ArticleJournal of medicinal chemistry2012
Chemical proteomics-based analysis of off-target binding profiles for rosiglitazone and pioglitazone: clues for assessing potential for cardiotoxicity.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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Who cites it
22 citing papers in PubMed.
- Limosilactobacillus reuteri and caffeoylquinic acid synergistically promote adipose browning and ameliorate obesity-associated disorders.Microbiome · 2022Article
- Activation of the endocannabinoid system mediates cardiac hypertrophy induced by rosiglitazone.Acta pharmacologica Sinica · 2022Article
- Functionally Essential Tubular Proteins Are Lost to Urine-Excreted, Large Extracellular Vesicles during Chronic Renal Insufficiency.Kidney360 · 2020Article
- PPARγ-Independent Side Effects of Thiazolidinediones on Mitochondrial Redox State in Rat Isolated Hearts.Cells · 2020Article
- Quantitative Proteomic Profiling of Mitochondrial Toxicants in a Human Cardiomyocyte Cell Line.Frontiers in genetics · 2020Article
- Article
- Thiazolidinediones: the Forgotten Diabetes Medications.Current diabetes reports · 2019Review
- Macrophage nuclear receptors: Emerging key players in infectious diseases.PLoS pathogens · 2019Review
- Pioglitazone Induces Cardiomyocyte Apoptosis and Inhibits Cardiomyocyte Hypertrophy Via VEGFR-2 Signaling Pathway.Arquivos brasileiros de cardiologia · 2018Article
- De novo fatty acid synthesis by Schwann cells is essential for peripheral nervous system myelination.The Journal of cell biology · 2018Article
- Autologous fat transplants to deliver glitazone and adiponectin for vasculoprotection.Journal of controlled release : official journal of the Controlled Release Society · 2017Article
- Diabetes and bone health: latest evidence and clinical implications.Therapeutic advances in musculoskeletal disease · 2017Review
- Transcriptome Profiling of Patient-Specific Human iPSC-Cardiomyocytes Predicts Individual Drug Safety and Efficacy Responses In Vitro.Cell stem cell · 2016Article
- Drug-induced mitochondrial dysfunction and cardiotoxicity.American journal of physiology. Heart and circulatory physiology · 2015Review
- Pharmacologic targeting of sirtuin and PPAR signaling improves longevity and mitochondrial physiology in respiratory chain complex I mutant Caenorhabditis elegans.Mitochondrion · 2015Article
- Activation of PPAR gamma receptors reduces levodopa-induced dyskinesias in 6-OHDA-lesioned rats.Neurobiology of disease · 2015Article
- Identification of Bexarotene as a PPARγ Antagonist with HDX.PPAR research · 2015Article
- Hypoglycemic and hypotensive activity of a root extract of Smilax aristolochiifolia, standardized on N-trans-feruloyl-tyramine.Molecules (Basel, Switzerland) · 2014Article
- A systems biology approach to understand the pathophysiological mechanisms of cardiac pathological hypertrophy associated with rosiglitazone.BMC medical genomics · 2014Article
- Rosiglitazone causes cardiotoxicity via peroxisome proliferator-activated receptor γ-independent mitochondrial oxidative stress in mouse hearts.Toxicological sciences : an official journal of the Society of Toxicology · 2014Article
Corrections and comments
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Authors and funding
4 authors.
Funding
Abstract
Drugs exert desired and undesired effects based on their binding interactions with protein target(s) and off-target(s), providing evidence for drug efficacy and toxicity. Pioglitazone and rosiglitazone possess a common functional core, glitazone, which is considered a privileged scaffold upon which to build a drug selective for a given target--in this case, PPARγ. Herein, we report a retrospective analysis of two variants of the glitazone scaffold, pioglitazone and rosiglitazone, in an effort to identify off-target binding events in the rat heart to explain recently reported cardiovascular risk associated with these drugs. Our results suggest that glitazone has affinity for dehydrogenases, consistent with known binding preferences for related rhodanine cores. Both drugs bound ion channels and modulators, with implications in congestive heart failure, arrhythmia, and peripheral edema. Additional proteins involved in glucose homeostasis, synaptic transduction, and mitochondrial energy production were detected and potentially contribute to drug efficacy and cardiotoxicity.
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