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BPTES is a small molecule that acts as a potent and selective allosteric inhibitor of glutaminase 1 (GLS1), also known as kidney-type glutaminase (KGA). It binds to an allosteric site on GLS1 and inhibits its enzymatic activity with high selectivity over other related enzymes such as GLS2 and γ-glutamyl transpeptidase. By inhibiting GLS1-mediated conversion of glutamine to glutamate—a key step in cellular metabolism—BPTES disrupts the process of glutaminolysis. This mechanism is particularly relevant in cancer cells that rely on increased glutamine metabolism for growth and survival. BPTES has demonstrated anticancer effects in preclinical models by inducing cell death in lymphoma cells and reducing tumor growth in xenograft mouse models. It is widely used as a research tool for studying cancer metabolism and immunometabolism but is not approved for clinical use[1][3][6].
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