Carborane-containing urea-based inhibitors of glutamate carboxypeptidase II: Synthesis and structural characterization
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F86652036%3A_____%2F15%3A00456306" target="_blank" >RIV/86652036:_____/15:00456306 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1016/j.bmcl.2015.09.062" target="_blank" >http://dx.doi.org/10.1016/j.bmcl.2015.09.062</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bmcl.2015.09.062" target="_blank" >10.1016/j.bmcl.2015.09.062</a>
Alternative languages
Result language
angličtina
Original language name
Carborane-containing urea-based inhibitors of glutamate carboxypeptidase II: Synthesis and structural characterization
Original language description
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 inhibitorat 1.79 angstrom 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. (C) 2015 Elsevier Ltd. All rights reserved.
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
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Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894X
e-ISSN
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Volume of the periodical
25
Issue of the periodical within the volume
22
Country of publishing house
GB - UNITED KINGDOM
Number of pages
5
Pages from-to
5232-5236
UT code for WoS article
000364535000044
EID of the result in the Scopus database
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