title: Development of an activity-based probe and in silico design reveal highly selective inhibitors for diacylglycerol lipase-α in brain.
authors.affiliation: Dept. of Bio-organic Synthesis, Leiden University, Einsteinweg 55, 2333 CC Leiden (The Netherlands).
authors.forename: Marc P
authors.initials: MP
authors.lastname: Baggelaar
authors.forename: Freek J
authors.initials: FJ
authors.lastname: Janssen
authors.forename: Annelot C M
authors.initials: AC
authors.lastname: van Esbroeck
authors.forename: Hans
authors.initials: H
authors.lastname: den Dulk
authors.forename: Marco
authors.initials: M
authors.lastname: Allarà
authors.forename: Sascha
authors.initials: S
authors.lastname: Hoogendoorn
authors.forename: Ross
authors.initials: R
authors.lastname: McGuire
authors.forename: Bogdan I
authors.initials: BI
authors.lastname: Florea
authors.forename: Nico
authors.initials: N
authors.lastname: Meeuwenoord
authors.forename: Hans
authors.initials: H
authors.lastname: van den Elst
authors.forename: Gijsbert A
authors.initials: GA
authors.lastname: van der Marel
authors.forename: Jaap
authors.initials: J
authors.lastname: Brouwer
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Di Marzo
authors.forename: Herman S
authors.initials: HS
authors.lastname: Overkleeft
authors.forename: Mario
authors.initials: M
authors.lastname: van der Stelt
mesh_terms: D000818:Animals; D001095:Arachidonic Acids / Q000378:metabolism; D001665:Binding Sites; D001921:Brain / Q000201:enzymology* / Q000378:metabolism; D002462:Cell Membrane / Q000378:metabolism; D063388:Endocannabinoids / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism; D005989:Glycerides / Q000378:metabolism; D057809:HEK293 Cells; D006801:Humans; D008071:Lipoprotein Lipase / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism*; D051379:Mice; D011485:Protein Binding; D017434:Protein Structure, Tertiary; D020543:Proteome; D013329:Structure-Activity Relationship
chemical_list: D001095:Arachidonic Acids; D063388:Endocannabinoids; D004791:Enzyme Inhibitors; D005989:Glycerides; D020543:Proteome; C094503:glyceryl 2-arachidonate; D008071:Lipoprotein Lipase
keywords: activity-based probe; drug discovery; endocannabinoid; hydrolases; proteomics