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Pharmacological inhibition of cystine–glutamate exchange induces endoplasmic reticulum stress and ferroptosis
Exchange of extracellular cystine for intracellular glutamate by the antiporter system xc− is implicated in numerous pathologies. Pharmacological agents that inhibit system xc− activity with highExpand
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Targeted inhibition of tumor-specific glutaminase diminishes cell-autonomous tumorigenesis.
Glutaminase (GLS), which converts glutamine to glutamate, plays a key role in cancer cell metabolism, growth, and proliferation. GLS is being explored as a cancer therapeutic target, but whether GLSExpand
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Synthesis and biological evaluation of D-amino acid oxidase inhibitors.
D-amino acid oxidase (DAAO) catalyzes the oxidation of D-amino acids including d-serine, a full agonist at the glycine site of the NMDA receptor. A series of benzo[ d]isoxazol-3-ol derivatives wereExpand
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Selective inhibition of NAALADase, which converts NAAG to glutamate, reduces ischemic brain injury
We describe here a new strategy for the treatment of stroke, through the inhibition of NAALADase (N-acetylated-α-linked-acidic dipeptidase), an enzyme responsible for the hydrolysis of theExpand
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Palonosetron triggers 5-HT(3) receptor internalization and causes prolonged inhibition of receptor function.
Palonosetron is a 5-HT(3) receptor antagonist that has demonstrated superiority in preventing both acute and delayed emesis when compared to older first generation 5-HT(3) receptor antagonists. TheExpand
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The Antiemetic 5-HT3 Receptor Antagonist Palonosetron Inhibits Substance P-Mediated Responses In Vitro and In Vivo
  • C. Rojas, Y. Li, +7 authors B. Slusher
  • Medicine, Chemistry
  • Journal of Pharmacology and Experimental…
  • 1 November 2010
Palonosetron is the only 5-HT3 receptor antagonist approved for the treatment of delayed chemotherapy-induced nausea and vomiting (CINV) in moderately emetogenic chemotherapy. Accumulating evidenceExpand
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Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors.
Bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide (BPTES) is a potent and selective allosteric inhibitor of kidney-type glutaminase (GLS) that has served as a molecular probe to determineExpand
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Palonosetron Exhibits Unique Molecular Interactions with the 5-HT3 Receptor
BACKGROUND: Palonosetron is a 5-HT3-receptor antagonist (5-HT3-RA) that has been shown to be superior to other 5-HT3-RAs in phase III clinical trials for the prevention of acute, delayed, and overallExpand
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Inhibition of xc⁻ transporter-mediated cystine uptake by sulfasalazine analogs.
A series of sulfasalazine analogs were synthesized and tested for their ability to block cystine-glutamate antiporter system xc⁻ using L-[(14)C]cystine as a substrate. Replacement of sulfasalazine'sExpand
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Preventing Allograft Rejection by Targeting Immune Metabolism.
Upon antigen recognition and co-stimulation, T lymphocytes upregulate the metabolic machinery necessary to proliferate and sustain effector function. This metabolic reprogramming in T cells regulatesExpand
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