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• W1756852897 abstract "Glutamate carboxypeptidase II (GCPII) is a zinc metalloprotease on the surface of astrocytes which cleaves N-acetylaspartylglutamate to release N-acetylaspartate and glutamate. GCPII inhibitors can decrease glutamate concentration and play a protective role against apoptosis or degradation of brain neurons. Herein, we report the synthesis and structural analysis of novel carborane-based GCPII inhibitors. We determined the X-ray crystal structure of GCPII in complex with a carborane-containing inhibitor at 1.79Å resolution. The X-ray analysis revealed that the bulky closo-carborane cluster is located in the spacious entrance funnel region of GCPII, indicating that the carborane cluster can be further structurally modified to identify promising lead structures of novel GCPII inhibitors." @default.
• W1756852897 created "2016-06-24" @default.
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• W1756852897 date "2015-11-01" @default.
• W1756852897 modified "2023-10-16" @default.
• W1756852897 title "Carborane-containing urea-based inhibitors of glutamate carboxypeptidase II: Synthesis and structural characterization" @default.
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• W1756852897 doi "https://doi.org/10.1016/j.bmcl.2015.09.062" @default.
• W1756852897 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26459214" @default.
• W1756852897 hasPublicationYear "2015" @default.
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