Cited by 310Metabolism, Diabetes, and CancerMitochondrial Function and PathologyAdipose Tissue and Metabolism

The DOI matches its Crossref record; 59 of the 59 references it cites were found in a registry or an index.

Thiazolidinediones are acute, specific inhibitors of the mitochondrial pyruvate carrier

Open access

Divakaruni, Ajit S., Wiley, Sandra E., Rogers, George W., Andreyev, Alexander Y., Petrosyan, Susanna, Loviscach, Mattias, Wall, Estelle A., Yadava, Nagendra, Heuck, Alejandro P., Ferrick, David A., Henry, Robert R., McDonald, William G., Colca, Jerry R., Simon, Melvin I., Ciaraldi, Theodore P., Murphy, Anne N.·2013·Proceedings of the National Academy of Sciences

DOI 10.1073/pnas.1303360110PMC PMC3619368

Open this paper in CoChat — free account Open PDF

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 EC 50 for respiratory inhibition by TZDs. Acute MPC inhibition significantly enhanced glucose uptake in human skeletal muscle myocytes after 2 h. These data ( i ) report that clinically used TZDs inhibit the MPC, ( ii ) validate that MPC1 and MPC2 are obligatory components of facilitated pyruvate transport in mammalian cells, ( iii ) indicate that the acute effect of TZDs may be related to insulin sensitization, and ( iv ) establish mitochondrial pyruvate uptake as a potential therapeutic target for diseases rooted in metabolic dysfunction.

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Integrity signals

Registry

Crossref · 10.1073/pnas.1303360110

Cites

59 of 59 references verified0 citation errors · 0 not checkable

Statistics

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

An Antidiabetic Thiazolidinedione Is a High Affinity Ligand for Peroxisome Proliferator-activated Receptor γ (PPARγ)
Lehmann, J. M., Moore, L. B., Smith-Oliver, T. A., Wilkison, W. O., Willson, T. M., & Kliewer, S. A. (1995) · Journal of Biological Chemistry · doi:10.1074/jbc.270.22.12953 · Cited by 3,645
The Anti-diabetic Drugs Rosiglitazone and Metformin Stimulate AMP-activated Protein Kinase through Distinct Signaling Pathways
Fryer, L. G. D., Patel, A. P., & Carling, D. (2002) · Journal of Biological Chemistry · doi:10.1074/jbc.m202489200 · Cited by 1,035
Anti-diabetic drugs inhibit obesity-linked phosphorylation of PPARγ by Cdk5
Choi, J. H., Banks, A. S., Estall, J. L., Kajimura, S., Boström, P., Laznik, D., Ruas, J. L., Chalmers, M. J., Kamenecka, T. M., Blüher, M., et al. (2010) · Nature · doi:10.1038/nature09291 · Cited by 897
A Mitochondrial Pyruvate Carrier Required for Pyruvate Uptake in Yeast, Drosophila , and Humans
Bricker, D. K., Taylor, E. B., Schell, J. C., Orsak, T., Boutron, A., Chen, Y.-C., Cox, J. E., Cardon, C. M., Van Vranken, J. G., Dephoure, N., et al. (2012) · Science · doi:10.1126/science.1218099 · Cited by 843
Use of Cells Expressing γ Subunit Variants to Identify Diverse Mechanisms of AMPK Activation
Hawley, S. A., Ross, F. A., Chevtzoff, C., Green, K. A., Evans, A., Fogarty, S., Towler, M. C., Brown, L. J., Ogunbayo, O. A., Evans, A. M., et al. (2010) · Cell Metabolism · doi:10.1016/j.cmet.2010.04.001 · Cited by 773
Identification and Functional Expression of the Mitochondrial Pyruvate Carrier
Herzig, S., Raemy, E., Montessuit, S., Veuthey, J.-L., Zamboni, N., Westermann, B., Kunji, E. R. S., & Martinou, J.-C. (2012) · Science · doi:10.1126/science.1218530 · Cited by 747
Brain fuel metabolism, aging, and Alzheimer’s disease
Cunnane, S. C., Nugent, S., Roy, M., Courchesne‐Loyer, A., Croteau, É., Tremblay, S., Castellano, A., Pifferi, F., Bocti, C., Paquet, N., et al. (2010) · Nutrition · doi:10.1016/j.nut.2010.07.021 · Cited by 633
The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and inhibitors
Halestrap, A. P. (1975) · Biochemical Journal · doi:10.1042/bj1480085 · Cited by 543
Thiazolidinediones, Like Metformin, Inhibit Respiratory Complex I
Brunmair, B., Staniek, K., Gras, F., Scharf, N., Althaym, A., Clara, R., Roden, M., Gnaiger, E., Nohl, H., Waldhäusl, W., et al. (2004) · Diabetes · doi:10.2337/diabetes.53.4.1052 · Cited by 521
Risk of Acute Myocardial Infarction, Stroke, Heart Failure, and Death in Elderly Medicare Patients Treated With Rosiglitazone or Pioglitazone
Graham, D. J., Ouellet‐Hellstrom, R., MaCurdy, T. E., Ali, F. N., Sholley, C., Worrall, C. M., & Kelman, J. A. (2010) · JAMA · doi:10.1001/jama.2010.920 · Cited by 512

Flagged first, then by citations

Show all 58 references

Sorted by citations

Items 101–200 of 310

Deuterium‐Stabilized (R)‐Pioglitazone (PXL065) Is Responsible for Pioglitazone Efficacy in NASH yet Exhibits Little to No PPARγ Activity
Jacques, V., Bolze, S., Hallakou‐Bozec, S., Czarnik, A. W., Divakaruni, A. S., Fouqueray, P., Murphy, A. N., der Ploeg, L. H. T. V., & DeWitt, S. H. (2021) · Hepatology Communications · doi:10.1002/hep4.1723 · Cited by 51
Self-citation
MSDC-0602K, a metabolic modulator directed at the core pathology of non-alcoholic steatohepatitis
Colca, J. R., McDonald, W. G., & Adams, W. J. (2018) · Expert Opinion on Investigational Drugs · doi:10.1080/13543784.2018.1494153 · Cited by 49
Self-citation
Berberine Reduces Pyruvate-driven Hepatic Glucose Production by Limiting Mitochondrial Import of Pyruvate through Mitochondrial Pyruvate Carrier 1
Li, A., Liu, Q., Li, Q., Liu, B., Yang, Y., & Zhang, N. (2018) · EBioMedicine · doi:10.1016/j.ebiom.2018.07.039 · Cited by 49
Mitochondrial pyruvate carrier-mediated metabolism is dispensable for the classical activation of macrophages
Ran, L., Zhang, S., Wang, G., Zhao, P., Sun, J., Zhou, J., Gan, H., Jeon, R., Li, Q., Herrmann, J., et al. (2023) · Nature Metabolism · doi:10.1038/s42255-023-00800-3 · Cited by 49
An Insulin-Sensitizing Thiazolidinedione, Which Minimally Activates PPARγ, Does Not Cause Bone Loss
Fukunaga, T., Zou, W., Rohatgi, N., Colca, J. R., & Teitelbaum, S. L. (2014) · Journal of Bone and Mineral Research · doi:10.1002/jbmr.2364 · Cited by 45
Self-citation
Perfringolysin O Structure and Mechanism of Pore Formation as a Paradigm for Cholesterol-Dependent Cytolysins
Johnson, B. B., & Heuck, A. P. (2014) · Sub-cellular biochemistry/Subcellular biochemistry · doi:10.1007/978-94-017-8881-6_5 · Cited by 45
Self-citation
An ancestral role for the mitochondrial pyruvate carrier in glucose-stimulated insulin secretion
McCommis, K. S., Hodges, W. T., Bricker, D. K., Wisidagama, D. R., Compan, V., Remedi, M. S., Thummel, C. S., & Finck, B. N. (2016) · Molecular Metabolism · doi:10.1016/j.molmet.2016.06.016 · Cited by 44
Reverse engineering the cancer metabolic network using flux analysis to understand drivers of human disease
Badur, M. G., & Metallo, C. M. (2017) · Metabolic Engineering · doi:10.1016/j.ymben.2017.11.013 · Cited by 44
Pyruvate metabolism controls chromatin remodeling during CD4+ T cell activation
Mocholí, E., Russo, L., Gopal, K., Ramstead, A. G., Hochrein, S. M., Vos, H. R., Geeven, G., Adegoke, A., Hoekstra, A. T., van Es, R. M., et al. (2023) · Cell Reports · doi:10.1016/j.celrep.2023.112583 · Cited by 44
Glucagon up‐regulates hepatic mitochondrial pyruvate carrier 1 through cAMP‐responsive element‐binding protein; inhibition of hepatic gluconeogenesis by ginsenoside Rb1
Lou, M., Li, J., Cheng, Y., Xiao, N., Ma, G., Li, P., Liu, B., Liu, Q., & Qi, L. (2019) · British Journal of Pharmacology · doi:10.1111/bph.14758 · Cited by 43
Beta-cell mitochondrial carriers and the diabetogenic stress response
Brun, T., & Maechler, P. (2016) · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research · doi:10.1016/j.bbamcr.2016.03.012 · Cited by 46
Fifty years of the mitochondrial pyruvate carrier: New insights into its structure, function, and inhibition
Tavoulari, S., Sichrovsky, M., & Kunji, E. R. S. (2023) · Acta Physiologica · doi:10.1111/apha.14016 · Cited by 45
Investigating mitochondrial dysfunction in human lung cells exposed to redox-active PM components
Lavrich, K. S., Corteselli, E., Wages, P. A., Bromberg, P. A., Simmons, S. O., Gibbs-Flournoy, E. A., & Samet, J. M. (2018) · Toxicology and Applied Pharmacology · doi:10.1016/j.taap.2018.01.024 · Cited by 42
Novel N,N-dialkyl cyanocinnamic acids as monocarboxylate transporter 1 and 4 inhibitors
Jonnalagadda, S., Jonnalagadda, S. K., Ronayne, C. T., Nelson, G. L., Solano, L. N., Rumbley, J. N., Holy, J. M., Mereddy, V. R., & Drewes, L. R. (2019) · Oncotarget · doi:10.18632/oncotarget.26760 · Cited by 42
Diabetic silkworms for evaluation of therapeutically effective drugs against type II diabetes
Matsumoto, Y., Ishii, M., Hayashi, Y., Miyazaki, S., Sugita, T., Sumiya, E., & Sekimizu, K. (2015) · Scientific Reports · doi:10.1038/srep10722 · Cited by 42
Lightening up Light Therapy: Activation of Retrograde Signaling Pathway by Photobiomodulation
Kim, H. P. (2014) · Biomolecules & Therapeutics · doi:10.4062/biomolther.2014.083 · Cited by 41
ACE overexpression in myeloid cells increases oxidative metabolism and cellular ATP
Cao, D., Spivia, W. R., Veiras, L. C., Khan, Z., Peng, Z., Jones, A. E., Bernstein, E. A., Saito, S., Okwan-Duodu, D. K., Parker, S. J., et al. (2019) · Journal of Biological Chemistry · doi:10.1074/jbc.ra119.011244 · Cited by 41
Self-citation
Treating Hepatic Steatosis and Fibrosis by Modulating Mitochondrial Pyruvate Metabolism
McCommis, K. S., & Finck, B. N. (2019) · Cellular and Molecular Gastroenterology and Hepatology · doi:10.1016/j.jcmgh.2018.09.017 · Cited by 39
Stimulating basal mitochondrial respiration decreases doxorubicin apoptotic signaling in H9c2 cardiomyoblasts
Deus, C. M., Zehowski, C., Nordgren, K. K. S., Wallace, K. B., Skildum, A. J., & Oliveira, P. J. (2015) · Toxicology · doi:10.1016/j.tox.2015.05.001 · Cited by 39
Eicosapentaenoic acid (EPA) activates PPARγ signaling leading to cell cycle exit, lipid accumulation, and autophagy in human meibomian gland epithelial cells (hMGEC)
Kim, S. W., Rho, C. R., Kim, J., Xie, Y., Prince, R. C., Mustafa, K. M., Potma, E. O., Brown, D. J., & Jester, J. V. (2020) · The Ocular Surface · doi:10.1016/j.jtos.2020.04.012 · Cited by 40
Mitochondrial pyruvate carrier function in health and disease across the lifespan
Buchanan, J., & Taylor, E. (2020) · Biomolecules · doi:10.3390/biom10081162 · Cited by 40
Diabetogenic milieus induce specific changes in mitochondrial transcriptome and differentiation of human pancreatic islets
Brun, T., Li, N., Jourdain, A. A., Gaudet, P., Duhamel, D., Meyer, J., Bosco, D., & Maechler, P. (2015) · Human Molecular Genetics · doi:10.1093/hmg/ddv247 · Cited by 41
Key features of inhibitor binding to the human mitochondrial pyruvate carrier hetero-dimer
Tavoulari, S., Schirris, T. J. J., Mavridou, V., Thangaratnarajah, C., King, M. S., Jones, D. T. D., Ding, S., Fearnley, I. M., & Kunji, E. R. S. (2022) · Molecular Metabolism · doi:10.1016/j.molmet.2022.101469 · Cited by 38
Pioglitazone inhibits mitochondrial pyruvate metabolism and glucose production in hepatocytes
Shannon, C. E., Daniele, G., Galindo, C., Abdul-Ghani, M. A., DeFronzo, R. A., & Norton, L. (2016) · FEBS Journal · doi:10.1111/febs.13992 · Cited by 36
The metabolic syndrome, thiazolidinediones, and implications for intersection of chronic and inflammatory disease
Colca, J. R., & Scherer, P. E. (2021) · Molecular Metabolism · doi:10.1016/j.molmet.2021.101409 · Cited by 39
Self-citation
Mitochondrial pyruvate carrier inhibitors improve metabolic parameters in diet-induced obese mice
Hodges, W. T., Jarasvaraparn, C., Ferguson, D., Griffett, K., Gill, L. E., Chen, Y., Ilagan, M. X. G., Hegazy, L., Elgendy, B., Cho, K., et al. (2021) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2021.101554 · Cited by 38
Fenofibrate suppresses melanogenesis in B16-F10 melanoma cells via activation of the p38 mitogen-activated protein kinase pathway
Huang, Y., Liu, K.-C., Chiou, Y.-L., Yang, C., Chen, T.-H., Li, T., & Liu, L. (2013) · Chemico-Biological Interactions · doi:10.1016/j.cbi.2013.07.008 · Cited by 36
The TZD insulin sensitizer clue provides a new route into diabetes drug discovery
Colca, J. R. (2015) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2015.1100164 · Cited by 37
Self-citation
Protective Effect of PPARγAgonists on Cerebellar Tissues Oxidative Damage in Hypothyroid Rats
Baghcheghi, Y., Beheshti, F., Salmani, H., Soukhtanloo, M., & Hosseini, M. (2016) · Neurology Research International · doi:10.1155/2016/1952561 · Cited by 36
Paradoxical neuronal hyperexcitability in a mouse model of mitochondrial pyruvate import deficiency
De La Rossa, A., Laporte, M. H., Astori, S., Marissal, T., Montessuit, S., Sheshadri, P., Ramos-Fernández, E., Mendez, P., Khani, A., Quairiaux, C., et al. (2022) · eLife · doi:10.7554/elife.72595 · Cited by 38
Development of Novel Mitochondrial Pyruvate Carrier Inhibitors to Treat Hair Loss
Liu, X., Flores, A., Situ, L., Gu, W., Ding, H., Christofk, H. R., Lowry, W. E., & Jung, M. E. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01570 · Cited by 34
Novel thiazolidinedione analog reduces a negative impact on bone and mesenchymal stem cell properties in obese mice compared to classical thiazolidinediones
Beňová, A., Ferenčáková, M., Bardová, K., Funda, J., Procházka, J., Špoutil, F., Čajka, T., Dzubanova, M., Balcaen, T., Kerckhofs, G., et al. (2022) · Molecular Metabolism · doi:10.1016/j.molmet.2022.101598 · Cited by 35
Mitochondrial damage‐associated molecular patterns: A new insight into metabolic inflammation in type 2 diabetes mellitus
Wang, Y., Wang, J., Tao, S., Liang, Z., xie, R., Liu, N., Deng, R., Zhang, Y., Deng, D., & Jiang, G. (2023) · Diabetes/Metabolism Research and Reviews · doi:10.1002/dmrr.3733 · Cited by 36
Mitochondrial pyruvate carriers control airway basal progenitor cell function through glycolytic-epigenetic reprogramming
Li, Y., He, Y., Zheng, Q., Zhang, J., Pan, X., Zhang, X., Yuan, H., Wang, G., Liu, X., Zhou, X.-L., et al. (2024) · Cell stem cell · doi:10.1016/j.stem.2024.09.015 · Cited by 35
Age Related Bioenergetics Profiles in Isolated Rat Cardiomyocytes Using Extracellular Flux Analyses
Mdaki, K. S., Larsen, T. D., Weaver, L. J., & Baack, M. L. (2016) · PLoS ONE · doi:10.1371/journal.pone.0149002 · Cited by 33
Measurement of Mitochondrial Oxygen Consumption in Permeabilized Fibers of Drosophila Using Minimal Amounts of Tissue
Simard, C. J., Pelletier, G., Boudreau, L. H., Hébert-Chatelain, É., & Pichaud, N. (2018) · Journal of Visualized Experiments · doi:10.3791/57376 · Cited by 34
Redox Biology of Peroxisome Proliferator-Activated Receptor-γ in Pulmonary Hypertension
Tseng, V., Sutliff, R. L., & Hart, C. M. (2018) · Antioxidants and Redox Signaling · doi:10.1089/ars.2018.7695 · Cited by 34
ACE overexpression in myeloid cells increases oxidative metabolism and cellular ATP
Cao, D., Spivia, W. R., Veiras, L. C., Khan, Z., Peng, Z., Jones, A. E., Bernstein, E. A., Saito, S., Okwan-Duodu, D. K., Parker, S. J., et al. (2020) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(17)49895-4 · Cited by 33
Self-citation
Visualization of Nicotine Adenine Dinucleotide Redox Homeostasis with Genetically Encoded Fluorescent Sensors
Zhao, Y., Zhang, Z., Zou, Y., & Yang, Y. A. (2017) · Antioxidants and Redox Signaling · doi:10.1089/ars.2017.7226 · Cited by 33
Pharmacological induction of mitochondrial biogenesis as a therapeutic strategy for the treatment of type 2 diabetes
Zamora, M., Pardo, R., & Villena, J. A. (2015) · Biochemical Pharmacology · doi:10.1016/j.bcp.2015.06.032 · Cited by 32
Structure of mitochondrial pyruvate carrier and its inhibition mechanism
Zheng, H., Zhang, J., Xu, Y., Fine, E. J., Suomivuori, C., Dror, R. O., & Feng, L. (2025) · Nature · doi:10.1038/s41586-025-08667-y · Cited by 34
Immune Cell Metabolism in Systemic Lupus Erythematosus
Choi, S., Titov, A. A., Sivakumar, R., Li, W., & Morel, L. M. (2016) · Current Rheumatology Reports · doi:10.1007/s11926-016-0615-7 · Cited by 32
Evaluating biological activity of compounds by transcription factor activity profiling
Medvedev, A. V., Moeser, M., Medvedeva, L., Martsen, E., Granick, A., Raines, L. N., Zeng, M., Makarov, S., Houck, K. A., & Makarov, S. S. (2018) · Science Advances · doi:10.1126/sciadv.aar4666 · Cited by 31
Forces, Fluxes, and Fuels: Tracking mitochondrial metabolism by integrating measurements of membrane potential, respiration, and metabolites
Jones, A. E., Li, S., Acevedo, A., Veliova, M., Shirihai, O. S., Stiles, L., & Divakaruni, A. S. (2020) · American Journal of Physiology-Cell Physiology · doi:10.1152/ajpcell.00235.2020 · Cited by 33
Self-citation
Novel insulin sensitizer MSDC-0602K improves insulinemia and fatty liver disease in mice, alone and in combination with liraglutide
Kamm, D. R., Pyles, K. D., Sharpe, M. C., Healy, L. N., Colca, J. R., & McCommis, K. S. (2021) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2021.100807 · Cited by 32
Self-citation
Pioglitazone-induced AMPK-Glutaminase-1 prevents high glucose-induced pancreatic β-cell dysfunction by glutathione antioxidant system
Karunakaran, U., Elumalai, S., Moon, J. S., & Won, K. C. (2021) · Redox Biology · doi:10.1016/j.redox.2021.102029 · Cited by 32
Mitochondrial target of thiazolidinediones
Colca, J. R., McDonald, W. G., & Kletzien, R. F. (2014) · Diabetes Obesity and Metabolism · doi:10.1111/dom.12308 · Cited by 32
Self-citation
Inhibition of mitochondrial pyruvate carrier 1 by lapatinib ditosylate mitigates Alzheimer’s-like disease in D-galactose/ovariectomized rats
Mansour, H. M., Fawzy, H. M., El-Khatib, A. S., & Khattab, M. M. (2021) · Neurochemistry International · doi:10.1016/j.neuint.2021.105178 · Cited by 32
Power2: The power of yeast genetics applied to the powerhouse of the cell
Rutter, J. P., & Hughes, A. L. (2015) · Trends in Endocrinology and Metabolism · doi:10.1016/j.tem.2014.12.002 · Cited by 30
Fatty acid oxidation alleviates the energy deficiency caused by the loss of MPC1 in MPC1+/− mice
Zou, S., Lang, T., Zhang, B., Huang, K., Gong, L., Luo, H., Xu, W., & He, X. (2017) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2017.11.134 · Cited by 28
STAT3 inhibition induced temozolomide-resistant glioblastoma apoptosis via triggering mitochondrial STAT3 translocation and respiratory chain dysfunction
Cui, P., Wei, F., Hou, J., Su, Y., Wang, J., & Wang, S. (2020) · Cellular Signalling · doi:10.1016/j.cellsig.2020.109598 · Cited by 30
Hypothyroidism: morphological and metabolic changes in the testis of adult albino rat and the amelioration by alpha-lipoic acid
Ibrahim, A. A. E.-M., Mohammed, N., Eid, K. A., Abomughaid, M. M., Abdelazim, A. M., & Aboregela, A. M. (2020) · Folia Morphologica · doi:10.5603/fm.a2020.0071 · Cited by 29
Discovery of Novel Insulin Sensitizers: Promising Approaches and Targets
Chen, Y., Ma, H., Dasheng, Z., Zhao, G., Wang, L., Fu, X., & Chen, W. (2017) · PPAR Research · doi:10.1155/2017/8360919 · Cited by 29
Pyruvate anaplerosis is a targetable vulnerability in persistent leukaemic stem cells
Rattigan, K. M., Brabcová, Z., Sarnello, D., Zarou, M. M., Roy, K., Kwan, R. S.-Y., de Beauchamp, L., Dawson, A., Ianniciello, A., Khalaf, A., et al. (2023) · Nature Communications · doi:10.1038/s41467-023-40222-z · Cited by 28
ROS/MMP-9 mediated CS degradation in BMSC inhibits citric acid metabolism participating in the dual regulation of bone remodelling
Da, W., Jiang, W., & Tao, L. (2024) · Cell Death Discovery · doi:10.1038/s41420-024-01835-5 · Cited by 28
Targeting mitochondrial homeostasis in the treatment of non-alcoholic fatty liver disease: a review
Deng, Y., Dong, Y., Zhang, S., & Feng, Y. (2024) · Frontiers in Pharmacology · doi:10.3389/fphar.2024.1463187 · Cited by 28
Metabolic Dysfunction-Associated Steatotic Liver Disease Complicated by Diabetes: Pathophysiology and Emerging Therapies
Goto, H., & Takamura, T. (2025) · Journal of Obesity & Metabolic Syndrome · doi:10.7570/jomes25017 · Cited by 28
Treating fatty liver disease by modulating mitochondrial pyruvate metabolism
Colca, J. R., McDonald, W. G., McCommis, K. S., & Finck, B. N. (2017) · Hepatology Communications · doi:10.1002/hep4.1036 · Cited by 23
Self-citation
Characterization of drug-induced human mitochondrial ADP/ATP carrier inhibition
Baron, S. J., King, M. S., Kunji, E. R. S., & Schirris, T. J. J. (2021) · Theranostics · doi:10.7150/thno.54936 · Cited by 23
Lessons on Drug Development: A Literature Review of Challenges Faced in Nonalcoholic Fatty Liver Disease (NAFLD) Clinical Trials
Chen, J. Y. S., Chua, D., Lim, C. O., Ho, W. X., & Tan, N. S. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms24010158 · Cited by 24
The PPARα/γAgonist, Tesaglitazar, Improves Insulin Mediated Switching of Tissue Glucose and Free Fatty Acid Utilization In Vivo in the Obese Zucker Rat
Wallenius, K., Kjellstedt, A., Thalén, P., Löfgren, L., & Oakes, N. D. (2013) · PPAR Research · doi:10.1155/2013/305347 · Cited by 22
Identification of Novel Mitochondrial Pyruvate Carrier Inhibitors by Homology Modeling and Pharmacophore-Based Virtual Screening
Hegazy, L., Gill, L. E., Pyles, K. D., Kaiho, C., Kchouk, S., Finck, B. N., McCommis, K. S., & Elgendy, B. (2022) · Biomedicines · doi:10.3390/biomedicines10020365 · Cited by 22
Diverse Molecular Targets for Therapeutic Strategies in Alzheimer's Disease
Han, S.-H., & Mook‐Jung, I. (2014) · Journal of Korean Medical Science · doi:10.3346/jkms.2014.29.7.893 · Cited by 23
Establishment of mitochondrial pyruvate carrier 1 (MPC1) gene knockout mice with preliminary gene function analyses
Li, X., Li, Y., Han, G., Li, X., Ji, Y., Fan, Z., Zhong, Y., Cao, J., Zhao, J., Goscinski, M. A., et al. (2016) · Oncotarget · doi:10.18632/oncotarget.13210 · Cited by 23
Measuring CPT-1-mediated respiration in permeabilized cells and isolated mitochondria
Yang, K., Doan, M. T., Stiles, L., & Divakaruni, A. S. (2021) · STAR Protocols · doi:10.1016/j.xpro.2021.100687 · Cited by 21
Self-citation
Loss of the redox mitochondrial protein mitoNEET leads to mitochondrial dysfunction in B-cell acute lymphoblastic leukemia
Geldenhuys, W. J., Piktel, D., Moore, J. C., Rellick, S. L., Meadows, E. M., Pinti, M. V., Hollander, J. M., Ammer, A. G., Martin, K. H., & Gibson, L. F. (2021) · Free Radical Biology and Medicine · doi:10.1016/j.freeradbiomed.2021.09.003 · Cited by 21
Re-routing Metabolism by the Mitochondrial Pyruvate Carrier Inhibitor MSDC-0160 Attenuates Neurodegeneration in a Rat Model of Parkinson’s Disease
Mallet, D., Goutaudier, R., Barbier, E., Carnicella, S., Colca, J. R., Fauvelle, F., & Boulet, S. (2022) · Molecular Neurobiology · doi:10.1007/s12035-022-02962-9 · Cited by 21
Self-citation
Fluoroquinolones: old drugs, putative new toxicities
Bove, C., Baldock, R. A., Champigneulle, O., Martin, L., & Bennett, C. L. (2022) · Expert Opinion on Drug Safety · doi:10.1080/14740338.2022.2147924 · Cited by 21
Additive Effects of Omega-3 Fatty Acids and Thiazolidinediones in Mice Fed a High-Fat Diet: Triacylglycerol/Fatty Acid Cycling in Adipose Tissue
Bardová, K., Funda, J., Pohl, R., Čajka, T., Hensler, M., Kuda, O., Janovská, P., Adamcová, K., Irodenko, I., Lenkova, L., et al. (2020) · Nutrients · doi:10.3390/nu12123737 · Cited by 24
Self-citation
Function of mitochondrial pyruvate carriers in hepatocellular carcinoma patients
Ma, X., Cui, Y., Zhou, H., & Li, Q. (2018) · Oncology Letters · doi:10.3892/ol.2018.8466 · Cited by 20
Pioglitazone does not synergize with mirabegron to increase beige fat or further improve glucose metabolism
Finlin, B. S., Memetimin, H., Zhu, B., Confides, A. L., Vekaria, H. J., Khouli, R. H. E., Johnson, Z., Westgate, P. M., Chen, J., Morris, A. J., et al. (2021) · JCI Insight · doi:10.1172/jci.insight.143650 · Cited by 19
Inhibition of the Mitochondrial Pyruvate Carrier by Tolylfluanid
Chen, Y., McCommis, K. S., Ferguson, D., Hall, A. M., Harris, C. A., & Finck, B. N. (2017) · Endocrinology · doi:10.1210/en.2017-00695 · Cited by 19
Molecular basis of pyruvate transport and inhibition of the human mitochondrial pyruvate carrier
Sichrovsky, M., Lacabanne, D., Ruprecht, J. J., Rana, J. J., Stanik, K., Dionysopoulou, M., Sowton, A. P., King, M. S., Jones, S. A., Cooper, L. R., et al. (2025) · Science Advances · doi:10.1126/sciadv.adw1489 · Cited by 22
Time to Change: A Systems Pharmacology Approach to Disentangle Mechanisms of Drug-Induced Mitochondrial Toxicity
Hoogstraten, C. A., Lyon, J. J., Smeitink, J. A. M., Rüssel, F. G. M., & Schirris, T. J. J. (2023) · Pharmacological Reviews · doi:10.1124/pharmrev.122.000568 · Cited by 19
Characteristic Analysis of Homo- and Heterodimeric Complexes of Human Mitochondrial Pyruvate Carrier Related to Metabolic Diseases
Lee, J., Jin, Z., Lee, D., Yun, J.-H., & Lee, W. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21093403 · Cited by 18
A Chemical Proteomic Probe for the Mitochondrial Pyruvate Carrier Complex
Yamashita, Y., Vinogradova, E. V., Zhang, X., Suciu, R. M., & Cravatt, B. F. (2019) · Angewandte Chemie International Edition · doi:10.1002/anie.201914391 · Cited by 19
S-nitrosation of monocarboxylate transporter 1: Inhibition of pyruvate-fueled respiration and proliferation of breast cancer cells
Diers, A. R., Broniowska, K. A., Chang, C.-F., Hill, R. B., & Hogg, N. (2014) · Free Radical Biology and Medicine · doi:10.1016/j.freeradbiomed.2014.01.031 · Cited by 17
The beneficial metabolic effects of insulin sensitizers are not attenuated by mitochondrial pyruvate carrier 2 hypomorphism
Vigueira, P. A., McCommis, K. S., Hodges, W. T., Schweitzer, G. G., Cole, S. L., Oonthonpan, L., Taylor, E. B., McDonald, W. G., Kletzien, R. F., Colca, J. R., et al. (2017) · Experimental Physiology · doi:10.1113/ep086380 · Cited by 16
Self-citation
In situ measurements of mitochondrial matrix enzyme activities using plasma and mitochondrial membrane permeabilization agents
Divakaruni, A. S., Andreyev, A. Y., Rogers, G. W., & Murphy, A. N. (2018) · Analytical Biochemistry · doi:10.1016/j.ab.2017.09.019 · Cited by 18
Self-citation
Traditional and novel tools to probe the mitochondrial metabolism in health and disease
Zhang, Y., & Avalos‬, J. L. (2017) · WIREs Systems Biology and Medicine · doi:10.1002/wsbm.1373 · Cited by 16
Metabolic Mechanisms Connecting Alzheimer’s and Parkinson’s Diseases: Potential Avenues for Novel Therapeutic Approaches
Colca, J. R., & Finck, B. N. (2022) · Frontiers in Molecular Biosciences · doi:10.3389/fmolb.2022.929328 · Cited by 16
Self-citation
Evidence of Insulin-Sensitizing and Mimetic Activity of the Sesquiterpene Quinone Avarone, a Protein Tyrosine Phosphatase 1B and Aldose Reductase Dual Targeting Agent from the Marine Sponge Dysidea avara
Casertano, M., Genovese, M., Santi, A., Pranzini, E., Balestri, F., Piazza, L., CORSO, A. D., Avunduk, S., Imperatore, C., Menna, M., et al. (2023) · Pharmaceutics · doi:10.3390/pharmaceutics15020528 · Cited by 16
UK5099 Inhibits the NLRP3 Inflammasome Independently of its Long‐Established Target Mitochondrial Pyruvate Carrier
Ran, L., Chen, M., Ye, J., Zhang, S., Luo, Z., Bai, T., Qian, C., Zhou, Q., Shan, M., Chu, Y., et al. (2024) · Advanced Science · doi:10.1002/advs.202307224 · Cited by 15
A novel mouse model overexpressing Nocturnin results in decreased fat mass in male mice
Le, P. T., Bornstein, S. A., Motyl, K. J., Tian, L., Stubblefield, J. J., Hong, H., Takahashi, J. S., Green, C. B., Rosen, C. J., & Guntur, A. R. (2019) · Journal of Cellular Physiology · doi:10.1002/jcp.28623 · Cited by 16
Considerations for using isolated cell systems to understand cardiac metabolism and biology
McNally, L. A., Altamimi, T., Fulghum, K., & Hill, B. G. (2020) · Journal of Molecular and Cellular Cardiology · doi:10.1016/j.yjmcc.2020.12.007 · Cited by 16
Mitochondrial metabolism is rapidly re-activated in mature neutrophils to support stimulation-induced response
Lika, J., Votava, J. A., Datta, R., Fritz, C. M., Kralovec, A., Smith, F. M., Huttenlocher, A., Skala, M. C., & Fan, J. (2025) · Frontiers in Immunology · doi:10.3389/fimmu.2025.1572927 · Cited by 15
5-Benzylidene, 5-benzyl, and 3-benzylthiazolidine-2,4-diones as potential inhibitors of the mitochondrial pyruvate carrier: Effects on mitochondrial functions and survival in Drosophila melanogaster
Touaibia, M., St‐Cœur, P., Duff, P., Faye, D. C., & Pichaud, N. (2021) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2021.174627 · Cited by 16
Optimization of cell permeabilization in electron flow based mitochondrial function assays
Lei, X.-H., & Bochner, B. R. (2021) · Free Radical Biology and Medicine · doi:10.1016/j.freeradbiomed.2021.10.014 · Cited by 15
Exploring the Protective Effect against 7,12-Dimethylbenz[a]anthracene-Induced Breast Tumors of Palmitoylethanolamide
Rai, N., Kailashiya, V., & Gautam, V. (2023) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.3c00188 · Cited by 14
Targeting the Mitochondrial Pyruvate Carrier for Neuroprotection
Tang, B. L. (2019) · Brain Sciences · doi:10.3390/brainsci9090238 · Cited by 15
The Hepatic Mitochondrial Pyruvate Carrier as a Regulator of Systemic Metabolism and a Therapeutic Target for Treating Metabolic Disease
McCommis, K. S., & Finck, B. N. (2023) · Biomolecules · doi:10.3390/biom13020261 · Cited by 14
The MitoLuc Assay System for Accurate Real-Time Monitoring of Mitochondrial Protein Import Within Mammalian Cells
Needs, H. I., Lorriman, J., Pereira, G. C., Henley, J. M., & Collinson, I. R. (2023) · Journal of Molecular Biology · doi:10.1016/j.jmb.2023.168129 · Cited by 12
Paradoxical Inhibition of Glycolysis by Pioglitazone Opposes the Mitochondriopathy Caused by AIF Deficiency
Bénit, P., Pelhaître, A., Saunier, E. F., Bortoli, S., Coulibaly, A., Rak, M., Schiff, M., Kroemer, G., Zeviani, M., & Rustin, P. (2017) · EBioMedicine · doi:10.1016/j.ebiom.2017.02.013 · Cited by 14
Insulin sensitizers in 2023: lessons learned and new avenues for investigation
Colca, J. R., Tanis, S. P., Kletzien, R. F., & Finck, B. N. (2023) · Expert Opinion on Investigational Drugs · doi:10.1080/13543784.2023.2263369 · Cited by 13
Self-citation
Stress increases sperm respiration and motility in mice and men
Moon, N., Morgan, C. P., Marx-Rattner, R., Jeng, A., Johnson, R. L., Chikezie, I., Mannella, C. A., Sammel, M. D., Epperson, C. N., & Bale, T. L. (2024) · Nature Communications · doi:10.1038/s41467-024-52319-0 · Cited by 15
Determining Compartment-Specific Metabolic Fluxes
Nonnenmacher, Y., Palorini, R., & Hiller, K. (2018) · Methods in molecular biology · doi:10.1007/978-1-4939-8769-6_10 · Cited by 13
A New Antidiabetic Agent Showing Short- and Long-Term Effects Due to Peroxisome Proliferator-Activated Receptor Alpha/Gamma Dual Agonism and Mitochondrial Pyruvate Carrier Inhibition
Laghezza, A., Cerchia, C., Genovese, M., Leuci, R., Pranzini, E., Santi, A., Brunetti, L., Piemontese, L., Tortorella, P., Biswas, A., et al. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c02093 · Cited by 12
Building and Testing PPARγ Therapeutic ELB00824 with an Improved Therapeutic Window for Neuropathic Pain
Westlund, K. N., & Zhang, M. (2020) · Molecules · doi:10.3390/molecules25051120 · Cited by 12
Novel mitoNEET ligand NL-1 improves therapeutic outcomes in an aged rat model of cerebral ischemia/reperfusion injury
Vijikumar, A., Saralkar, P. A., Saylor, S. D., Sullivan, P. G., Huber, J. D., & Geldenhuys, W. J. (2022) · Experimental Neurology · doi:10.1016/j.expneurol.2022.114128 · Cited by 12
Toxicity of Pioglitazone on Mitochondria Isolated from Brain and Heart: An Analysis for Probable Drug-Induced Neurotoxicity and Cardiotoxicity
Seydi, E., Servati, T., Samiei, F., Naserzadeh, P., & Pourahmad, J. (2020) · Drug Research · doi:10.1055/a-1085-2542 · Cited by 12

Authors: 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., Henry, R. R., McDonald, W. G., Colca, J. R., Simon, M. I., Ciaraldi, T. P., & Murphy, A. N.
Affiliations: Departments of aPharmacology and
Seahorse Bioscience, North Billerica, MA 01862;
VA San Diego Healthcare System (US)
Pioneer Valley Life Sciences Institute, Springfield, MA 01107;
University of Massachusetts Amherst (US)
University of California San Diego (US)
Metabolic Solutions Development Company (United States) (US)
ORCID: Divakaruni, Ajit S.
Wiley, Sandra E.
Andreyev, Alexander Y.
Yadava, Nagendra
Heuck, Alejandro P.
Henry, Robert R.
Colca, Jerry R.
Ciaraldi, Theodore P.
Murphy, Anne N.
Venue: Proceedings of the National Academy of Sciences
Publisher: National Academy of Sciences
Published: 2013-03-19
Volume: 110
Issue: 14
Pages: 5422-5427
ISSN: 0027-8424 (ISSN-L)
1091-6490
DOI: 10.1073/pnas.1303360110
PMC: PMC3619368
OpenAlex: W1981961082
Cited by: 308
References: 58
Citations by year: 2026: 15 · 2025: 22 · 2024: 25 · 2023: 22 · 2022: 25 · 2021: 26 · 2020: 27 · 2019: 20 · 2018: 27 · 2017: 24 · 2016: 23 · 2015: 16 · 2014: 24 · 2013: 12
FWCI: 11.21
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: Proceedings of the National Academy of Sciences (publishedVersion)
Europe PMC (PubMed Central) (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
Funders: American Diabetes Association
National Institutes of Health
National Heart, Lung, and Blood Institute (P01HL085577)
National Institute of Diabetes and Digestive and Kidney Diseases (R42DK081298, R24DK092154)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Mitochondrial Function and Pathology
Health Sciences › Medicine › Physiology (medical) › Adipose Tissue and Metabolism
Keywords: thiazolidinediones, mitochondrial pyruvate carrier, MPC1, MPC2, pyruvate transport, mitochondrial respiration inhibition, methyl pyruvate, glucose uptake, skeletal muscle fibers, insulin sensitization, metabolic dysfunction
MeSH terms: Solute Carrier Proteins, Acrylates, Analysis of Variance, Animals, Cell Line, Glucose, Humans, Blotting, Western, Muscle, Skeletal, Cell Respiration, Reverse Transcriptase Polymerase Chain Reaction, Mitochondrial Proteins, Membrane Transport Proteins, Anion Transport Proteins, Monocarboxylic Acid Transporters, Mitochondrial Membrane Transport Proteins, Thiazolidinediones, Cytochromes c, Mitochondrial Membranes, Mice, Rats, Membrane Potential, Mitochondrial, Metabolic Networks and Pathways

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

Thiazolidinediones are acute, specific inhibitors of the mitochondrial pyruvate carrier

Abstract

Overview

Integrity signals

Verification

Claims the paper makes

Claims other papers make about this one

Self-check

Citations

Cites

Cited by

Related

Metadata

Record

About these checks