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 |
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| container_title | Angewandte Chemie International Edition |
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| creator | 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 |
| description | 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. |
| doi_str_mv | 10.1002/anie.201306295 |
| format | Article |
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| language | eng |
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| source | Wiley Online Library Journals Frontfile Complete |
| subjects | Brain Inhibitors Knowledge base Mathematical models Profiling Proteins Selectivity Strategy |
| title | Development of an Activity-Based Probe and In Silico Design Reveal Highly Selective Inhibitors for Diacylglycerol Lipase-[alpha] in Brain |
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