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Carborane-containing urea-based inhibitors of glutamate carboxypeptidase II: Synthesis and structural characterization
- Carborane-containing urea-based inhibitors of glutamate carboxypeptidase II: Synthesis and structural characterization
- Youn, S[Youn, Sihyun]; Kim, KI[Kim, Kyung Im]; Ptacek, J[Ptacek, Jakub]; Ok, K[Ok, Kiwon]; Novakova, Z[Novakova, Zora]; Kim, Y[Kim, YunHye]; Koo, J[Koo, JaeHyung]; Barinka, C[Barinka, Cyril]; Byun, Y[Byun, Youngjoo]
- DGIST Authors
- Koo, J[Koo, JaeHyung]
- Issue Date
- Bioorganic and Medicinal Chemistry Letters, 25(22), 5232-5236
- Article Type
- Analogs and Derivatives; Antagonists and Inhibitors; Boron Compounds; Boron Derivative; Carborane; Carborane Derivative; Chemistry; Controlled Study; Crystal Structure; Crystallography, X-Ray; Drug Synthesis; Enzyme Inhibitor; Enzyme Inhibitors; Glutamate Carboxypeptidase Ii; Glutamate Carboxypeptidase Ii Inhibitor; Human; Humans; Hydrogen Bond; Structure Analysis; Synthesis; Ultrastructure; Urea; X-Ray Crystal Structure; X Ray Crystallography
- 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 1.79 Å 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. © 2015 Elsevier Ltd. All rights reserved.
- Elsevier Ltd
- Related Researcher
Koo, Jae Hyung
The Koo Lab - ChemoReception Laboratory(CRLab)
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