产品描述:
The peroxisome proliferator-activated receptor-γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones (TZDs). TZDs are a group of structurally related synthetic PPARγ receptor agonists with antidiabetic actions in vivo.{7575,8930} There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.{8953,8224} However, only a few antagonists have been reported.{8241} T0070907 is a potent and selective antagonist of the human PPARγ with an apparent IC50 of 1 nM for the binding inhibition of rosiglitazone, a reference TZD. T0070907 covalently binds to Cys313 of PPARγ, inducing conformational changes that block the recruitment of transcriptional cofactors to the PPARγ/RXR heterodimer.{10311}