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Items: 1 to 50 of 94

1.

High Fat Diet Increases Circulating Endocannabinoids Accompanied by Increased Synthesis Enzymes in Adipose Tissue.

Kuipers EN, Kantae V, Maarse BCE, van den Berg SM, van Eenige R, Nahon KJ, Reifel-Miller A, Coskun T, de Winther MPJ, Lutgens E, Kooijman S, Harms AC, Hankemeier T, van der Stelt M, Rensen PCN, Boon MR.

Front Physiol. 2019 Jan 10;9:1913. doi: 10.3389/fphys.2018.01913. eCollection 2018.

2.

Comprehensive structure-activity-relationship of azaindoles as highly potent FLT3 inhibitors.

Grimm SH, Gagestein B, Keijzer JF, Liu N, Wijdeven RH, Lenselink EB, Tuin AW, van den Nieuwendijk AMCH, van Westen GJP, van Boeckel CAA, Overkleeft HS, Neefjes J, van der Stelt M.

Bioorg Med Chem. 2019 Mar 1;27(5):692-699. doi: 10.1016/j.bmc.2019.01.006. Epub 2019 Jan 14.

3.

Activity-Based Protein Profiling Identifies α-Ketoamides as Inhibitors for Phospholipase A2 Group XVI.

Zhou J, Mock ED, Martella A, Kantae V, Di X, Burggraaff L, Baggelaar MP, Al-Ayed K, Bakker A, Florea BI, Grimm SH, den Dulk H, Li CT, Mulder L, Overkleeft HS, Hankemeier T, van Westen GJP, van der Stelt M.

ACS Chem Biol. 2019 Feb 15;14(2):164-169. doi: 10.1021/acschembio.8b00969. Epub 2019 Jan 18.

4.

Anti-neuroinflammatory effects of GPR55 antagonists in LPS-activated primary microglial cells.

Saliba SW, Jauch H, Gargouri B, Keil A, Hurrle T, Volz N, Mohr F, van der Stelt M, Bräse S, Fiebich BL.

J Neuroinflammation. 2018 Nov 19;15(1):322. doi: 10.1186/s12974-018-1362-7.

5.

Drug Discovery Maps, a Machine Learning Model That Visualizes and Predicts Kinome-Inhibitor Interaction Landscapes.

Janssen APA, Grimm SH, Wijdeven RHM, Lenselink EB, Neefjes J, van Boeckel CAA, van Westen GJP, van der Stelt M.

J Chem Inf Model. 2018 Nov 8. doi: 10.1021/acs.jcim.8b00640. [Epub ahead of print]

PMID:
30372617
6.

Activity-Based Protein Profiling Delivers Selective Drug Candidate ABX-1431, a Monoacylglycerol Lipase Inhibitor, To Control Lipid Metabolism in Neurological Disorders.

Jiang M, van der Stelt M.

J Med Chem. 2018 Oct 25;61(20):9059-9061. doi: 10.1021/acs.jmedchem.8b01405. Epub 2018 Oct 11.

7.

Opportunities for Lipid-Based Probes in the Field of Immunology.

Koenders STA, Gagestein B, van der Stelt M.

Curr Top Microbiol Immunol. 2019;420:283-319. doi: 10.1007/82_2018_127.

PMID:
30242513
8.

Improving CLL Vγ9Vδ2-T-cell fitness for cellular therapy by ex vivo activation and ibrutinib.

de Weerdt I, Hofland T, Lameris R, Endstra S, Jongejan A, Moerland PD, de Bruin RCG, Remmerswaal EBM, Ten Berge IJM, Liu N, van der Stelt M, Faber LM, Levin MD, Eldering E, Tonino SH, de Gruijl TD, van der Vliet HJ, Kater AP.

Blood. 2018 Nov 22;132(21):2260-2272. doi: 10.1182/blood-2017-12-822569. Epub 2018 Sep 13.

PMID:
30213872
9.

Development of a Multiplexed Activity-Based Protein Profiling Assay to Evaluate Activity of Endocannabinoid Hydrolase Inhibitors.

Janssen APA, van der Vliet D, Bakker AT, Jiang M, Grimm SH, Campiani G, Butini S, van der Stelt M.

ACS Chem Biol. 2018 Sep 21;13(9):2406-2413. doi: 10.1021/acschembio.8b00534. Epub 2018 Sep 12.

10.

An Affinity-Based Probe for the Human Adenosine A2A Receptor.

Yang X, Michiels TJM, de Jong C, Soethoudt M, Dekker N, Gordon E, van der Stelt M, Heitman LH, van der Es D, IJzerman AP.

J Med Chem. 2018 Sep 13;61(17):7892-7901. doi: 10.1021/acs.jmedchem.8b00860. Epub 2018 Aug 21.

11.

Gene Expression of Endocannabinoid System Components in Skeletal Muscle and Adipose Tissue of South Asians and White Caucasians with Overweight.

Nahon KJ, Kantae V, den Haan R, Hanssen MJW, Harms AC, van der Stelt M, Hankemeier T, Jazet IM, van Marken Lichtenbelt WD, Rensen PCN, Boon MR.

Obesity (Silver Spring). 2018 Aug;26(8):1332-1337. doi: 10.1002/oby.22245. Epub 2018 Aug 1.

PMID:
30070030
12.

Chemical Proteomic Analysis of Serine Hydrolase Activity in Niemann-Pick Type C Mouse Brain.

van Rooden EJ, van Esbroeck ACM, Baggelaar MP, Deng H, Florea BI, Marques ARA, Ottenhoff R, Boot RG, Overkleeft HS, Aerts JMFG, van der Stelt M.

Front Neurosci. 2018 Jul 3;12:440. doi: 10.3389/fnins.2018.00440. eCollection 2018.

13.

Two-step activity-based protein profiling of diacylglycerol lipase.

van Rooden EJ, Kreekel R, Hansen T, Janssen APA, van Esbroeck ACM, den Dulk H, van den Berg RJBHN, Codée JDC, van der Stelt M.

Org Biomol Chem. 2018 Jul 25;16(29):5250-5253. doi: 10.1039/c8ob01499j.

PMID:
30004552
14.

Development of a Cannabinoid-Based Photoaffinity Probe to Determine the Δ8/9-Tetrahydrocannabinol Protein Interaction Landscape in Neuroblastoma Cells.

Soethoudt M, Alachouzos G, van Rooden EJ, Moya-Garzón MD, van den Berg RJBHN, Heitman LH, van der Stelt M.

Cannabis Cannabinoid Res. 2018 Jul 1;3(1):136-151. doi: 10.1089/can.2018.0003. eCollection 2018.

15.

Design and Synthesis of Quenched Activity-based Probes for Diacylglycerol Lipase and α,β-Hydrolase Domain Containing Protein 6.

van Rooden EJ, Kohsiek M, Kreekel R, van Esbroeck ACM, van den Nieuwendijk AMCH, Janssen APA, van den Berg RJBHN, Overkleeft HS, van der Stelt M.

Chem Asian J. 2018 Nov 16;13(22):3491-3500. doi: 10.1002/asia.201800452. Epub 2018 Jun 14.

PMID:
29901868
16.

2-Arachidonoylglycerol: A signaling lipid with manifold actions in the brain.

Baggelaar MP, Maccarrone M, van der Stelt M.

Prog Lipid Res. 2018 Jul;71:1-17. doi: 10.1016/j.plipres.2018.05.002. Epub 2018 May 8. Review.

17.

Regulation of Adipose Tissue Metabolism by the Endocannabinoid System.

van Eenige R, van der Stelt M, Rensen PCN, Kooijman S.

Trends Endocrinol Metab. 2018 May;29(5):326-337. doi: 10.1016/j.tem.2018.03.001. Epub 2018 Mar 24. Review.

PMID:
29588112
18.

Structure-kinetic relationship studies of cannabinoid CB2 receptor agonists reveal substituent-specific lipophilic effects on residence time.

Soethoudt M, Hoorens MWH, Doelman W, Martella A, van der Stelt M, Heitman LH.

Biochem Pharmacol. 2018 Jun;152:129-142. doi: 10.1016/j.bcp.2018.03.018. Epub 2018 Mar 21.

19.

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

van Rooden EJ, Florea BI, Deng H, Baggelaar MP, van Esbroeck ACM, Zhou J, Overkleeft HS, van der Stelt M.

Nat Protoc. 2018 Apr;13(4):752-767. doi: 10.1038/nprot.2017.159. Epub 2018 Mar 22.

PMID:
29565900
20.

Evaluation of different drug classes on transient sciatic nerve injury-depressed marble burying in mice.

Wilkerson JL, Curry ZA, Kinlow PD, Mason BL, Hsu KL, van der Stelt M, Cravatt BF, Lichtman AH.

Pain. 2018 Jun;159(6):1155-1165. doi: 10.1097/j.pain.0000000000001199.

PMID:
29528965
21.

Localization of the cannabinoid type-1 receptor in subcellular astrocyte compartments of mutant mouse hippocampus.

Gutiérrez-Rodríguez A, Bonilla-Del Río I, Puente N, Gómez-Urquijo SM, Fontaine CJ, Egaña-Huguet J, Elezgarai I, Ruehle S, Lutz B, Robin LM, Soria-Gómez E, Bellocchio L, Padwal JD, van der Stelt M, Mendizabal-Zubiaga J, Reguero L, Ramos A, Gerrikagoitia I, Marsicano G, Grandes P.

Glia. 2018 Jul;66(7):1417-1431. doi: 10.1002/glia.23314. Epub 2018 Feb 26.

PMID:
29480581
22.

Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells.

Soethoudt M, Stolze SC, Westphal MV, van Stralen L, Martella A, van Rooden EJ, Guba W, Varga ZV, Deng H, van Kasteren SI, Grether U, IJzerman AP, Pacher P, Carreira EM, Overkleeft HS, Ioan-Facsinay A, Heitman LH, van der Stelt M.

J Am Chem Soc. 2018 May 16;140(19):6067-6075. doi: 10.1021/jacs.7b11281. Epub 2018 Feb 16.

23.

Caloric restriction lowers endocannabinoid tonus and improves cardiac function in type 2 diabetes.

van Eyk HJ, van Schinkel LD, Kantae V, Dronkers CEA, Westenberg JJM, de Roos A, Lamb HJ, Jukema JW, Harms AC, Hankemeier T, van der Stelt M, Jazet IM, Rensen PCN, Smit JWA.

Nutr Diabetes. 2018 Jan 17;8(1):6. doi: 10.1038/s41387-017-0016-7.

24.

The endocannabinoid system and its therapeutic exploitation in multiple sclerosis: Clues for other neuroinflammatory diseases.

Chiurchiù V, van der Stelt M, Centonze D, Maccarrone M.

Prog Neurobiol. 2018 Jan;160:82-100. doi: 10.1016/j.pneurobio.2017.10.007. Epub 2017 Oct 31. Review.

25.

Novel activity-based probes for N-acylethanolamine acid amidase.

Petracca R, Romeo E, Baggelaar MP, Artola M, Pontis S, Ponzano S, Overkleeft HS, van der Stelt M, Piomelli D.

Chem Commun (Camb). 2017 Aug 22;53(86):11810-11813. doi: 10.1039/c7cc06838g.

PMID:
29035406
26.

A Fluorescence Polarization Activity-Based Protein Profiling Assay in the Discovery of Potent, Selective Inhibitors for Human Nonlysosomal Glucosylceramidase.

Lahav D, Liu B, van den Berg RJBHN, van den Nieuwendijk AMCH, Wennekes T, Ghisaidoobe AT, Breen I, Ferraz MJ, Kuo CL, Wu L, Geurink PP, Ovaa H, van der Marel GA, van der Stelt M, Boot RG, Davies GJ, Aerts JMFG, Overkleeft HS.

J Am Chem Soc. 2017 Oct 11;139(40):14192-14197. doi: 10.1021/jacs.7b07352. Epub 2017 Sep 29.

27.

Endocannabinoid tone is higher in healthy lean South Asian than white Caucasian men.

Kantae V, Nahon KJ, Straat ME, Bakker LEH, Harms AC, van der Stelt M, Hankemeier T, Jazet IM, Boon MR, Rensen PCN.

Sci Rep. 2017 Aug 8;7(1):7558. doi: 10.1038/s41598-017-07980-5.

28.

A Novel Selective Inverse Agonist of the CB2 Receptor as a Radiolabeled Tool Compound for Kinetic Binding Studies.

Martella A, Sijben H, Rufer AC, Grether U, Fingerle J, Ullmer C, Hartung T, IJzerman AP, van der Stelt M, Heitman LH.

Mol Pharmacol. 2017 Oct;92(4):389-400. doi: 10.1124/mol.117.108605. Epub 2017 Jul 26.

PMID:
28747489
29.

Piperidine and octahydropyrano[3,4-c] pyridine scaffolds for drug-like molecular libraries of the European Lead Factory.

Narhe BD, Breman AC, Padwal J, Vandenput DAL, Scheidt JM, Benningshof JCJ, van der Marel GA, Overkleeft HS, van der Stelt M, Filippov DV.

Bioorg Med Chem. 2017 Oct 1;25(19):5160-5170. doi: 10.1016/j.bmc.2017.07.016. Epub 2017 Jul 10.

30.

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

van Esbroeck ACM, Janssen APA, Cognetta AB 3rd, Ogasawara D, Shpak G, van der Kroeg M, Kantae V, Baggelaar MP, de Vrij FMS, Deng H, Allarà M, Fezza F, Lin Z, van der Wel T, Soethoudt M, Mock ED, den Dulk H, Baak IL, Florea BI, Hendriks G, De Petrocellis L, Overkleeft HS, Hankemeier T, De Zeeuw CI, Di Marzo V, Maccarrone M, Cravatt BF, Kushner SA, van der Stelt M.

Science. 2017 Jun 9;356(6342):1084-1087. doi: 10.1126/science.aaf7497.

31.

Chemical tools to modulate 2-arachidonoylglycerol biosynthesis.

Deng H, van der Stelt M.

Biotechnol Appl Biochem. 2018 Jan;65(1):9-15. doi: 10.1002/bab.1568. Epub 2017 Aug 2. Review.

PMID:
28589628
32.

Chiral disubstituted piperidinyl ureas: a class of dual diacylglycerol lipase-α and ABHD6 inhibitors.

Deng H, van der Wel T, van den Berg RJBHN, van den Nieuwendijk AMCH, Janssen FJ, Baggelaar MP, Overkleeft HS, van der Stelt M.

Medchemcomm. 2017 Mar 10;8(5):982-988. doi: 10.1039/c7md00029d. eCollection 2017 May 1.

33.

Chemical Proteomics Maps Brain Region Specific Activity of Endocannabinoid Hydrolases.

Baggelaar MP, van Esbroeck AC, van Rooden EJ, Florea BI, Overkleeft HS, Marsicano G, Chaouloff F, van der Stelt M.

ACS Chem Biol. 2017 Mar 17;12(3):852-861. doi: 10.1021/acschembio.6b01052. Epub 2017 Feb 13.

PMID:
28106377
34.

Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity.

Soethoudt M, Grether U, Fingerle J, Grim TW, Fezza F, de Petrocellis L, Ullmer C, Rothenhäusler B, Perret C, van Gils N, Finlay D, MacDonald C, Chicca A, Gens MD, Stuart J, de Vries H, Mastrangelo N, Xia L, Alachouzos G, Baggelaar MP, Martella A, Mock ED, Deng H, Heitman LH, Connor M, Di Marzo V, Gertsch J, Lichtman AH, Maccarrone M, Pacher P, Glass M, van der Stelt M.

Nat Commun. 2017 Jan 3;8:13958. doi: 10.1038/ncomms13958.

35.

Quantitative profiling of endocannabinoids and related N-acylethanolamines in human CSF using nano LC-MS/MS.

Kantae V, Ogino S, Noga M, Harms AC, van Dongen RM, Onderwater GL, van den Maagdenberg AM, Terwindt GM, van der Stelt M, Ferrari MD, Hankemeier T.

J Lipid Res. 2017 Mar;58(3):615-624. doi: 10.1194/jlr.D070433. Epub 2016 Dec 20.

36.

Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding.

Deng H, Kooijman S, van den Nieuwendijk AM, Ogasawara D, van der Wel T, van Dalen F, Baggelaar MP, Janssen FJ, van den Berg RJ, den Dulk H, Cravatt BF, Overkleeft HS, Rensen PC, van der Stelt M.

J Med Chem. 2017 Jan 12;60(1):428-440. doi: 10.1021/acs.jmedchem.6b01482. Epub 2016 Dec 19.

PMID:
27992221
37.

Competitive ABPP of Serine Hydrolases: A Case Study on DAGL-Alpha.

Baggelaar MP, Van der Stelt M.

Methods Mol Biol. 2017;1491:161-169.

PMID:
27778288
38.

Structure-Based Design of β5c Selective Inhibitors of Human Constitutive Proteasomes.

Xin BT, de Bruin G, Huber EM, Besse A, Florea BI, Filippov DV, van der Marel GA, Kisselev AF, van der Stelt M, Driessen C, Groll M, Overkleeft HS.

J Med Chem. 2016 Aug 11;59(15):7177-87. doi: 10.1021/acs.jmedchem.6b00705. Epub 2016 Aug 1.

PMID:
27438186
39.

Inhibitors of diacylglycerol lipases in neurodegenerative and metabolic disorders.

Janssen FJ, van der Stelt M.

Bioorg Med Chem Lett. 2016 Aug 15;26(16):3831-7. doi: 10.1016/j.bmcl.2016.06.076. Epub 2016 Jun 27. Review.

PMID:
27394666
40.

Oxygenation of Anandamide by Lipoxygenases.

van Zadelhoff G, van der Stelt M.

Methods Mol Biol. 2016;1412:217-25. doi: 10.1007/978-1-4939-3539-0_22.

PMID:
27245907
41.

Protocol to Study β-Arrestin Recruitment by CB1 and CB2 Cannabinoid Receptors.

Soethoudt M, van Gils N, van der Stelt M, Heitman LH.

Methods Mol Biol. 2016;1412:103-11. doi: 10.1007/978-1-4939-3539-0_11.

PMID:
27245896
42.

Photo-crosslinking of clinically relevant kinases using H89-derived photo-affinity probes.

Stolze SC, Liu N, Wijdeven RH, Tuin AW, van den Nieuwendijk AM, Florea BI, van der Stelt M, van der Marel GA, Neefjes JJ, Overkleeft HS.

Mol Biosyst. 2016 May 24;12(6):1809-17. doi: 10.1039/c6mb00257a.

PMID:
27138522
43.

Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition.

Ogasawara D, Deng H, Viader A, Baggelaar MP, Breman A, den Dulk H, van den Nieuwendijk AM, Soethoudt M, van der Wel T, Zhou J, Overkleeft HS, Sanchez-Alavez M, Mori S, Nguyen W, Conti B, Liu X, Chen Y, Liu QS, Cravatt BF, van der Stelt M.

Proc Natl Acad Sci U S A. 2016 Jan 5;113(1):26-33. doi: 10.1073/pnas.1522364112. Epub 2015 Dec 14. Erratum in: Proc Natl Acad Sci U S A. 2016 Feb 2;113(5):E664. van den Nieuwendijk, Adriann M C H [corrected to van den Nieuwendijk, Adrianus M C H]; Mo, Simone [corrected to Mori, Simone].

44.

Identification of an allosteric binding site for RORγt inhibition.

Scheepstra M, Leysen S, van Almen GC, Miller JR, Piesvaux J, Kutilek V, van Eenennaam H, Zhang H, Barr K, Nagpal S, Soisson SM, Kornienko M, Wiley K, Elsen N, Sharma S, Correll CC, Trotter BW, van der Stelt M, Oubrie A, Ottmann C, Parthasarathy G, Brunsveld L.

Nat Commun. 2015 Dec 7;6:8833. doi: 10.1038/ncomms9833.

45.

Comprehensive Analysis of Structure-Activity Relationships of α-Ketoheterocycles as sn-1-Diacylglycerol Lipase α Inhibitors.

Janssen FJ, Baggelaar MP, Hummel JJ, Overkleeft HS, Cravatt BF, Boger DL, van der Stelt M.

J Med Chem. 2015 Dec 24;58(24):9742-53. doi: 10.1021/acs.jmedchem.5b01627. Epub 2015 Dec 2.

46.

A Set of Activity-Based Probes to Visualize Human (Immuno)proteasome Activities.

de Bruin G, Xin BT, Kraus M, van der Stelt M, van der Marel GA, Kisselev AF, Driessen C, Florea BI, Overkleeft HS.

Angew Chem Int Ed Engl. 2016 Mar 18;55(13):4199-203. doi: 10.1002/anie.201509092. Epub 2015 Oct 29.

PMID:
26511210
47.

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

Mukhopadhyay P, Baggelaar M, Erdelyi K, Cao Z, Cinar R, Fezza F, Ignatowska-Janlowska B, Wilkerson J, van Gils N, Hansen T, Ruben M, Soethoudt M, Heitman L, Kunos G, Maccarrone M, Lichtman A, Pacher P, Van der Stelt M.

Br J Pharmacol. 2016 Feb;173(3):446-58. doi: 10.1111/bph.13338. Epub 2016 Jan 15.

48.

Highly Selective, Reversible Inhibitor Identified by Comparative Chemoproteomics Modulates Diacylglycerol Lipase Activity in Neurons.

Baggelaar MP, Chameau PJ, Kantae V, Hummel J, Hsu KL, Janssen F, van der Wel T, Soethoudt M, Deng H, den Dulk H, Allarà M, Florea BI, Di Marzo V, Wadman WJ, Kruse CG, Overkleeft HS, Hankemeier T, Werkman TR, Cravatt BF, van der Stelt M.

J Am Chem Soc. 2015 Jul 15;137(27):8851-7. doi: 10.1021/jacs.5b04883. Epub 2015 Jul 1.

49.

Direct and two-step bioorthogonal probes for Bruton's tyrosine kinase based on ibrutinib: a comparative study.

Liu N, Hoogendoorn S, van de Kar B, Kaptein A, Barf T, Driessen C, Filippov DV, van der Marel GA, van der Stelt M, Overkleeft HS.

Org Biomol Chem. 2015 May 14;13(18):5147-57. doi: 10.1039/c5ob00474h.

PMID:
25849561
50.

Development of an acid ceramidase activity-based probe.

Ouairy CM, Ferraz MJ, Boot RG, Baggelaar MP, van der Stelt M, Appelman M, van der Marel GA, Florea BI, Aerts JM, Overkleeft HS.

Chem Commun (Camb). 2015 Apr 11;51(28):6161-3. doi: 10.1039/c5cc00356c.

PMID:
25748248

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