Ontology highlight
ABSTRACT:
SUBMITTER: Pavlicek J
PROVIDER: S-EPMC4077459 | biostudies-literature | 2014 May
REPOSITORIES: biostudies-literature
Pavlicek Jiri J Ptacek Jakub J Cerny Jiri J Byun Youngjoo Y Skultetyova Lubica L Pomper Martin G MG Lubkowski Jacek J Barinka Cyril C
Bioorganic & medicinal chemistry letters 20140328 10
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 the structural and computational characterization of six complexes between GCPII and P1'-diversified urea-based inhibitors that have the C-terminal glutamate replaced by more hydrophobic moieties. The ...[more]