| Title : Development of an activity-based probe and in silico design reveal highly selective inhibitors for diacylglycerol lipase-alpha in brain - Baggelaar_2013_Angew.Chem.Int.Ed.Engl_52_12081 |
| Author(s) : Baggelaar MP , Janssen FJ , van Esbroeck AC , den Dulk H , Allara 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 |
| Ref : Angew Chem Int Ed Engl , 52 :12081 , 2013 |
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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-a (DAGL-a) is presented. This approach resulted in the rapid identification of new DAGL-a inhibitors with high selectivity in the brain proteome. ABPP=activity-based protein profiling. |
| PubMedSearch : Baggelaar_2013_Angew.Chem.Int.Ed.Engl_52_12081 |
| PubMedID: 24173880 |
| Gene_locus related to this paper: human-DAGLA |
| Inhibitor | Rhc80267 LEI104 MB064 |
| Gene_locus | human-DAGLA |
Baggelaar MP, Janssen FJ, van Esbroeck AC, den Dulk H, Allara 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 (2013)
Development of an activity-based probe and in silico design reveal highly selective inhibitors for diacylglycerol lipase-alpha in brain
Angew Chem Int Ed Engl
52 :12081
Baggelaar MP, Janssen FJ, van Esbroeck AC, den Dulk H, Allara 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 (2013)
Angew Chem Int Ed Engl
52 :12081