Insulin sensitizer; enhances insulin sensitivity and lowers blood-glucose levels in diabetic mouse models. Inhibits mitochondria pyruvate carriers; increases mitochondrial respiration rates, leading to a reduction in expression of lipogenic enzymes. Suppresses gluconeogenesis and lipogenesis in primary hepatocytes. Exhibits low binding affinity and activity at PPARγ
= 23.7 μ
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Identification of a mitochondrial target of thiazolidinedione insulin sensitizers (mTOT) relationship to newly identified mitochondrial pyruvate carrier proteins.
Colca et al.
PLoS One, 2013;8:e61551
Thiazolidinediones are acute, specific inhibitors of the mitochondrial pyruvate carrier.
Divakaruni et al.
Insulin resistance and metabolic derangements in obese mice are ameliorated by a novel peroxisome proliferator-activated receptor γ-sparing thiazolidinedione.
Chen et al.