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Angewandte Chemie - International Edition

Volumn 52, Issue 46, 2013, Pages 12081-12085

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

(15) Baggelaar, Marc P a Janssen, Freek J a Vanesbroeck, Annelot C M a Dendulk, Hans a Allarà, Marco b Hoogendoorn, Sascha a McGuire, Ross c Florea, Bogdan I a Meeuwenoord, Nico a Vandenelst, Hans a Vandermarel, Gijsbert A a Brouwer, Jaap a Dimarzo, Vincenzo b Overkleeft, Herman S a Vanderstelt, Mario a

a LEIDEN UNIVERSITY (Netherlands)

b CNR (Italy)

c BioAxis Research (Netherlands)

Author keywords

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

Indexed keywords

ACTIVITY-BASED PROBE; ACTIVITY-BASED PROTEIN PROFILING; DESIGN APPROACHES; DRUG DISCOVERY; ENDOCANNABINOID; PROTEOMICS; RAPID IDENTIFICATION; SELECTIVE INHIBITORS;

HYDROLASES; KNOWLEDGE BASED SYSTEMS; MOLECULAR BIOLOGY; PROBES;

BRAIN;

2-ARACHIDONYLGLYCEROL; ACYLGLYCEROL; ARACHIDONIC ACID DERIVATIVE; ENDOCANNABINOID; ENZYME INHIBITOR; LIPOPROTEIN LIPASE; PROTEIN BINDING; PROTEOME;

ANIMAL; ANTAGONISTS AND INHIBITORS; BINDING SITE; BRAIN; CELL MEMBRANE; CHEMISTRY; ENZYMOLOGY; GENETICS; HEK293 CELL LINE; HUMAN; METABOLISM; MOUSE; PROTEIN TERTIARY STRUCTURE; STRUCTURE ACTIVITY RELATION;

ANIMALS; ARACHIDONIC ACIDS; BINDING SITES; BRAIN; CELL MEMBRANE; ENDOCANNABINOIDS; ENZYME INHIBITORS; GLYCERIDES; HEK293 CELLS; HUMANS; LIPOPROTEIN LIPASE; MICE; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; PROTEOME; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84887498917 PISSN: 14337851 EISSN: 15213773 Source Type: Journal
DOI: 10.1002/anie.201306295 Document Type: Article

Times cited : (63)

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