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Drug Screening · Journal article
Magnetic Resonance Letters · June 12, 2026
Early or partial results. Treat as a signal, not a conclusion.
A real-time NMR method was developed to track intracellular glutamine metabolic flux in living cells and applied to screen traditional Chinese medicine compounds. The approach identified quercetin (Compound 2) from Astragalus membranaceus as a direct GLS1 enzymatic inhibitor through molecular docking followed by in vitro recombinant enzyme assays.
Method development with virtual screening and in vitro enzyme assay. Living cells (cancer cells, specific lines not detailed) and recombinant human GLS1 enzyme. Intervention: Quercetin (Compound 2) and 11 other compounds from Astragalus membranaceus.
12 potential compounds from Astragalus membranaceus were flagged as candidate GLS1 binders via molecular docking Compound 2 (quercetin) was identified as the exclusive direct enzymatic inhibitor of GLS1 among tested monomers In vitro recombinant human GLS1 enzyme activity assays ruled out computational false positives
Specificity, off-target effects, and toxicity of quercetin not addressed
This platform offers a tool for metabolic profiling and early-stage drug discovery targeting glutamine metabolism, but translation to clinical anticancer therapy requires demonstration of tumor efficacy and safety in preclinical models and trials.
A novel NMR method for tracking glutamine metabolism identifies quercetin as a GLS1 inhibitor through in vitro assays, but clinical efficacy and anticancer activity are not demonstrated.
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Quoted from the source exactly as published.
This platform offers a tool for metabolic profiling and early-stage drug discovery targeting glutamine metabolism, but translation to clinical anticancer therapy requires demonstration of tumor efficacy and safety in preclinical models and trials.
Graded across the dimensions that decide whether you should act, each from what the source actually supports. There is no single score, and where a dimension was not assessed it says so.
Metabolic reprogramming is a substantial obstacle for anticancer drug screening, as targeted therapeutics often lose efficiency due to the dynamic adaption of cancer cells. Glutamine metabolism in cancer profoundly impacts tumor initiation, progression and metastasis. The existing agents are compromised by resistance and off-target toxicity. In this study, a real-time NMR tracking method for intracellular glutamine metabolic flux was established. This method enables comprehensive profiling of nitrogen metabolism and serves as a valuable tool for characterizing specific cancer metabolic phenotypes and screening drugs against targeted cancer cells. Applying this approach to traditional Chinese medicine (TCM) discovery, we identified Astragalus membranaceus as a potent regulator of glutamine metabolism. Through virtual screening via molecular docking, 12 potential compounds from Astragalus membranaceus were initially flagged as candidate binders toward the allosteric pocket of glutaminase 1 (GLS1). Crucially, subsequent in vitro recombinant human GLS1 enzyme activity assays successfully ruled out computational false positives and demonstrated that Compound 2 (quercetin) acts as the exclusive, direct enzymatic inhibitor among the tested monomers, capable of effectively suppressing GLS1 activity. Overall, this work provides a robust platform for real-time metabolic profiling of glutamine metabolism and drug screening at the living cell level, and offers new insights into the mechanisms of TCMs in anticancer therapy.
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