Structural characterization of P1′-diversified urea-based inhibitors of glutamate carboxypeptidase II

Urea-based inhibitors of human glutamate carboxypeptidase II (GCPII) have advanced into clinical trials for imaging metastatic prostate cancer. In parallel efforts, agents with increased lipophilicity have been designed and evaluated for targeting GCPII residing within the neuraxis. Here we report t...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-05, Vol.24 (10), p.2340-2345
Hauptverfasser:	Pavlicek, Jiri, Ptacek, Jakub, Cerny, Jiri, Byun, Youngjoo, Skultetyova, Lubica, Pomper, Martin G., Lubkowski, Jacek, Barinka, Cyril
Format:	Artikel
Sprache:	eng
Schlagworte:	Antigens, Surface - chemistry Crystallography, X-Ray Drug Design Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology GCPII Glutamate Carboxypeptidase II - antagonists & inhibitors Glutamate Carboxypeptidase II - chemistry Humans Kinetics Metallopeptidase Models, Molecular Molecular Conformation Prostate-specific membrane antigen Protein Conformation PSMA Structure-Activity Relationship Structure-based drug design Urea - analogs & derivatives Urea - chemistry Urea - pharmacology Urea-based inhibitor X-ray crystallography
Online-Zugang:	Volltext
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