title: A method to determine the mode of binding for GCPII inhibitors using bio-layer interferometry.
abstract: The rapid dilution of the enzyme-inhibitor complex assay to monitor the recovery of enzyme activity is a well-established assay to determine the reversibility of inhibition. Our laboratory has previously employed this method to ascertain the reversibility of known glutamate carboxypeptidase II (GCPII)-targeting agents. Due to the tedious and time-consuming nature of the assay, we sought to develop a facile method to determine the reversibility of well-characterized GCPII inhibitors using bio-layer interferometry (BLI). The results from the BLI assay are in agreement with the rapid dilution method. Herein, we report for the first time, a rapid, novel real-time BLI method to determine reversibility of inhibition.
authors.affiliation: a Department of Chemistry , Washington State University , Pullman , WA , USA.
authors.forename: Cindy J
authors.initials: CJ
authors.lastname: Choy
authors.affiliation: a Department of Chemistry , Washington State University , Pullman , WA , USA.
authors.forename: Clifford E
authors.initials: CE
authors.lastname: Berkman
mesh_terms: D000954:Antigens, Surface; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D043425:Glutamate Carboxypeptidase II / Q000037:antagonists & inhibitors*
chemical_list: D000954:Antigens, Surface; D004791:Enzyme Inhibitors; C473848:FOLH1 protein, human; D043425:Glutamate Carboxypeptidase II
keywords: BLI; GCPII; PSMA