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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
Glucose-independent glutamine metabolism via TCA cycling for proliferation and survival in B cells.
TLDR
The metabolic responses of a MYC-inducible human Burkitt lymphoma model P493 cell line to aerobic and hypoxic conditions, and to glucose deprivation, are determined using stable isotope-resolved metabolomics to demonstrate an alternative energy-generating glutaminolysis pathway involving a glucose-independent TCA cycle. Expand
HIV-associated neurocognitive disorder — pathogenesis and prospects for treatment
TLDR
It is suggested that adjunctive therapies — treatments targeting CNS inflammation and other metabolic processes, including glutamate homeostasis, lipid and energy metabolism — are needed to reverse or improve HAND-related neurological dysfunction. Expand
Inhibition of glutaminase preferentially slows growth of glioma cells with mutant IDH1.
TLDR
The ability to selectively slow growth in cells with IDH1 mutations by inhibiting glutaminase suggests a unique reprogramming of intermediary metabolism and a potential therapeutic strategy. Expand
Targeted inhibition of tumor-specific glutaminase diminishes cell-autonomous tumorigenesis.
TLDR
It is reported that loss of one copy of Gls blunted tumor progression in an immune-competent MYC-mediated mouse model of hepatocellular carcinoma and small molecule and genetic inhibition of GLS are supported for targeting the tumor cell-autonomous dependence on GLS for cancer therapy. Expand
HIV-associated neurocognitive disorder — pathogenesis and prospects for treatment
TLDR
This work presents a meta-anatomy of the central nervous system using a simple, scalable, and scalable approach that allows for rapid and efficient analysis of the immune system’s response to foreign substance abuse. Expand
Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated alpha-linked acidic dipeptidase.
TLDR
Inhibition of NAALADase may show utility as a therapeutic intervention in diseases in which altered levels of glutamate are thought to be involved, and is suggested to act as a storage form of synaptic glutamate. Expand
Abnormal excitatory neurotransmitter metabolism in schizophrenic brains.
TLDR
The hypothesis that schizophrenia results from a hypofunction of certain glutamatergic neuronal systems is supported and the therapeutic efficacy of neuroleptics may be related to increased glutamatorgic activity. Expand
Selective inhibition of NAALADase, which converts NAAG to glutamate, reduces ischemic brain injury
TLDR
It is demonstrated that the newly described 2-PMPA (2-(phosphonomethyl)pentanedioic acid) robustly protects against ischemic injury in a neuronal culture model of stroke and in rats after transient middle cerebral artery occlusion, indicating that NAALADase inhibition may have use in neurological disorders in which excessive excitatory amino acid transmission is pathogenic. Expand
Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors.
TLDR
In an attempt to identify more potent GLS inhibitors with improved drug-like molecular properties, a series of BPTES analogs were synthesized and evaluated and revealed that some truncated analogs retained the potency of B PTES, presenting an opportunity to improve its aqueous solubility. Expand
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