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Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II
J. Tykvart, J. Schimer, A. Jančařík, J. Bařinková, V. Navrátil, J. Starková, K. Šrámková, J. Konvalinka, P. Majer, P. Šácha,
Journal of medicinal chemistry.
2015 ;
58 (10) :
4357-63.
[pub] 20150507
Language English Country United States
Document type Journal Article, Research Support, Non-U.S. Gov't
Persistent link
https://www.medvik.cz/link/bmc15031367
- MeSH
- Glutamate Carboxypeptidase II antagonists & inhibitors chemistry metabolism MeSH
- HEK293 Cells drug effects MeSH
- Enzyme Inhibitors chemistry metabolism pharmacology MeSH
- Protein Conformation MeSH
- Humans MeSH
- Urea chemistry MeSH
- Molecular Structure MeSH
- Drug Evaluation, Preclinical methods MeSH
- Drug Design MeSH
- Chemistry Techniques, Synthetic MeSH
- Binding Sites MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
We present here a structure-aided design of inhibitors targeting the active site as well as exosites of glutamate carboxypeptidase II (GCPII), a prostate cancer marker, preparing potent and selective inhibitors that are more than 1000-fold more active toward GCPII than its closest human homologue, glutamate carboxypeptidase III (GCPIII). Additionally, we demonstrate that the prepared inhibitor conjugate can be used for sensitive and selective imaging of GCPII in mammalian cells.
References provided by Crossref.org
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- $a Šácha, Pavel $u †Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i., Flemingovo n. 2, Prague 6, 166 10, Czech Republic. ‡Department of Biochemistry, Faculty of Science, Charles University, Albertov 6, Prague 2, 128 43, Czech Republic.
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