Robyn Wiseman
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View article: Mass spectrometry-guided discovery of novel GCPII inhibitor scaffolds
Mass spectrometry-guided discovery of novel GCPII inhibitor scaffolds Open
Introduction There is an unmet need for therapeutics with a novel mechanism to address Q9 symptoms associated with conditions where aberrant glutamatergic neurotransmission is presumed pathogenic. One enzyme of potential relevance is gluta…
View article: Inhibition of brain glutamate carboxypeptidase II (GCPII) to enhance cognitive function
Inhibition of brain glutamate carboxypeptidase II (GCPII) to enhance cognitive function Open
View article: Development of a high‐throughput dual‐stream liquid chromatography–tandem mass spectrometry method to screen for inhibitors of glutamate carboxypeptidase II
Development of a high‐throughput dual‐stream liquid chromatography–tandem mass spectrometry method to screen for inhibitors of glutamate carboxypeptidase II Open
Rationale Glutamate carboxypeptidase II (GCPII) catalyzes the hydrolysis of N ‐acetylaspartylglutamate (NAAG) to yield glutamate (Glu) and N ‐acetylaspartate (NAA). Inhibition of GCPII has been shown to remediate the neurotoxicity of exces…
View article: Nelfinavir inhibition of Kaposi’s sarcoma-associated herpesvirus protein expression and capsid assembly
Nelfinavir inhibition of Kaposi’s sarcoma-associated herpesvirus protein expression and capsid assembly Open
View article: Brain N-acetyl-aspartyl-glutamate is associated with cognitive function in older virally suppressed people with HIV
Brain N-acetyl-aspartyl-glutamate is associated with cognitive function in older virally suppressed people with HIV Open
Objectives: Cognitive impairment persists in virally suppressed people with HIV (VS-PWH) especially in higher order domains. One cortical circuit, linked to these domains, is regulated by N -acetyl-aspartyl glutamate (NAAG), the endogenous…
View article: Nelfinavir Inhibition of Kaposi’s sarcoma-associated herpesvirus protein expression and capsid assembly
Nelfinavir Inhibition of Kaposi’s sarcoma-associated herpesvirus protein expression and capsid assembly Open
Background Antiviral therapies that target herpesviruses are clinically important. Nelfinavir is a protease inhibitor that targets the human immunodeficiency virus (HIV) infections aspartyl protease. Previous studies demonstrated that this…
View article: Chronic GCPII (glutamate‐carboxypeptidase‐II) inhibition reduces pT217Tau levels in the entorhinal and dorsolateral prefrontal cortices of aged macaques
Chronic GCPII (glutamate‐carboxypeptidase‐II) inhibition reduces pT217Tau levels in the entorhinal and dorsolateral prefrontal cortices of aged macaques Open
Introduction Current approaches for treating sporadic Alzheimer's disease (sAD) focus on removal of amyloid beta 1‐42 (Aβ 1‐42 ) or phosphorylated tau, but additional strategies are needed to reduce neuropathology at earlier stages prior t…
View article: Degrading stimuli by reducing image resolution impairs performance in a rodent continuous performance test
Degrading stimuli by reducing image resolution impairs performance in a rodent continuous performance test Open
View article: D-DOPA Is a Potent, Orally Bioavailable, Allosteric Inhibitor of Glutamate Carboxypeptidase II
D-DOPA Is a Potent, Orally Bioavailable, Allosteric Inhibitor of Glutamate Carboxypeptidase II Open
Glutamate carboxypeptidase-II (GCPII) is a zinc-dependent metalloenzyme implicated in numerous neurological disorders. The pharmacophoric requirements of active-site GCPII inhibitors makes them highly charged, manifesting poor pharmacokine…
View article: Neuroprotective Effects of σ <sub>2</sub> R/TMEM97 Receptor Modulators in the Neuronal Model of Huntington’s Disease
Neuroprotective Effects of σ <sub>2</sub> R/TMEM97 Receptor Modulators in the Neuronal Model of Huntington’s Disease Open
Huntington's disease (HD) is a genetic neurodegenerative disease caused by an expanded CAG repeat in the Huntingtin (HTT) gene that encodes for an expanded polyglutamine (polyQ) repeat in exon-1 of the human mutant huntingtin…
View article: Neuroprotective Effects of σ2R/TMEM97 Receptor Modulators in Neuronal Model of Huntington's Disease
Neuroprotective Effects of σ2R/TMEM97 Receptor Modulators in Neuronal Model of Huntington's Disease Open
Huntington's disease (HD) is a genetic neurodegenerative disease caused by an expanded CAG repeat in the human Huntingtin gene (HTT) that yields an expanded polyglutamine (polyQ) repeat in exon-1 of the human mutant huntingtin (mHTT) prote…
View article: Dendrimer-2PMPA selectively blocks upregulated microglial GCPII activity and improves cognition in a mouse model of multiple sclerosis
Dendrimer-2PMPA selectively blocks upregulated microglial GCPII activity and improves cognition in a mouse model of multiple sclerosis Open
Cognitive impairment is a common aspect of multiple sclerosis (MS) for which there are no treatments. Reduced brain N-acetylaspartylglutamate (NAAG) levels are linked to impaired cognition in various neurological diseases, including…
View article: Stimulus degradation impairs performance in a rodent continuous performance test
Stimulus degradation impairs performance in a rodent continuous performance test Open
Sustained attention is a core cognitive domain that is often disrupted in neuropsychiatric disorders. Continuous performance tests (CPTs) are the most common clinical assay of sustained attention. In CPTs, participants produce a behavioral…