Development of an Activity-Based Probe and In Silico Design Reveal Highly Selective Inhibitors for Diacylglycerol Lipase-[alpha] in Brain

Development of an Activity-Based Probe and In Silico Design Reveal Highly Selective Inhibitors for Diacylglycerol Lipase-[alpha] in Brain

A model method: A strategy that combines a knowledge-based insilico design approach and the development of novel activity-based probes (ABPs) for the detection of endogenous diacylglycerol lipase-[alpha] (DAGL-[alpha]) is presented. This approach resulted in the rapid identification of new DAGL-[alp...

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Veröffentlicht in:Angewandte Chemie International Edition 2013-11, Vol.52 (46), p.12081-12085
Hauptverfasser: Baggelaar, Marc P, Janssen, Freek J, vanEsbroeck, Annelot C M, denDulk, Hans, Allara, Marco, Hoogendoorn, Sascha, McGuire, Ross, Florea, Bogdan I, Meeuwenoord, Nico, vandenElst, Hans, vanderMarel, Gijsbert A, Brouwer, Jaap, DiMarzo, Vincenzo, Overkleeft, Herman S, vanderStelt, Mario
Format: Artikel
Sprache:eng
Schlagworte:
Brain
Inhibitors
Knowledge base
Mathematical models
Profiling
Proteins
Selectivity
Strategy
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Zusammenfassung:A model method: A strategy that combines a knowledge-based insilico design approach and the development of novel activity-based probes (ABPs) for the detection of endogenous diacylglycerol lipase-[alpha] (DAGL-[alpha]) is presented. This approach resulted in the rapid identification of new DAGL-[alpha] inhibitors with high selectivity in the brain proteome. ABPP=activity-based protein profiling.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201306295