Literature DB >> 24173880

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

Marc P Baggelaar1, 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.   

Abstract

Entities:  

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

Mesh：

Substances：

Year:  2013        PMID： 24173880     DOI： 10.1002/anie.201306295

Source DB:  PubMed          Journal:  Angew Chem Int Ed Engl        ISSN： 1433-7851            Impact factor:   15.336


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  33 in total

1.  Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474.

Authors:  Annelot C M van Esbroeck; Antonius P A Janssen; Armand B Cognetta; Daisuke Ogasawara; Guy Shpak; Mark van der Kroeg; Vasudev Kantae; Marc P Baggelaar; Femke M S de Vrij; Hui Deng; Marco Allarà; Filomena Fezza; Zhanmin Lin; Tom van der Wel; Marjolein Soethoudt; Elliot D Mock; Hans den Dulk; Ilse L Baak; Bogdan I Florea; Giel Hendriks; Luciano De Petrocellis; Herman S Overkleeft; Thomas Hankemeier; Chris I De Zeeuw; Vincenzo Di Marzo; Mauro Maccarrone; Benjamin F Cravatt; Steven A Kushner; Mario van der Stelt
Journal:  Science       Date:  2017-06-09       Impact factor: 47.728

2.  Diacylglycerol lipase disinhibits VTA dopamine neurons during chronic nicotine exposure.

Authors:  Matthew W Buczynski; Melissa A Herman; Ku-Lung Hsu; Luis A Natividad; Cristina Irimia; Ilham Y Polis; Holly Pugh; Jae Won Chang; Micah J Niphakis; Benjamin F Cravatt; Marisa Roberto; Loren H Parsons
Journal:  Proc Natl Acad Sci U S A       Date:  2016-01-11       Impact factor: 11.205

3.  The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity.

Authors:  Partha Mukhopadhyay; Marc Baggelaar; Katalin Erdelyi; Zongxian Cao; Resat Cinar; Filomena Fezza; Bogna Ignatowska-Janlowska; Jenny Wilkerson; Noortje van Gils; Thomas Hansen; Marc Ruben; Marjolein Soethoudt; Laura Heitman; George Kunos; Mauro Maccarrone; Aron Lichtman; Pál Pacher; Mario Van der Stelt
Journal:  Br J Pharmacol       Date:  2016-01-15       Impact factor: 8.739

4.  A natural substrate-based fluorescence assay for inhibitor screening on diacylglycerol lipase α.

Authors:  Tom van der Wel; Freek J Janssen; Marc P Baggelaar; Hui Deng; Hans den Dulk; Herman S Overkleeft; Mario van der Stelt
Journal:  J Lipid Res       Date:  2015-02-15       Impact factor: 5.922

5.  Inhibiting endocannabinoid biosynthesis: a novel approach to the treatment of constipation.

Authors:  M Bashashati; Y Nasser; C M Keenan; W Ho; F Piscitelli; M Nalli; K Mackie; M A Storr; V Di Marzo; K A Sharkey
Journal:  Br J Pharmacol       Date:  2015-04-23       Impact factor: 8.739

6.  Mapping in vivo target interaction profiles of covalent inhibitors using chemical proteomics with label-free quantification.

Authors:  Eva J van Rooden; Bogdan I Florea; Hui Deng; Marc P Baggelaar; Annelot C M van Esbroeck; Juan Zhou; Herman S Overkleeft; Mario van der Stelt
Journal:  Nat Protoc       Date:  2018-03-22       Impact factor: 13.491

Review 7.  Strategies for Tuning the Selectivity of Chemical Probes that Target Serine Hydrolases.

Authors:  Franco Faucher; John M Bennett; Matthew Bogyo; Scott Lovell
Journal:  Cell Chem Biol       Date:  2020-07-28       Impact factor: 8.116

Review 8.  Lipid-metabolizing serine hydrolases in the mammalian central nervous system: endocannabinoids and beyond.

Authors:  Myungsun Shin; Timothy B Ware; Hyeon-Cheol Lee; Ku-Lung Hsu
Journal:  Biochim Biophys Acta Mol Cell Biol Lipids       Date:  2018-08-16       Impact factor: 4.698

9.  Liposomal Delivery of Diacylglycerol Lipase-Beta Inhibitors to Macrophages Dramatically Enhances Selectivity and Efficacy in Vivo.

Authors:  Myungsun Shin; Helena W Snyder; Giulia Donvito; Lesley D Schurman; Todd E Fox; Aron H Lichtman; Mark Kester; Ku-Lung Hsu
Journal:  Mol Pharm       Date:  2017-09-13       Impact factor: 4.939

10.  Activity-based protein profiling of the human failing ischemic heart reveals alterations in hydrolase activities involving the endocannabinoid system.

Authors:  Annelot C M van Esbroeck; Zoltan V Varga; Xinyu Di; Eva J van Rooden; Viktória E Tóth; Zsófia Onódi; Mariusz Kuśmierczyk; Przemyslaw Leszek; Péter Ferdinandy; Thomas Hankemeier; Mario van der Stelt; Pál Pacher
Journal:  Pharmacol Res       Date:  2019-11-30       Impact factor: 7.658
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