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Carborane-containing urea-based inhibitors of glutamate carboxypeptidase II: Synthesis and structural characterization
S. Youn, KI. Kim, J. Ptacek, K. Ok, Z. Novakova, Y. Kim, J. Koo, C. Barinka, Y. Byun,
Jazyk angličtina Země Anglie, Velká Británie
Typ dokumentu časopisecké články, práce podpořená grantem
- MeSH
- glutamátkarboxypeptidasa II antagonisté a inhibitory ultrastruktura MeSH
- inhibitory enzymů chemická syntéza chemie farmakologie MeSH
- krystalografie rentgenová MeSH
- lidé MeSH
- močovina analogy a deriváty chemická syntéza chemie farmakologie MeSH
- sloučeniny boru chemická syntéza chemie farmakologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
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.
Biomedical Research Center Korea University Guro Hospital Korea University Seoul South Korea
College of Pharmacy Korea University 2511 Sejong ro Jochiwon eup Sejong 339 700 South Korea
Citace poskytuje Crossref.org
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- $a Youn, Sihyun $u College of Pharmacy, Korea University, 2511 Sejong-ro, Jochiwon-eup, Sejong 339-700, South Korea.
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- $a 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.
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- $a Novakova, Zora $u Institute of Biotechnology, Academy of Sciences of the Czech Republic, v.v.i., Laboratory of Structural Biology, Vídeňská 1083, 14220 Prague 4, Czech Republic.
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- $a Koo, JaeHyung $u Department of Brain Science, Daegu Gyeongbuk Institute of Science & Technology, 50-1 Sang-Ri, Hyeonpung-Myeon, Dalseong-Gun, Daegu 711-873, South Korea.
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- $a Barinka, Cyril $u Institute of Biotechnology, Academy of Sciences of the Czech Republic, v.v.i., Laboratory of Structural Biology, Vídeňská 1083, 14220 Prague 4, Czech Republic. Electronic address: cyril.barinka@ibt.cas.cz.
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- $a Byun, Youngjoo $u College of Pharmacy, Korea University, 2511 Sejong-ro, Jochiwon-eup, Sejong 339-700, South Korea; Biomedical Research Center, Korea University Guro Hospital, Korea University, Seoul, South Korea. Electronic address: yjbyun1@korea.ac.kr.
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