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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.

SUBMITTER: Choy CJ

PROVIDER: S-EPMC7643579 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature

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A method to determine the mode of binding for GCPII inhibitors using bio-layer interferometry.

Choy Cindy J CJ Berkman Clifford E CE

Journal of enzyme inhibition and medicinal chemistry 20160212 6

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-lay ...[more]

PMID: 26873576

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