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Clinical development of metabolic inhibitors for oncology

The Journal of clinical investigation, 2022-01, Vol.132 (1), p.1-15

2022

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Small Molecule Inhibitors Targeting Biosynthesis of Ceramide, the Central Hub of the Sphingolipid Network

Journal of medicinal chemistry, 2021-01, Vol.64 (1), p.279-297

2021

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We're Not "DON" Yet: Optimal Dosing and Prodrug Delivery of 6-Diazo-5-oxo-L-norleucine

Molecular cancer therapeutics, 2018-09, Vol.17 (9), p.1824-1832

2018

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Glutamine blockade induces divergent metabolic programs to overcome tumor immune evasion

Science (American Association for the Advancement of Science), 2019-11, Vol.366 (6468), p.1013-1021

2019

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Pharmacological mechanisms of 5-HT3 and tachykinin NK1 receptor antagonism to prevent chemotherapy-induced nausea and vomiting

European journal of pharmacology, 2012-06, Vol.684 (1-3), p.1-7

2012

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Preventing Allograft Rejection by Targeting Immune Metabolism

Cell reports (Cambridge), 2015-10, Vol.13 (4), p.760-770

2015

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Cambinol, a novel inhibitor of neutral sphingomyelinase 2 shows neuroprotective properties

PloS one, 2015-05, Vol.10 (5), p.e0124481-e0124481

2015

Volltextzugriff (PDF)

HIV-associated neurocognitive disorder--pathogenesis and prospects for treatment

Nature reviews. Neurology, 2016-04, Vol.12 (4), p.234

2016

Volltextzugriff (PDF)

Targeting glutamine metabolism enhances tumor-specific immunity by modulating suppressive myeloid cells

The Journal of clinical investigation, 2020-07, Vol.130 (7), p.3865-3884

2020

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Targeted inhibition of tumor-specific glutaminase diminishes cell-autonomous tumorigenesis

The Journal of clinical investigation, 2015-06, Vol.125 (6), p.2293-2306

2015

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Neuronal deletion of nSMase2 reduces the production of Aβ and directly protects neurons

Neurobiology of disease, 2023-02, Vol.177, p.105987, Article 105987

2023

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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

Neurobiology of disease, 2016-10, Vol.94, p.116-128

2016

Volltextzugriff (PDF)

Neuromuscular NMDA Receptors Modulate Developmental Synapse Elimination

The Journal of neuroscience, 2016-08, Vol.36 (34), p.8783-8789

2016

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Inhibition of substance P-mediated responses in NG108-15 cells by netupitant and palonosetron exhibit synergistic effects

European journal of pharmacology, 2012-08, Vol.689 (1-3), p.25-30

2012

Volltextzugriff (PDF)

A gut-restricted glutamate carboxypeptidase II inhibitor reduces monocytic inflammation and improves preclinical colitis

Science translational medicine, 2023-08, Vol.15 (708), p.eabn7491

2023

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Glutamine metabolism inhibition has dual immunomodulatory and antibacterial activities against Mycobacterium tuberculosis

Nature communications, 2023-11, Vol.14 (1), p.7427-7427, Article 7427

2023

Volltextzugriff (PDF)

Discovery of a para-Acetoxy-benzyl Ester Prodrug of a Hydroxamate-Based Glutamate Carboxypeptidase II Inhibitor as Oral Therapy for Neuropathic Pain

Journal of medicinal chemistry, 2017-09, Vol.60 (18), p.7799-7809

2017

Volltextzugriff (PDF)

Nipping disease in the bud: nSMase2 inhibitors as therapeutics in extracellular vesicle-mediated diseases

Drug discovery today, 2021-07, Vol.26 (7), p.1656-1668

2021

Volltextzugriff (PDF)

Selective CNS Uptake of the GCP-II Inhibitor 2-PMPA following Intranasal Administration

PloS one, 2015-07, Vol.10 (7), p.e0131861-e0131861

2015

Volltextzugriff (PDF)

Discovery of 6‑Diazo-5-oxo‑l‑norleucine (DON) Prodrugs with Enhanced CSF Delivery in Monkeys: A Potential Treatment for Glioblastoma

Journal of medicinal chemistry, 2016-09, Vol.59 (18), p.8621-8633

2016

Volltextzugriff (PDF)

Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells

Experimental brain research, 2014-08, Vol.232 (8), p.2637-2644

2014

Volltextzugriff (PDF)

Discovery of Orally Bioavailable and Brain-Penetrable Prodrugs of the Potent nSMase2 Inhibitor DPTIP

Journal of medicinal chemistry, 2022-08, Vol.65 (16), p.11111-11125

2022

Volltextzugriff (PDF)

Targeting the Glutamatergic System for the Treatment of HIV-Associated Neurocognitive Disorders

Journal of neuroimmune pharmacology, 2013-06, Vol.8 (3), p.594-607

2013

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MRI demonstrates glutamine antagonist-mediated reversal of cerebral malaria pathology in mice

Proceedings of the National Academy of Sciences - PNAS, 2018-12, Vol.115 (51), p.E12024-E12033

2018

Volltextzugriff (PDF)

Neutral sphingomyelinase 2 inhibition attenuates extracellular vesicle release and improves neurobehavioral deficits in murine HIV

Neurobiology of disease, 2022-07, Vol.169, p.105734-105734, Article 105734

2022

Volltextzugriff (PDF)

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Clinical development of metabolic inhibitors for oncology

Small Molecule Inhibitors Targeting Biosynthesis of Ceramide, the Central Hub of the Sphingolipid Network

We're Not "DON" Yet: Optimal Dosing and Prodrug Delivery of 6-Diazo-5-oxo-L-norleucine

Glutamine blockade induces divergent metabolic programs to overcome tumor immune evasion

Pharmacological mechanisms of 5-HT3 and tachykinin NK1 receptor antagonism to prevent chemotherapy-induced nausea and vomiting

Preventing Allograft Rejection by Targeting Immune Metabolism

Cambinol, a novel inhibitor of neutral sphingomyelinase 2 shows neuroprotective properties

HIV-associated neurocognitive disorder--pathogenesis and prospects for treatment

Targeting glutamine metabolism enhances tumor-specific immunity by modulating suppressive myeloid cells

Targeted inhibition of tumor-specific glutaminase diminishes cell-autonomous tumorigenesis

Neuronal deletion of nSMase2 reduces the production of Aβ and directly protects neurons

Maternal inflammation leads to impaired glutamate homeostasis and up-regulation of glutamate carboxypeptidase II in activated microglia in the fetal/newborn rabbit brain

Neuromuscular NMDA Receptors Modulate Developmental Synapse Elimination

Inhibition of substance P-mediated responses in NG108-15 cells by netupitant and palonosetron exhibit synergistic effects

A gut-restricted glutamate carboxypeptidase II inhibitor reduces monocytic inflammation and improves preclinical colitis

Glutamine metabolism inhibition has dual immunomodulatory and antibacterial activities against Mycobacterium tuberculosis

Discovery of a para-Acetoxy-benzyl Ester Prodrug of a Hydroxamate-Based Glutamate Carboxypeptidase II Inhibitor as Oral Therapy for Neuropathic Pain

Nipping disease in the bud: nSMase2 inhibitors as therapeutics in extracellular vesicle-mediated diseases

Selective CNS Uptake of the GCP-II Inhibitor 2-PMPA following Intranasal Administration

Discovery of 6‑Diazo-5-oxo‑l‑norleucine (DON) Prodrugs with Enhanced CSF Delivery in Monkeys: A Potential Treatment for Glioblastoma

Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells

Discovery of Orally Bioavailable and Brain-Penetrable Prodrugs of the Potent nSMase2 Inhibitor DPTIP

Targeting the Glutamatergic System for the Treatment of HIV-Associated Neurocognitive Disorders

MRI demonstrates glutamine antagonist-mediated reversal of cerebral malaria pathology in mice

Neutral sphingomyelinase 2 inhibition attenuates extracellular vesicle release and improves neurobehavioral deficits in murine HIV

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