Peroxisome proliferator-activated receptor gamma (PPARγ) is emerging as a major regulator in neurological diseases. However, the role of (PPARγ) and its co-regulators in cerebrovascular endothelial dysfunction after stroke is unclear. Here, we have demonstrated that (PPARγ) activation by pioglitazone significantly inhibited both oxygen-glucose deprivation-induced cerebral vascular endothelial c...

Peroxisome proliferator-activated receptor-γ (PPARγ), a ligand-activated transcription factor, has protective roles in the cerebral circulation and is highly activated during pregnancy. Thus, we hypothesized that PPARγ is involved in the adaptation of cerebral vasculature to pregnancy. Non-pregnant (NP) and late-pregnant (LP) rats were treated with a specific PPARγ inhibitor GW9662 (10 ]mg/kg/d...

Conformational change in helix 12 can alter ligand-induced PPARγ activity; based on this reason, isoquinolinoquinazolinones, structural homologs of berberine, were designed and synthesized as PPARγ antagonists. Computational docking and mutational study indicated that isoquinolinoquinazolinones form hydrogen bonds with the Cys285 and Arg288 residues of PPARγ. Furthermore, SPR results demonstrat...

PPARγ is a target for insulin-sensitizing drugs such as glitazones, which improve plasma glucose maintenance in patients with diabetes. Synthetic ligands have been designed to mimic endogenous ligand binding to a canonical ligand-binding pocket to hyperactivate PPARγ. Here we reveal that synthetic PPARγ ligands also bind to an alternate site, leading to unique receptor conformational changes th...

Prostaglandin D2 (PGD2) has been demonstrated to have antitumor effects on cancer cells. PGD2 acts through two major receptors of DP1 and DP2, as well as through the peroxisome proliferator-activated receptor γ (PPARγ) via the PGD2 metabolite, 15-deoxy-Δ12-14-PGJ2. The expression levels of DP1, DP2, and PPARγ were analyzed by immunohistochemistry on 277 primary gastric carcinomas. Either DP1- o...

background: peroxisome proliferator activated receptor gamma (pparγ), a member of nuclear receptor superfamily, comprises two isoforms in mouse. these two isoforms are encoded by different mrnas, which are arisen by alternative promoter usage. there are two promoter regions upstream of pparγ gene. a 3 kb fragment, containing several transcription factor binding sites, acts as pparγ1 promoter re...

Trans-3,5-dimethoxy-4'-hydroxystilbene (PTER), a natural dimethylated analog of resveratrol, preferentially induces certain cancer cells to undergo apoptosis and could thus have a role in cancer chemoprevention. Peroxisome proliferator-activated receptor γ (PPARγ), a member of the nuclear receptor superfamily, is a ligand-dependent transcription factor whose activation results in growth arrest ...

Peroxisome proliferator-activated receptor gamma (PPARγ) is a ligand-activated transcription factor that was originally identified as a regulator of peroxisome proliferation and adipocyte differentiation. Emerging evidence suggests that functional PPARγ signaling also occurs within the hypothalamus. However, the exact distribution and identities of PPARγ-expressing hypothalamic cells remains un...

The nuclear hormone receptor peroxisome proliferator-activated receptor γ (PPARγ) is a ligand-dependent transcription factor of increasing importance in cardiovascular physiology. Treatment of type II diabetes patients with thiazolidinediones (TZD), synthetic ligands of PPARγ, improves insulin sensitivity and also lowers blood pressure despite increased water and salt retention by the kidneys. ...