List of works - Barbara S Slusher

2-MPPA, a selective glutamate carboxypeptidase II inhibitor, attenuates morphine tolerance but not dependence in C57/Bl mice

scientific article published on 12 October 2005

6-Hydroxy-1,2,4-triazine-3,5(2H,4H)-dione Derivatives as Novel D-Amino Acid Oxidase Inhibitors

scientific article published on 26 August 2015

A novel and potent brain penetrant inhibitor of extracellular vesicle release

scientific article published on 04 September 2019

Activation of MrgC receptor inhibits N-type calcium channels in small-diameter primary sensory neurons in mice

scientific article

Amino acids at the N- and C-termini of human glutamate carboxypeptidase II are required for enzymatic activity and proper folding.

scientific article

An efficient synthetic route to l-γ-methyleneglutamine and its amide derivatives, and their selective anticancer activity

scientific article published on 10 February 2021

Bioanalysis of 6-diazo-5-oxo-l-norleucine in plasma and brain by ultra-performance liquid chromatography mass spectrometry

scientific article published on 10 January 2015

Biodistribution, tumor detection, and radiation dosimetry of 18F-DCFBC, a low-molecular-weight inhibitor of prostate-specific membrane antigen, in patients with metastatic prostate cancer

scientific article published on December 2012

Bringing together the academic drug discovery community

scientific article

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

scientific article

Combination therapy with BPTES nanoparticles and metformin targets the metabolic heterogeneity of pancreatic cancer

scientific article published on 24 August 2016

Correction: JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress.

scientific article published on 13 March 2019

D-Amino acid oxidase inhibitors based on the 5-hydroxy-1,2,4-triazin-6(1H)-one scaffold.

scientific article published on 23 February 2016

D-Amino-Acid Oxidase Inhibition Increases D-Serine Plasma Levels in Mouse But not in Monkey or Dog.

scientific article published on 16 October 2015

Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors.

scientific article published on 30 November 2012

Design, synthesis, and pharmacological evaluation of fluorinated tetrahydrouridine derivatives as inhibitors of cytidine deaminase

scientific article published on 24 February 2014

Development of a High-Throughput Fluorescence Polarization Assay to Identify Novel Ligands of Glutamate Carboxypeptidase II ⬇️

scientific article published on June 29, 2012

Development of a high-throughput method for the determination of pharmacological levels of plasma D-serine.

scientific article published on 16 August 2011

Development of a primary microglia screening assay and its use to characterize inhibition of system xc- by erastin and its analogs

scientific article published on 17 January 2017

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

scientific article published on 25 August 2016

Discovery of Benzamidine- and 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists

scientific article published on 09 September 2019

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

scientific article published on 31 July 2017

Dose-dependent inhibition of GCPII to prevent and treat cognitive impairment in the EAE model of multiple sclerosis

scientific article published on 26 January 2016

Effect of 2-(phosphono-methyl)-pentanedioic acid on allodynia and afferent ectopic discharges in a rat model of neuropathic pain

scientific article (publication date: February 2002)

Effect of middle cerebral artery occlusion on mRNA expression for the sodium-coupled vitamin C transporter SVCT2 in rat brain

scientific journal article

Enhanced Brain Delivery of 2-(Phosphonomethyl)pentanedioic Acid Following Intranasal Administration of Its γ-Substituted Ester Prodrugs

scientific article

Enhanced Oral Bioavailability of 2-(Phosphonomethyl)-pentanedioic Acid (2-PMPA) from its (5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl (ODOL)-Based Prodrugs

scientific article published on 24 September 2019

GCP II (NAALADase) inhibition suppresses mossy fiber-CA3 synaptic neurotransmission by a presynaptic mechanism

scientific article

Gastrointestinal delivery of propofol from fospropofol: its bioavailability and activity in rodents and human volunteers

scientific article published on 29 May 2015

Glucose-independent glutamine metabolism via TCA cycling for proliferation and survival in B cells

scientific journal article

Glutamate carboxypeptidase II (NAALADase) inhibition as a novel therapeutic strategy

scientific article published on January 2006

Glutamate carboxypeptidase II inhibition behaviorally and physiologically improves pyridoxine-induced neuropathy in rats

scientific article

Glutamate carboxypeptidase II inhibition protects motor neurons from death in familial amyotrophic lateral sclerosis models

scientific journal article

Glutamate carboxypeptidase II is not an amyloid peptide-degrading enzyme.

scientific article

Glutamine blockade induces divergent metabolic programs to overcome tumor immune evasion

scientific article published on 07 November 2019

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

scientific article

High-Throughput Assay Development for Cystine-Glutamate Antiporter (xc-) Highlights Faster Cystine Uptake than Glutamate Release in Glioma Cells

scientific article

High-affinity near-infrared fluorescent small-molecule contrast agents for in vivo imaging of prostate-specific membrane antigen

scientific article

Identification of the N-glycosylation sites on glutamate carboxypeptidase II necessary for proteolytic activity

scientific article

Inhibition of NAALADase by 2-PMPA attenuates cocaine-induced relapse in rats: a NAAG-mGluR2/3-mediated mechanism

scientific article

Inhibition of glutamate carboxypeptidase II (GCPII) activity as a treatment for cognitive impairment in multiple sclerosis

scientific article

Inhibition of mTORC1 in pediatric low-grade glioma depletes glutathione and therapeutically synergizes with carboplatin

scientific article published on 01 February 2019

Inhibition of neutral sphingomyelinase 2 promotes remyelination

scientific article published on 02 October 2020

Inhibition of xc- transporter-mediated cystine uptake by sulfasalazine analogs ⬇️

scientific article published on August 12, 2011

Investigation of Novel Primary and Secondary Pharmacophores and 3-Substitution in the Linking Chain of a Series of Highly Selective and Bitopic Dopamine D3 Receptor Antagonists and Partial Agonists

scientific article published on 15 October 2019

JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress

scientific article published on 13 August 2018

Kinetic characterization of ebselen, chelerythrine and apomorphine as glutaminase inhibitors

scientific article

Kinetics and inhibition of glutamate carboxypeptidase II using a microplate assay

scientific article (publication date: November 2002)

Looking for Drugs in All the Wrong Places: Use of GCPII Inhibitors Outside the Brain

scientific article published on 20 November 2019

MBRS-61. IN VIVO METABOLOMICS REVEALS A POTENT COMBINATION THERAPY FOR MYC-DRIVEN MEDULLOBLASTOMA.

scientific article published on 22 June 2018

Mice lacking glutamate carboxypeptidase II are protected from peripheral neuropathy and ischemic brain injury

scientific article

Mouse brain serine racemase catalyzes specific elimination of L-serine to pyruvate

scientific article (publication date: 30 January 2003)

Mutant disrupted-in-schizophrenia 1 in astrocytes: focus on glutamate metabolism

scientific article published on 8 August 2014

N-(Pivaloyloxy)alkoxy-carbonyl Prodrugs of the Glutamine Antagonist 6-Diazo-5-oxo-l-norleucine (DON) as a Potential Treatment for HIV Associated Neurocognitive Disorders.

scientific article

N-Substituted Prodrugs of Mebendazole Provide Improved Aqueous Solubility and Oral Bioavailability in Mice and Dogs

scientific article published on 19 April 2018

Neurological sequelae induced by alphavirus infection of the CNS are attenuated by treatment with the glutamine antagonist 6-diazo-5-oxo-l-norleucine

scientific article

Neuropathy-inducing effects of eribulin mesylate versus paclitaxel in mice with preexisting neuropathy

scientific article

New approaches to chemotherapy-induced nausea and vomiting: from neuropharmacology to clinical investigations

scientific article published on September 2006

New therapeutic and biomarker discovery for peripheral diabetic neuropathy: PARP inhibitor, nitrotyrosine, and tumor necrosis factor-{alpha}

scientific article

Oral administration of D-alanine in monkeys robustly increases plasma and cerebrospinal fluid levels but experimental D-amino acid oxidase inhibitors had minimal effect

scientific article published on 10 June 2016

Oral administration of the NAALADase inhibitor GPI-5693 attenuates cocaine-induced reinstatement of drug-seeking behavior in rats.

scientific article

Orally bioavailable glutamine antagonist prodrug JHU-083 penetrates mouse brain and suppresses the growth of MYC-driven medulloblastoma

scientific article published on 21 July 2019

PARP inhibition or gene deficiency counteracts intraepidermal nerve fiber loss and neuropathic pain in advanced diabetic neuropathy

scientific article

Palonosetron exhibits unique molecular interactions with the 5-HT3 receptor

scientific article

Palonosetron triggers 5-HT(3) receptor internalization and causes prolonged inhibition of receptor function

scientific article published on 15 October 2009

Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors.

scientific article

Pharmacokinetics and pharmacodynamics of the glutamate carboxypeptidase II inhibitor 2-MPPA show prolonged alleviation of neuropathic pain through an indirect mechanism

scientific article

Pharmacokinetics of Intranasal versus Subcutaneous Insulin in the Mouse.

scientific article published on 19 December 2017

Pharmacokinetics of Oral d-Serine in d-Amino Acid Oxidase Knockout Mice ⬇️

scientific article published on July 26, 2012

Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis

scientific article

Poly(ADP-ribose) polymerase (PARP) inhibition counteracts multiple manifestations of kidney disease in long-term streptozotocin-diabetic rat model

scientific article

Prostate-specific membrane antigen (PSMA)-mediated laminin proteolysis generates a pro-angiogenic peptide

scientific article published on 8 July 2016

Protection against glucose-induced neuronal death by NAAG and GCP II inhibition is regulated by mGluR3

scientific article

Regional brain distribution of translocator protein using [(11)C]DPA-713 PET in individuals infected with HIV.

scientific article

Reversible Disulfide Formation of the Glutamate Carboxypeptidase II Inhibitor E2072 Results in Prolonged Systemic Exposures In Vivo ⬇️

scientific article published on September 4, 2012

Role of Academic Drug Discovery in the Quest for New CNS Therapeutics

scientific article

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

scientific article published on 7 July 2015

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

scientific article published on 04 January 2021

Small molecule glutaminase inhibitors block glutamate release from stimulated microglia

scientific article

Sowing the Seeds of Discovery: Tau-Propagation Models of Alzheimer's Disease

scientific article published on 13 October 2020

Structural Basis of Interactions between Human Glutamate Carboxypeptidase II and Its Substrate Analogs

scientific article

Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II

scientific article

Structure of glutamate carboxypeptidase II, a drug target in neuronal damage and prostate cancer

scientific article

Structure-Activity Relationship Studies on a Series of 3α-[Bis(4-fluorophenyl)methoxy]tropanes and 3α-[Bis(4-fluorophenyl)methylamino]tropanes As Novel Atypical Dopamine Transporter (DAT) Inhibitors for the Treatment of Cocaine Use Disorders

scientific article

Structure-Activity Relationships for a Series of (Bis(4-fluorophenyl)methyl)sulfinyl Alkyl Alicyclic Amines at the Dopamine Transporter: Functionalizing the Terminal Nitrogen Affects Affinity, Selectivity, and Metabolic Stability

scientific article published on 14 November 2019

Structure-Metabolism Relationships in the Glucuronidation of d-Amino Acid Oxidase Inhibitors.

scientific article

Substrate specificity, inhibition and enzymological analysis of recombinant human glutamate carboxypeptidase II.

scientific article published in February 2002

Synthesis and Biological Evaluation of Low Molecular Weight Fluorescent Imaging Agents for the Prostate-Specific Membrane Antigen ⬇️

scientific article published on December 4, 2012

Synthesis and SAR of 1-hydroxy-1H-benzo[d]imidazol-2(3H)-ones as Inhibitors of D-Amino Acid Oxidase.

scientific article

Synthesis of kojic acid derivatives as secondary binding site probes of D-amino acid oxidase

scientific article published on May 2013

Targeting the glutamatergic system for the treatment of HIV-associated neurocognitive disorders

scientific article published on 4 April 2013

The Antiemetic 5-HT3 Receptor Antagonist Palonosetron Inhibits Substance P-Mediated Responses In Vitro and In Vivo ⬇️

scientific article published on August 19, 2010

The NAAG'ing Concerns of Modeling Human Alzheimer's Disease in Mice

scientific article published on 01 January 2019

The Novel Glutamine Antagonist Prodrug JHU395 Has Antitumor Activity in Malignant Peripheral Nerve Sheath Tumor

scientific article published on 08 October 2019

The Psychiatric Impact of HIV.

scientific article published on 24 May 2017

The Significance of Chirality in Drug Design and Synthesis of Bitopic Ligands as D3 Receptor (D3R) Selective Agonists

scientific article published on 01 July 2019

Tumor-Targeted Delivery of 6-Diazo-5-oxo-l-norleucine (DON) Using Substituted Acetylated Lysine Prodrugs

scientific article published on 29 March 2019

Unbiased Metabolic Profiling Predicts Sensitivity of High MYC-Expressing Atypical Teratoid/Rhabdoid Tumors to Glutamine Inhibition with 6-Diazo-5-Oxo-L-Norleucine

scientific article published on 12 July 2019

Unprecedented Binding Mode of Hydroxamate-Based Inhibitors of Glutamate Carboxypeptidase II: Structural Characterization and Biological Activity

scientific article

Using click chemistry toward novel 1,2,3-triazole-linked dopamine D3 receptor ligands

scientific article published on 17 January 2015

δ-Thiolactones as prodrugs of thiol-based glutamate carboxypeptidase II (GCPII) inhibitors

scientific article published on 27 December 2013

List of works by Barbara S Slusher

2-MPPA, a selective glutamate carboxypeptidase II inhibitor, attenuates morphine tolerance but not dependence in C57/Bl mice

6-Hydroxy-1,2,4-triazine-3,5(2H,4H)-dione Derivatives as Novel D-Amino Acid Oxidase Inhibitors

A novel and potent brain penetrant inhibitor of extracellular vesicle release

Activation of MrgC receptor inhibits N-type calcium channels in small-diameter primary sensory neurons in mice

Amino acids at the N- and C-termini of human glutamate carboxypeptidase II are required for enzymatic activity and proper folding.

An efficient synthetic route to l-γ-methyleneglutamine and its amide derivatives, and their selective anticancer activity

Bioanalysis of 6-diazo-5-oxo-l-norleucine in plasma and brain by ultra-performance liquid chromatography mass spectrometry

Biodistribution, tumor detection, and radiation dosimetry of 18F-DCFBC, a low-molecular-weight inhibitor of prostate-specific membrane antigen, in patients with metastatic prostate cancer

Bringing together the academic drug discovery community

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

Combination therapy with BPTES nanoparticles and metformin targets the metabolic heterogeneity of pancreatic cancer

Correction: JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress.

D-Amino acid oxidase inhibitors based on the 5-hydroxy-1,2,4-triazin-6(1H)-one scaffold.

D-Amino-Acid Oxidase Inhibition Increases D-Serine Plasma Levels in Mouse But not in Monkey or Dog.

Design, synthesis, and pharmacological evaluation of bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide 3 (BPTES) analogs as glutaminase inhibitors.

Design, synthesis, and pharmacological evaluation of fluorinated tetrahydrouridine derivatives as inhibitors of cytidine deaminase

Development of a High-Throughput Fluorescence Polarization Assay to Identify Novel Ligands of Glutamate Carboxypeptidase II ⬇️

Development of a high-throughput method for the determination of pharmacological levels of plasma D-serine.

Development of a primary microglia screening assay and its use to characterize inhibition of system xc- by erastin and its analogs

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

Discovery of Benzamidine- and 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists

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

Dose-dependent inhibition of GCPII to prevent and treat cognitive impairment in the EAE model of multiple sclerosis

Effect of 2-(phosphono-methyl)-pentanedioic acid on allodynia and afferent ectopic discharges in a rat model of neuropathic pain

Effect of middle cerebral artery occlusion on mRNA expression for the sodium-coupled vitamin C transporter SVCT2 in rat brain

Enhanced Brain Delivery of 2-(Phosphonomethyl)pentanedioic Acid Following Intranasal Administration of Its γ-Substituted Ester Prodrugs

Enhanced Oral Bioavailability of 2-(Phosphonomethyl)-pentanedioic Acid (2-PMPA) from its (5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl (ODOL)-Based Prodrugs

GCP II (NAALADase) inhibition suppresses mossy fiber-CA3 synaptic neurotransmission by a presynaptic mechanism

Gastrointestinal delivery of propofol from fospropofol: its bioavailability and activity in rodents and human volunteers

Glucose-independent glutamine metabolism via TCA cycling for proliferation and survival in B cells

Glutamate carboxypeptidase II (NAALADase) inhibition as a novel therapeutic strategy

Glutamate carboxypeptidase II inhibition behaviorally and physiologically improves pyridoxine-induced neuropathy in rats

Glutamate carboxypeptidase II inhibition protects motor neurons from death in familial amyotrophic lateral sclerosis models

Glutamate carboxypeptidase II is not an amyloid peptide-degrading enzyme.

Glutamine blockade induces divergent metabolic programs to overcome tumor immune evasion

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

High-Throughput Assay Development for Cystine-Glutamate Antiporter (xc-) Highlights Faster Cystine Uptake than Glutamate Release in Glioma Cells

High-affinity near-infrared fluorescent small-molecule contrast agents for in vivo imaging of prostate-specific membrane antigen

Identification of the N-glycosylation sites on glutamate carboxypeptidase II necessary for proteolytic activity

Inhibition of NAALADase by 2-PMPA attenuates cocaine-induced relapse in rats: a NAAG-mGluR2/3-mediated mechanism

Inhibition of glutamate carboxypeptidase II (GCPII) activity as a treatment for cognitive impairment in multiple sclerosis

Inhibition of mTORC1 in pediatric low-grade glioma depletes glutathione and therapeutically synergizes with carboplatin

Inhibition of neutral sphingomyelinase 2 promotes remyelination

Inhibition of xc- transporter-mediated cystine uptake by sulfasalazine analogs ⬇️

Investigation of Novel Primary and Secondary Pharmacophores and 3-Substitution in the Linking Chain of a Series of Highly Selective and Bitopic Dopamine D3 Receptor Antagonists and Partial Agonists

JHU-083 selectively blocks glutaminase activity in brain CD11b+ cells and prevents depression-associated behaviors induced by chronic social defeat stress

Kinetic characterization of ebselen, chelerythrine and apomorphine as glutaminase inhibitors

Kinetics and inhibition of glutamate carboxypeptidase II using a microplate assay

Looking for Drugs in All the Wrong Places: Use of GCPII Inhibitors Outside the Brain

MBRS-61. IN VIVO METABOLOMICS REVEALS A POTENT COMBINATION THERAPY FOR MYC-DRIVEN MEDULLOBLASTOMA.

Mice lacking glutamate carboxypeptidase II are protected from peripheral neuropathy and ischemic brain injury

Mouse brain serine racemase catalyzes specific elimination of L-serine to pyruvate

Mutant disrupted-in-schizophrenia 1 in astrocytes: focus on glutamate metabolism

N-(Pivaloyloxy)alkoxy-carbonyl Prodrugs of the Glutamine Antagonist 6-Diazo-5-oxo-l-norleucine (DON) as a Potential Treatment for HIV Associated Neurocognitive Disorders.

N-Substituted Prodrugs of Mebendazole Provide Improved Aqueous Solubility and Oral Bioavailability in Mice and Dogs

Neurological sequelae induced by alphavirus infection of the CNS are attenuated by treatment with the glutamine antagonist 6-diazo-5-oxo-l-norleucine

Neuropathy-inducing effects of eribulin mesylate versus paclitaxel in mice with preexisting neuropathy

New approaches to chemotherapy-induced nausea and vomiting: from neuropharmacology to clinical investigations

New therapeutic and biomarker discovery for peripheral diabetic neuropathy: PARP inhibitor, nitrotyrosine, and tumor necrosis factor-{alpha}

Oral administration of D-alanine in monkeys robustly increases plasma and cerebrospinal fluid levels but experimental D-amino acid oxidase inhibitors had minimal effect

Oral administration of the NAALADase inhibitor GPI-5693 attenuates cocaine-induced reinstatement of drug-seeking behavior in rats.

Orally bioavailable glutamine antagonist prodrug JHU-083 penetrates mouse brain and suppresses the growth of MYC-driven medulloblastoma

PARP inhibition or gene deficiency counteracts intraepidermal nerve fiber loss and neuropathic pain in advanced diabetic neuropathy

Palonosetron exhibits unique molecular interactions with the 5-HT3 receptor

Palonosetron triggers 5-HT(3) receptor internalization and causes prolonged inhibition of receptor function

Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors.

Pharmacokinetics and pharmacodynamics of the glutamate carboxypeptidase II inhibitor 2-MPPA show prolonged alleviation of neuropathic pain through an indirect mechanism

Pharmacokinetics of Intranasal versus Subcutaneous Insulin in the Mouse.

Pharmacokinetics of Oral d-Serine in d-Amino Acid Oxidase Knockout Mice ⬇️

Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis

Poly(ADP-ribose) polymerase (PARP) inhibition counteracts multiple manifestations of kidney disease in long-term streptozotocin-diabetic rat model

Prostate-specific membrane antigen (PSMA)-mediated laminin proteolysis generates a pro-angiogenic peptide

Protection against glucose-induced neuronal death by NAAG and GCP II inhibition is regulated by mGluR3

Regional brain distribution of translocator protein using [(11)C]DPA-713 PET in individuals infected with HIV.

Reversible Disulfide Formation of the Glutamate Carboxypeptidase II Inhibitor E2072 Results in Prolonged Systemic Exposures In Vivo ⬇️

Role of Academic Drug Discovery in the Quest for New CNS Therapeutics

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

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

Small molecule glutaminase inhibitors block glutamate release from stimulated microglia