Development of an activity-based probe and in silico design reveal highly selective inhibitors for diacylglycerol lipase-&#945; in brain.

Baggelaar, Marc P; Janssen, Freek J; van Esbroeck, Annelot C M; den Dulk, Hans; Allarà, Marco; Hoogendoorn, Sascha; McGuire, Ross; Florea, Bogdan I; Meeuwenoord, Nico; van den Elst, Hans; van der Marel, Gijsbert A; Brouwer, Jaap; Di Marzo, Vincenzo; Overkleeft, Herman S; van der Stelt, Mario

Development of an activity-based probe and in silico design reveal highly selective inhibitors for diacylglycerol lipase-α in brain.

Baggelaar, Marc P; Janssen, Freek J; van Esbroeck, Annelot C M; den Dulk, Hans; Allarà, Marco; Hoogendoorn, Sascha; McGuire, Ross; Florea, Bogdan I; Meeuwenoord, Nico; van den Elst, Hans; van der Marel, Gijsbert A; Brouwer, Jaap; Di Marzo, Vincenzo; Overkleeft, Herman S; van der Stelt, Mario.

Affiliation

Baggelaar MP; Dept. of Bio-organic Synthesis, Leiden University, Einsteinweg 55, 2333 CC Leiden (The Netherlands).

Angew Chem Int Ed Engl ; 52(46): 12081-5, 2013 Nov 11.

Article in En | MEDLINE | ID: mdl-24173880

Subject(s)

Brain/enzymology; Enzyme Inhibitors/chemistry; Lipoprotein Lipase/metabolism; Animals; Arachidonic Acids/metabolism; Binding Sites; Brain/metabolism; Cell Membrane/metabolism; Endocannabinoids/metabolism; Enzyme Inhibitors/metabolism; Glycerides/metabolism; HEK293 Cells; Humans; Lipoprotein Lipase/antagonists & inhibitors; Lipoprotein Lipase/genetics; Mice; Protein Binding; Protein Structure, Tertiary; Proteome; Structure-Activity Relationship

Key words

activity-based probe; drug discovery; endocannabinoid; hydrolases; proteomics

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Brain / Enzyme Inhibitors / Lipoprotein Lipase Limits: Animals / Humans Language: En Journal: Angew Chem Int Ed Engl Year: 2013 Type: Article

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