ArticlePloS one2016
ENOblock Does Not Inhibit the Activity of the Glycolytic Enzyme Enolase.
Article in PloS one, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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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
18 citing papers in PubMed, 40 citations in OpenAlex.
- Giardiavirus rewires host translation and glycolytic metabolism to support its replication inVirulence · 2026Article
- Enolase-1 and Inflammation.Biomolecules · 2026Review
- Non-orthosteric inhibition of enolase 1 impedes growth of triple-negative breast cancer.Cell reports. Medicine · 2025Article
- Multifunctional roles of γ-enolase in the central nervous system: more than a neuronal marker.Cell & bioscience · 2024Review
- Role of Glycolytic and Glutamine Metabolism Reprogramming on the Proliferation, Invasion, and Apoptosis Resistance through Modulation of Signaling Pathways in Glioblastoma.International journal of molecular sciences · 2023Review
- Mediation of PKM2-dependent glycolytic and non-glycolytic pathways by ENO2 in head and neck cancer development.Journal of experimental & clinical cancer research : CR · 2023Article
- ENO1 and Cancer.Molecular therapy oncolytics · 2022Review
- Macrosphelide A Exhibits a Specific Anti-Cancer Effect by Simultaneously Inactivating ENO1, ALDOA, and FH.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Targeting Host Glycolysis as a Strategy for Antimalarial Development.Frontiers in cellular and infection microbiology · 2021Article
- Discovery and evaluation of inhibitory activity and mechanism of arylcoumarin derivatives on Theileria annulata enolase by in vitro and molecular docking studies.Molecular diversity · 2020Article
- A moonlighting role for enzymes of glycolysis in the co-localization of mitochondria and chloroplasts.Nature communications · 2020Article
- Alpha-Enolase: Emerging Tumor-Associated Antigen, Cancer Biomarker, and Oncotherapeutic Target.Frontiers in genetics · 2020Review
- ENOblock inhibits the pathology of diet-induced obesity.Scientific reports · 2019Article
- The Synergism of the Small Molecule ENOblock and Fluconazole Against Fluconazole-ResistantFrontiers in microbiology · 2019Article
- Alpha-enolase regulates the malignant phenotype of pulmonary artery smooth muscle cells via the AMPK-Akt pathway.Nature communications · 2018Article
- Next Generation Immunotherapy for Pancreatic Cancer: DNA Vaccination is Seeking New Combo Partners.Cancers · 2018Review
- In silico-based identification of human α-enolase inhibitors to block cancer cell growth metabolically.Drug design, development and therapy · 2017Article
- Deciphering T Cell Immunometabolism with Activity-Based Protein Profiling.Current topics in microbiology and immunologyReview
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Inhibition of glycolysis is of great potential for the treatment of cancer. However, inhibitors of glycolytic enzymes with favorable pharmacological profiles have not been forthcoming. Due to the nature of their active sites, most high-affinity transition-state analogue inhibitors of glycolysis enzymes are highly polar with poor cell permeability. A recent publication reported a novel, non-active site inhibitor of the glycolytic enzyme Enolase, termed ENOblock (N-[2-[2-2-aminoethoxy)ethoxy]ethyl]4-4-cyclohexylmethyl)amino]6-4-fluorophenyl)methyl]amino]1,3,5-triazin-2-yl]amino]benzeneacetamide). This would present a major advance, as this is heterocyclic and fully cell permeable molecule. Here, we present evidence that ENOblock does not inhibit Enolase enzymatic activity in vitro as measured by three different assays, including a novel 31P NMR based method which avoids complications associated with optical interferences in the UV range. Indeed, we note that due to strong UV absorbance, ENOblock interferes with the direct spectrophotometric detection of the product of Enolase, phosphoenolpyruvate. Unlike established Enolase inhibitors, ENOblock does not show selective toxicity to ENO1-deleted glioma cells in culture. While our data do not dispute the biological effects previously attributed to ENOblock, they indicate that such effects must be caused by mechanisms other than direct inhibition of Enolase enzymatic activity.
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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.