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

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

doi:10.1002/anie.201306295

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

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

extern

Research output: Contribution to journal › Article › Academic › peer-review

Original language	English
Pages (from-to)	12081-5
Number of pages	5
Journal	Angewandte Chemie-International Edition
Volume	52
Issue number	46
DOIs	https://doi.org/10.1002/anie.201306295
Publication status	Published - 11 Nov 2013
Externally published	Yes

Keywords

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

Access to Document

10.1002/anie.201306295

Cite this

Baggelaar, M. P., Janssen, F. J., van Esbroeck, A. C. M., den Dulk, H., Allarà, M., Hoogendoorn, S., McGuire, R., Florea, B. I., Meeuwenoord, N., van den Elst, H., van der Marel, G. A., Brouwer, J., Di Marzo, V., Overkleeft, H. S., & van der Stelt, M. (2013). Development of an activity-based probe and in silico design reveal highly selective inhibitors for diacylglycerol lipase-α in brain. Angewandte Chemie-International Edition, 52(46), 12081-5. https://doi.org/10.1002/anie.201306295

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

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

author = "Baggelaar, \{Marc P\} and Janssen, \{Freek J\} and \{van Esbroeck\}, \{Annelot C M\} and \{den Dulk\}, Hans and Marco Allar{\`a} and Sascha Hoogendoorn and Ross McGuire and Florea, \{Bogdan I\} and Nico Meeuwenoord and \{van den Elst\}, Hans and \{van der Marel\}, \{Gijsbert A\} and Jaap Brouwer and \{Di Marzo\}, Vincenzo and Overkleeft, \{Herman S\} and \{van der Stelt\}, Mario",

year = "2013",

month = nov,

day = "11",

doi = "10.1002/anie.201306295",

language = "English",

volume = "52",

pages = "12081--5",

journal = "Angewandte Chemie-International Edition",

issn = "1433-7851",

publisher = "John Wiley and Sons Ltd",

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}

Baggelaar, MP, Janssen, FJ, van Esbroeck, ACM, den Dulk, H, Allarà, 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-α in brain', Angewandte Chemie-International Edition, vol. 52, no. 46, pp. 12081-5. https://doi.org/10.1002/anie.201306295

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 et al.
In: Angewandte Chemie-International Edition, Vol. 52, No. 46, 11.11.2013, p. 12081-5.

Research output: Contribution to journal › Article › Academic › peer-review

TY - JOUR

T1 - Development of an activity-based probe and in silico design reveal highly selective inhibitors for diacylglycerol lipase-α in brain

AU - Baggelaar, Marc P

AU - Janssen, Freek J

AU - van Esbroeck, Annelot C M

AU - den Dulk, Hans

AU - Allarà, Marco

AU - Hoogendoorn, Sascha

AU - McGuire, Ross

AU - Florea, Bogdan I

AU - Meeuwenoord, Nico

AU - van den Elst, Hans

AU - van der Marel, Gijsbert A

AU - Brouwer, Jaap

AU - Di Marzo, Vincenzo

AU - Overkleeft, Herman S

AU - van der Stelt, Mario

PY - 2013/11/11

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KW - Arachidonic Acids/metabolism

KW - Binding Sites

KW - Brain/enzymology

KW - Cell Membrane/metabolism

KW - Endocannabinoids/metabolism

KW - Enzyme Inhibitors/chemistry

KW - Glycerides/metabolism

KW - HEK293 Cells

KW - Humans

KW - Lipoprotein Lipase/antagonists & inhibitors

KW - Mice

KW - Protein Binding

KW - Protein Structure, Tertiary

KW - Proteome

KW - Structure-Activity Relationship

U2 - 10.1002/anie.201306295

DO - 10.1002/anie.201306295

M3 - Article

C2 - 24173880

SN - 1433-7851

VL - 52

SP - 12081

EP - 12085

JO - Angewandte Chemie-International Edition

JF - Angewandte Chemie-International Edition

IS - 46

ER -