Search Results - "Slusher, Barbara"
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We're Not "DON" Yet: Optimal Dosing and Prodrug Delivery of 6-Diazo-5-oxo-L-norleucine
Published in Molecular cancer therapeutics (01-09-2018)“…The broadly active glutamine antagonist 6-diazo-5-oxo-L-norleucine (DON) has been studied for 60 years as a potential anticancer therapeutic. Clinical studies…”
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Clinical development of metabolic inhibitors for oncology
Published in The Journal of clinical investigation (01-01-2022)“…Metabolic inhibitors have been used in oncology for decades, dating back to antimetabolites developed in the 1940s. In the past 25 years, there has been…”
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Small Molecule Inhibitors Targeting Biosynthesis of Ceramide, the Central Hub of the Sphingolipid Network
Published in Journal of medicinal chemistry (14-01-2021)“…Ceramides are composed of a sphingosine and a single fatty acid connected by an amide linkage. As one of the major classes of biologically active lipids,…”
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4
Glutamine blockade induces divergent metabolic programs to overcome tumor immune evasion
Published in Science (American Association for the Advancement of Science) (22-11-2019)“…The metabolic characteristics of tumors present considerable hurdles to immune cell function and cancer immunotherapy. Using a glutamine antagonist, we…”
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Pharmacological mechanisms of 5-HT3 and tachykinin NK1 receptor antagonism to prevent chemotherapy-induced nausea and vomiting
Published in European journal of pharmacology (05-06-2012)“…Nausea and vomiting are among the most common and distressing consequences of cytotoxic chemotherapies. Nausea and vomiting can be acute (0–24h) or delayed…”
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6
Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis
Published in eLife (20-05-2014)“…Exchange of extracellular cystine for intracellular glutamate by the antiporter system xc (-) is implicated in numerous pathologies. Pharmacological agents…”
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Glucose-Independent Glutamine Metabolism via TCA Cycling for Proliferation and Survival in B Cells
Published in Cell metabolism (04-01-2012)“…Because MYC plays a causal role in many human cancers, including those with hypoxic and nutrient-poor tumor microenvironments, we have determined the metabolic…”
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Preventing Allograft Rejection by Targeting Immune Metabolism
Published in Cell reports (Cambridge) (27-10-2015)“…Upon antigen recognition and co-stimulation, T lymphocytes upregulate the metabolic machinery necessary to proliferate and sustain effector function. This…”
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Targeting glutamine metabolism enhances tumor-specific immunity by modulating suppressive myeloid cells
Published in The Journal of clinical investigation (01-07-2020)“…Myeloid cells comprise a major component of the tumor microenvironment (TME) that promotes tumor growth and immune evasion. By employing a small-molecule…”
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10
Combination therapy with BPTES nanoparticles and metformin targets the metabolic heterogeneity of pancreatic cancer
Published in Proceedings of the National Academy of Sciences - PNAS (06-09-2016)“…Targeting glutamine metabolism via pharmacological inhibition of glutaminase has been translated into clinical trials as a novel cancer therapy, but available…”
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Cambinol, a novel inhibitor of neutral sphingomyelinase 2 shows neuroprotective properties
Published in PloS one (26-05-2015)“…Ceramide is a bioactive lipid that plays an important role in stress responses leading to apoptosis, cell growth arrest and differentiation. Ceramide…”
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HIV-associated neurocognitive disorder — pathogenesis and prospects for treatment
Published in Nature reviews. Neurology (01-04-2016)“…Key Points Despite entering the era of combination antiretroviral therapy (CART), HIV-associated neurocognitive disorder (HAND) remains prevalent; however,…”
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Targeted inhibition of tumor-specific glutaminase diminishes cell-autonomous tumorigenesis
Published in The Journal of clinical investigation (01-06-2015)“…Glutaminase (GLS), which converts glutamine to glutamate, plays a key role in cancer cell metabolism, growth, and proliferation. GLS is being explored as a…”
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Therapeutic resurgence of 6-diazo-5-oxo-l-norleucine (DON) through tissue-targeted prodrugs
Published in Advances in pharmacology (1990) (2024)“…The recognition that rapidly proliferating cancer cells rely heavily on glutamine for their survival and growth has renewed interest in the development of…”
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Targeting Mitochondria in Tumor-Associated Macrophages using a Dendrimer-Conjugated TSPO Ligand that Stimulates Antitumor Signaling in Glioblastoma
Published in Biomacromolecules (14-09-2020)“…Mitochondria mediate critical cellular processes, including proliferation, apoptosis, and immune responses; as such, their dysfunction is pathogenic in many…”
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The pathogenesis of, and pharmacological treatment for, Canavan disease
Published in Drug discovery today (01-09-2022)“…[Display omitted] •Canavan disease (CD) is an inherited leukodystrophy resulting from mutations in the ASPA gene.•ASPA deficiency results in severe…”
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Phosphonates and Phosphonate Prodrugs in Medicinal Chemistry: Past Successes and Future Prospects
Published in Frontiers in chemistry (20-05-2022)“…Compounds with a phosphonate group, i.e., -P(O)(OH) group attached directly to the molecule a P-C bond serve as suitable non-hydrolyzable phosphate mimics in…”
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Mechanisms and latest clinical studies of new NK1 receptor antagonists for chemotherapy-induced nausea and vomiting: Rolapitant and NEPA (netupitant/palonosetron)
Published in Cancer treatment reviews (01-12-2015)“…Highlights • Nausea and delayed emesis in patients undergoing chemotherapy remain a challenge. • Data show that combined 5-HT3 receptor antagonists (RAs) and…”
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Maternal inflammation leads to impaired glutamate homeostasis and up-regulation of glutamate carboxypeptidase II in activated microglia in the fetal/newborn rabbit brain
Published in Neurobiology of disease (01-10-2016)“…Abstract Astrocyte dysfunction and excessive activation of glutamatergic systems has been implicated in a number of neurologic disorders, including…”
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Neuronal deletion of nSMase2 reduces the production of Aβ and directly protects neurons
Published in Neurobiology of disease (01-02-2023)“…Extracellular vesicles (EVs) have been proposed to regulate the deposition of Aβ. Multiple publications have shown that APP, amyloid processing enzymes and Aβ…”
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