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Items: 1 to 50 of 103

1.

STA-55, An Easily Accessible Broadspectrum Activity-Based Aldehyde Dehydrogenase Probe.

Koenders STA, Van Rooden EJ, Van den Elst H, Florea BI, Overkleeft H, van der Stelt M.

Chembiochem. 2020 Jan 27. doi: 10.1002/cbic.201900771. [Epub ahead of print]

PMID:
31985142
2.

Development of a Retinal-Based Probe for the Profiling of Retinaldehyde Dehydrogenases in Cancer Cells.

Koenders STA, Wijaya LS, Erkelens MN, Bakker AT, van der Noord VE, van Rooden EJ, Burggraaff L, Putter PC, Botter E, Wals K, van den Elst H, den Dulk H, Florea BI, van de Water B, van Westen GJP, Mebius RE, Overkleeft HS, Le Dévédec SE, van der Stelt M.

ACS Cent Sci. 2019 Dec 26;5(12):1965-1974. doi: 10.1021/acscentsci.9b01022. Epub 2019 Dec 12.

3.

Identification of α,β-Hydrolase Domain Containing Protein 6 as a Diacylglycerol Lipase in Neuro-2a Cells.

van Esbroeck ACM, Kantae V, Di X, van der Wel T, den Dulk H, Stevens AF, Singh S, Bakker AT, Florea BI, Stella N, Overkleeft HS, Hankemeier T, van der Stelt M.

Front Mol Neurosci. 2019 Nov 26;12:286. doi: 10.3389/fnmol.2019.00286. eCollection 2019.

4.

Stress-induced modulation of endocannabinoid signaling leads to delayed strengthening of synaptic connectivity in the amygdala.

Yasmin F, Colangeli R, Morena M, Filipski S, van der Stelt M, Pittman QJ, Hillard CJ, Teskey GC, McEwen BS, Hill MN, Chattarji S.

Proc Natl Acad Sci U S A. 2020 Jan 7;117(1):650-655. doi: 10.1073/pnas.1910322116. Epub 2019 Dec 16.

PMID:
31843894
5.

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

van Esbroeck ACM, Varga ZV, Di X, van Rooden EJ, Tóth VE, Onódi Z, Kuśmierczyk M, Leszek P, Ferdinandy P, Hankemeier T, van der Stelt M, Pacher P.

Pharmacol Res. 2020 Jan;151:104578. doi: 10.1016/j.phrs.2019.104578. Epub 2019 Nov 30.

PMID:
31794870
6.

ABHD2 Inhibitor Identified by Activity-Based Protein Profiling Reduces Acrosome Reaction.

Baggelaar MP, den Dulk H, Florea BI, Fazio D, Perruzza D, Bernabò N, Raspa M, Janssen APA, Scavizzi F, Barboni B, Overkleeft HS, Maccarrone M, van der Stelt M.

ACS Chem Biol. 2019 Dec 20;14(12):2943. doi: 10.1021/acschembio.9b00824. Epub 2019 Nov 7. No abstract available.

PMID:
31697462
7.

ABHD2 Inhibitor Identified by Activity-Based Protein Profiling Reduces Acrosome Reaction.

Baggelaar MP, den Dulk H, Florea BI, Fazio D, Bernabò N, Raspa M, Janssen APA, Scavizzi F, Barboni B, Overkleeft HS, Maccarrone M, van der Stelt M.

ACS Chem Biol. 2019 Oct 18;14(10):2295-2304. doi: 10.1021/acschembio.9b00640. Epub 2019 Oct 1. Erratum in: ACS Chem Biol. 2019 Dec 20;14(12):2943.

8.

Structure Kinetics Relationships and Molecular Dynamics Show Crucial Role for Heterocycle Leaving Group in Irreversible Diacylglycerol Lipase Inhibitors.

Janssen APA, van Hengst JMA, Béquignon OJM, Deng H, van Westen GJP, van der Stelt M.

J Med Chem. 2019 Sep 12;62(17):7910-7922. doi: 10.1021/acs.jmedchem.9b00686. Epub 2019 Aug 30.

9.

Endocannabinoid contributions to alcohol habits and motivation: Relevance to treatment.

Gianessi CA, Groman SM, Thompson SL, Jiang M, van der Stelt M, Taylor JR.

Addict Biol. 2019 May 6:e12768. doi: 10.1111/adb.12768. [Epub ahead of print]

PMID:
31056846
10.

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.

11.

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.

12.

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.

13.

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.

14.

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. 2019 Mar 25;59(3):1221-1229. doi: 10.1021/acs.jcim.8b00640. Epub 2018 Nov 8.

15.

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.

16.

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. Review.

PMID:
30242513
17.

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. Erratum in: Blood. 2019 Oct 10;134(15):1271-1272.

PMID:
30213872
18.

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.

19.

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.

20.

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.

21.

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.

22.

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
23.

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.

24.

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
25.

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.

26.

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
27.

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.

28.

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
29.

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.

30.

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
31.

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.

32.

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.

33.

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.

34.

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
35.

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.

36.

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.

37.

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
38.

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.

39.

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.

40.

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
41.

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.

42.

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
43.

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.

44.

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.

45.

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
46.

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
47.

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
48.

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
49.

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
50.

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

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