[Epub ahead of print]
Development of an Activity-Based Probe and In Silico Design Reveal Highly Selective Inhibitors for Diacylglycerol Lipase-α in Brain.
Baggelaar MP, Janssen FJ, van Esbroeck AC, den Dulk H, Allarà M, Hoogendoorn S, McGuire R, Florea BI, Meeuwenoord N, van den Elst H, van der Marel GA, Brouwer J, Di Marzo V, Overkleeft HS, van der Stelt M.
Source
Dept. of Bio-organic Synthesis, Leiden University, Einsteinweg 55, 2333 CC Leiden (The Netherlands).
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.
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
KEYWORDS:
activity-based probe, drug discovery, endocannabinoid, hydrolases, proteomics
- PMID:
- 24173880
- [PubMed – as supplied by publisher]
