ArticlePloS one2014
Novel inhibitors of mitochondrial sn-glycerol 3-phosphate dehydrogenase.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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Who cites it
38 citing papers in PubMed, 66 citations in OpenAlex.
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- Decoding the metabolic cipher of dormant cancer cells: molecular mechanisms and therapeutic potentials.Cell communication and signaling : CCS · 2026Review
- Energy dissipation via the glycerol phosphate shuttle: coupling glycolysis to mitochondrial thermogenesis in Drosophila melanogaster flight muscle.Journal of comparative physiology. B, Biochemical, systemic, and environmental physiology · 2026Article
- Novel plasmid curing mediated restoration of antimicrobial sensitivity by Nigella sativa extract against multidrug resistant Staphylococcus aureus.Scientific reports · 2026Article
- Mitochondrial glutamic-oxaloacetic transaminase (GOT2) in the growth of C2C12 myoblasts.Journal of bioenergetics and biomembranes · 2025Article
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- Targeting Malaria's Achilles' Heels: A Review of Plasmodium Life Cycle Vulnerabilities for Drug Discovery.Current topics in medicinal chemistry · 2025Review
- Metabolic insights into the warfarin-mango interaction: A pilot study integrating clinical observations and metabolomics.ADMET & DMPK · 2025Article
- Plate-Based Measurement of Respiration by Isolated Mitochondria and by Intact Cells.Methods in molecular biology (Clifton, N.J.) · 2025Article
- Fasting as a precursor to high-fat diet enhances mitochondrial resilience in Drosophila melanogaster.Insect science · 2024Article
- Inhibition of Shikimate Kinase from Methicillin-ResistantInternational journal of molecular sciences · 2024Article
- Glycerol 3-phosphate dehydrogenases (1 and 2) in cancer and other diseases.Experimental & molecular medicine · 2024Review
- Site IQ in mitochondrial complex I generates S1QEL-sensitive superoxide/hydrogen peroxide in both the reverse and forward reactions.The Biochemical journal · 2023Article
- Artificial neural network applied to fragile X-associated tremor/ataxia syndrome stage diagnosis based on peripheral mitochondrial bioenergetics and brain imaging outcomes.Scientific reports · 2022Article
- Conditions Conducive to the Glutathionylation of Complex I Subunit NDUFS1 Augment ROS Production following the Oxidation of Ubiquinone Linked Substrates, Glycerol-3-Phosphate and Proline.Antioxidants (Basel, Switzerland) · 2022Article
- Review
- A ferroptosis defense mechanism mediated by glycerol-3-phosphate dehydrogenase 2 in mitochondria.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Prescription drugs and mitochondrial metabolism.Bioscience reports · 2022Review
- Exploring Thermal Sensitivities and Adaptations of Oxidative Phosphorylation Pathways.Metabolites · 2022Review
- Mitochondria in human neutrophils mediate killing of Staphylococcus aureus.Redox biology · 2022Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
Mitochondrial sn-glycerol 3-phosphate dehydrogenase (mGPDH) is a ubiquinone-linked enzyme in the mitochondrial inner membrane best characterized as part of the glycerol phosphate shuttle that transfers reducing equivalents from cytosolic NADH into the mitochondrial electron transport chain. Despite the widespread expression of mGPDH and the availability of mGPDH-null mice, the physiological role of this enzyme remains poorly defined in many tissues, likely because of compensatory pathways for cytosolic regeneration of NAD⁺ and mechanisms for glycerol phosphate metabolism. Here we describe a novel class of cell-permeant small-molecule inhibitors of mGPDH (iGP) discovered through small-molecule screening. Structure-activity analysis identified a core benzimidazole-phenyl-succinamide structure as being essential to inhibition of mGPDH while modifications to the benzimidazole ring system modulated both potency and off-target effects. Live-cell imaging provided evidence that iGPs penetrate cellular membranes. Two compounds (iGP-1 and iGP-5) were characterized further to determine potency and selectivity and found to be mixed inhibitors with IC₅₀ and K(i) values between ∼1-15 µM. These novel mGPDH inhibitors are unique tools to investigate the role of glycerol 3-phosphate metabolism in both isolated and intact systems.
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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.