publication . Other literature type . Article . 2013

Thiazolidinediones are acute, specific inhibitors of the mitochondrial pyruvate carrier

Divakaruni A. S.; Wiley S. E.; Rogers G. W.; Andreyev A. Y.; Petrosyan S.; Loviscach M.; Wall E. A.; Yadava N.; Heuck A. P.; Ferrick D. A.; ...
Open Access English
  • Published: 19 Mar 2013
  • Publisher: National Academy of Sciences
Abstract
Facilitated pyruvate transport across the mitochondrial inner membrane is a critical step in carbohydrate, amino acid, and lipid metabolism. We report that clinically relevant concentrations of thiazolidinediones (TZDs), a widely used class of insulin sensitizers, acutely and specifically inhibit mitochondrial pyruvate carrier (MPC) activity in a variety of cell types. Respiratory inhibition was overcome with methyl pyruvate, localizing the effect to facilitated pyruvate transport, and knockdown of either paralog, MPC1 or MPC2, decreased the EC50 for respiratory inhibition by TZDs. Acute MPC inhibition significantly enhanced glucose uptake in human skeletal musc...
Subjects
free text keywords: Biological Sciences, Multidisciplinary, Membrane transport protein, biology.protein, biology, Glucose uptake, Pyruvate transport, Inner mitochondrial membrane, Biochemistry, Pyruvate dehydrogenase kinase, PKM2, Cellular respiration, Insulin, medicine.medical_treatment, medicine
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publication . Other literature type . Article . 2013

Thiazolidinediones are acute, specific inhibitors of the mitochondrial pyruvate carrier

Divakaruni A. S.; Wiley S. E.; Rogers G. W.; Andreyev A. Y.; Petrosyan S.; Loviscach M.; Wall E. A.; Yadava N.; Heuck A. P.; Ferrick D. A.; ...