of type 2 diabetes and its complication in 2013.
-> Urgent need to find new types of drugs.
Thiazolidinediones (TZDs) are insulin sensitizers that act through activation of peroxisome proliferator-activated receptor-γ (PPARγ) and are highly effective oral medications for type 2 diabetes. However, their unique benefits are ruined by the risk for sodium and fluid retention, weight gain/lipid storage, bone loss and fractures and congestive heart failure. Most of them were withdrawn from the market.
HOW IT WORKS
New class of organic small molecules, partial PPAR-ɣ agonists (different than TZDs that are full agonist of PPAR-ɣ). Their singular interaction with the PPAR ligand binding domain provide them with unique properties.
In vitro results:
40 analogues synthesized, 1 lead
In vitro model: luminescence (PPARg GAL4 reporter assay)
Type 2 Diabetes
Nonalcoholic fatty liver disease (NAFLD) / nonalcoholic steatohepatitis (NASH) and hepatic fibrosis
Other potential applications: Cancer, Alzheimer’s disease, Asthma…