ArticleBiochemistry2014
A noncompetitive inhibitor for Mycobacterium tuberculosis's class IIa fructose 1,6-bisphosphate aldolase.
Article in Biochemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 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.
The trial behind it
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
29 citing papers in PubMed, 55 citations in OpenAlex.
- Chemical Speciation of Vanadium(IV/V)/8-Hydroxyquinoline-2-Carboxylic Acid System in Aqueous Solution: A Multitechnique Study.Inorganic chemistry · 2026Article
- A Key Metabolic Protein in Active Mycobacterium tuberculosis: Insights into Carbon, Nitrogen, and Sulfur Metabolism.Advances in experimental medicine and biology · 2026Review
- Genome-wide analysis of theFrontiers in plant science · 2026Article
- The Significance of Mono- and Dual-Effective Agents in the Development of New Antifungal Strategies.Chemical biology & drug design · 2025Review
- The metal cofactor: stationary or mobile?Applied microbiology and biotechnology · 2024Review
- Characterization ofFrontiers in genetics · 2024Article
- Comparative proteomic investigation unravels the pathobiology of Mycobacterium fortuitum biofilm.Applied microbiology and biotechnology · 2023Article
- Thermal Ring-Based Heat Switches in Hyperthermophilic Class II Bacterial Fructose Aldolase.ACS omega · 2023Article
- PfCRT mutations conferring piperaquine resistance in falciparum malaria shape the kinetics of quinoline drug binding and transport.PLoS pathogens · 2023Article
- A Superior Corrosion Protection of Mg Alloy via Smart Nontoxic Hybrid Inhibitor-Containing Coatings.Molecules (Basel, Switzerland) · 2023Article
- Insights into the molecular determinants involved inVirulence · 2021Review
- Multifunctional Fructose 1,6-Bisphosphate Aldolase as a Therapeutic Target.Frontiers in molecular biosciences · 2021Review
- Genome-Wide Characterization and Expression Analysis Provide Basis to the Biological Function of Cotton FBA Genes.Frontiers in plant science · 2021Article
- Article
- The human milk protein-lipid complex HAMLET disrupts glycolysis and induces death inThe Journal of biological chemistry · 2019Article
- Structure-based identification of a potential non-catalytic binding site for rational drug design in the fructose 1,6-biphosphate aldolase from Giardia lamblia.Scientific reports · 2019Article
- Article
- Targeting Metalloenzymes for Therapeutic Intervention.Chemical reviews · 2019Review
- Active site remodeling during the catalytic cycle in metal-dependent fructose-1,6-bisphosphate aldolases.The Journal of biological chemistry · 2018Article
- Putative vaccine candidates and drug targets identified by reverse vaccinology and subtractive genomics approaches to controlJournal of the Royal Society, Interface · 2018Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 4 institutions in 1 country.
Funding
Abstract
Class II fructose 1,6-bisphosphate aldolase (FBA) is an enzyme critical for bacterial, fungal, and protozoan glycolysis/gluconeogenesis. Importantly, humans lack this type of aldolase, having instead a class I FBA that is structurally and mechanistically distinct from class II FBAs. As such, class II FBA is considered a putative pharmacological target for the development of novel antibiotics against pathogenic bacteria such as Mycobacterium tuberculosis, the causative agent for tuberculosis (TB). To date, several competitive class II FBA substrate mimic-styled inhibitors have been developed; however, they lack either specificity, potency, or properties that limit their potential as possible therapeutics. Recently, through the use of enzymatic and structure-based assisted screening, we identified 8-hydroxyquinoline carboxylic acid (HCA) that has an IC50 of 10 ± 1 μM for the class II FBA present in M. tuberculosis (MtFBA). As opposed to previous inhibitors, HCA behaves in a noncompetitive manner, shows no inhibitory properties toward human and rabbit class I FBAs, and possesses anti-TB properties. Furthermore, we were able to determine the crystal structure of HCA bound to MtFBA to 2.1 Å. HCA also demonstrates inhibitory effects for other class II FBAs, including pathogenic bacteria such as methicillin-resistant Staphylococcus aureus. With its broad-spectrum potential, unique inhibitory characteristics, and flexibility of functionalization, the HCA scaffold likely represents an important advancement in the development of class II FBA inhibitors that can serve as viable preclinical candidates.
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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.