Development of an Activity‐Based Probe and In Silico Design Reveal Highly Selective Inhibitors for Diacylglycerol Lipase‐α in Brain

Abstract

A model method: A strategy that combines a knowledge-based in silico design approach and the development of novel activity-based probes (ABPs) for the detection of endogenous diacylglycerol lipase-α (DAGL-α) is presented. This approach resulted in the rapid identification of new DAGL-α inhibitors with high selectivity in the brain proteome. ABPP=activity-based protein profiling.