ArticleBiochemistry2014
The estrogen-related receptor α inverse agonist XCT 790 is a nanomolar mitochondrial uncoupler.
Article in Biochemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed, 35 citations in OpenAlex.
- Stomach at the crossroads: nuclear receptor signaling at the interface between what we are and what we eat.Physiological reviews · 2026Review
- Nuclear Receptor-Targeted Therapies: Reprogramming Metabolism with TRβ, ERRα, and LXR Modulators.Biomolecules · 2026Review
- Perimenopausal state oestradiol to progesterone imbalance drives Alzheimer's risk via ERRα dysregulation and energy dyshomeostasis.Nature communications · 2025Article
- A key role of the PGC-1α/ERR-α pathway in regulation of angiogenic factors in proliferative diabetic retinopathy.Frontiers in endocrinology · 2025Article
- Reprogramming of Fatty Acid Metabolism in Gynaecological Cancers: Is There a Role for Oestradiol?Metabolites · 2022Review
- Estrogen-related Receptor Alpha (ERRα) is Required for PGC-1α-dependent Gene Expression in the Mouse Brain.Neuroscience · 2021Article
- Pioglitazone improves skeletal muscle functions in reserpine-induced fibromyalgia rat model.Annals of medicine · 2021Article
- Calcific aortic valve disease: turning therapeutic discovery up a notch.Nature reviews. Cardiology · 2021Article
- Estrogen-related receptor alpha directly binds to p53 and cooperatively controls colon cancer growth through the regulation of mitochondrial biogenesis and function.Cancer & metabolism · 2020Article
- Repression of the transcriptional activity of ERRα with sequence-specific DNA-binding polyamides.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2020Article
- Crosstalk between autophagy and metabolic regulation of cancer stem cells.Molecular cancer · 2020Review
- Inhibition of ERROxidative medicine and cellular longevity · 2020Article
- A Genome-wide Functional Signature Ontology Map and Applications to Natural Product Mechanism of Action Discovery.Cell chemical biology · 2019Article
- Regulatory mechanisms leading to differential Acyl-CoA synthetase 4 expression in breast cancer cells.Scientific reports · 2019Article
- The PGC-1/ERR network and its role in precision oncology.NPJ precision oncology · 2019Review
- ERRα suppression enhances the cytotoxicity of the MEK inhibitor trametinib against colon cancer cells.Journal of experimental & clinical cancer research : CR · 2018Article
- Modulation of Autophagy by a Small Molecule Inverse Agonist of ERRα Is Neuroprotective.Frontiers in molecular neuroscience · 2018Article
- Mitochondrial uncoupler carbonyl cyanide m-chlorophenylhydrazone induces vasorelaxation without involving KBritish journal of pharmacology · 2016Article
- Ligand Activation of ERRα by Cholesterol Mediates Statin and Bisphosphonate Effects.Cell metabolism · 2016Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
XCT 790 is widely used to inhibit estrogen-related receptor α (ERRα) activity as an inverse agonist. Here, we report that XCT 790 potently activates AMP kinase (AMPK) in a dose-dependent and ERRα-independent manner, with active concentrations more than 25-fold below those typically used to perturb ERRα. AMPK activation is secondary to inhibition of energy production as XCT 790 rapidly depletes the pool of cellular ATP. A concomitant increase in oxygen consumption rates suggests uncoupling of the mitochondrial electron transport chain. Consistent with this, XCT 790 decreased mitochondrial membrane potential without affecting mitochondrial mass. Therefore, XCT 790 is a potent, fast-acting, mitochondrial uncoupler independent of its inhibition of ERRα. The biological activity together with structural features in common with the chemical uncouplers FCCP and CCCP indicates likely mode of action as a proton ionophore.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.