Glutamate Carboxypeptidase II (NAALADase) Inhibition as a Novel Therapeutic Strategy
2006GCP II inhibition decreases extracellular excitotoxic glutamate and increases extracellular NAAG, both of which provide neuroprotection. We have demonstrated with our potent and selective GCP II inhibitors efficacy in models of stroke, ALS and neuropathic pain.
Ajit G, Thomas +7 more
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Progress in the discovery and development of glutamate carboxypeptidase II inhibitors
Drug Discovery Today, 2007During the past 10 years, substantial progress has been made in the discovery and development of small molecule glutamate carboxypeptidase II (GCP II) inhibitors. These inhibitors have provided the necessary tools to investigate the physiological role of GCP II as well as the potential therapeutic benefits of its inhibition in neurological disorders of
Takashi, Tsukamoto +2 more
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Neuroprotection mediated by glutamate carboxypeptidase II (NAALADase) inhibition requires TGF-β
European Journal of Pharmacology, 2001Inhibition of glutamate carboxypeptidase (GCP) II (EC 3.4.17.21), also termed N-acetylated alpha-linked acidic dipeptidase (NAALADase), has been shown to protect against ischemic injury presumably via decreasing glutamate and increasing N-acetyl-aspartyl-glutamate (NAAG). NAAG is a potent and selective mGlu3 receptor agonist.
A G, Thomas +6 more
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Site-Directed Mutagenesis of Predicted Active Site Residues in Glutamate Carboxypeptidase II
Molecular Pharmacology, 1999Glutamate carboxypeptidase II (GCP II) catalyzes the extracellular hydrolysis of the neuromodulator N-acetyl-aspartylglutamate to N-acetyl-aspartate and glutamate. GCP II also hydrolyzes gamma-glutamyl bonds in folylpolyglutamate. The predicted amino acid sequence of GCP II displays similarities to aminopeptidases from Streptomyces griseus and Vibrio ...
H S, Speno +5 more
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Acetylation regulates the stability of glutamate carboxypeptidase II protein in human astrocytes
Biochemical and Biophysical Research Communications, 2014Glutamate carboxypeptidase II (GCPII) is known to be implicated in brain diseases such as schizophrenia and bipolar disorder, and dramatically increases in prostate cancer. Here, we investigated the regulation of GCPII expression in astrocytes and examined whether GCPII is epigenetically regulated through histone modification.
Ji-Young, Choi +2 more
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Synthesis and biological evaluation of hydroxamate-Based inhibitors of glutamate carboxypeptidase II
Bioorganic & Medicinal Chemistry Letters, 2003A series of hydroxamic acids has been prepared as potential inhibitors of glutamate carboxypeptidase II (GCP II). Compounds based on a P1' residue (primed-side inhibitors) were more potent than those based on a P1 group (unprimed-side inhibitors).
Doris, Stoermer +7 more
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Glutamate carboxypeptidase II levels in rodent brain using [125I]DCIT quantitative autoradiography
Neuroscience Letters, 2005The ability to visualize quantitatively glutamate carboxypeptidase II (GCPII) levels in vivo could advance our understanding of its function in health and disease. In the current study, we synthesized and evaluated a radiolabeled (iodine-125) analog of N-[N-[(S)-1,3-dicarboxypropyl]carbamoyl]-S-3-iodo-L-tyrosine (DCIT), a potent antagonist of GCPII ...
Guilarte, Tomás R. +6 more
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Enzymes | Glutamate Carboxypeptidase II (EC 3.4.17.21)
2021Joseph H. Neale, Stefano Costanzi
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Integrative oncology: Addressing the global challenges of cancer prevention and treatment
Ca-A Cancer Journal for Clinicians, 2022Jun J Mao,, Msce +2 more
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