Mario van der Stelt (1975) is professor and chair of the department of Molecular Physiology of the Leiden University (the Netherlands). He is a medicinal chemist and worked as a project leader for almost 8 years in the pharmaceutical industry (Merck Research Laboratories). He and his group discovered highly selective and peripherally restricted cannabinoid CB2 receptor agonists and the first brain active inhibitors for the biosynthesis of endocannabinoids. His group reported the off-target profile of the FAAH inhibitor BIA 10-2474 that killed a healthy volunteer in a phase 1 clinical trial in France in 2016. Dr. Van der Stelt received for his research the Prix Galien Research for best preclinical drug discovery research in the Netherlands (2017), the Young Investigator Award of the International Cannabinoid Research Society (2017) and a VICI-award from the Netherlands Organisation for Scientific Research (2018). He is elected as a senior investigator of Oncode Institute (2019) and (vice)-chair of the Gordon Research Conference on Cannabinoid Function in the CNS (2021-2023). Multidisciplinary collaboration is key in his research to connect chemistry and biology to discover drug candidates modulating the endocannabinoid system.

• 2000 Coy W. Waller Award, ICRS meeting, Baltimore, USA

• 2001 Coy W. Waller Award, ICRS meeting Madrid, Spain

• 2001 Bijvoet PhD-competition Award, Utrecht, the Netherlands

• 2003 Young Investigator Award from the European Society for Neuroscience, Krakow, Poland

• 2005 Young Investigator Award from International Cannabis Association as Medicine, Leiden, NL

• 2017 Prix Galien Research for best preclinical drug discovery research in the Netherlands

• 2018 Young Investigator Award from the ICRS for major contributions to cannabinoid research

• 2018 VICI-award (1.5 M Euro) from the Netherlands Research Council

1. van Esbroeck, A. C. M.; Janssen, A. P. A.; Cognetta, A. B., 3rd; Ogasawara, D.; Shpak, G.; van der Kroeg, M.; Kantae, V.; Baggelaar, M. P.; de Vrij, F. M. S.; Deng, H.; Allara, M.; Fezza, F.; Lin, Z.; van der Wel, T.; Soethoudt, M.; Mock, E. D.; den Dulk, H.; Baak, I. L.; Florea, B. I.; Hendriks, G.; De Petrocellis, L.; Overkleeft, H. S.; Hankemeier, T.; De Zeeuw, C. I.; Di Marzo, V.; Maccarrone, M.; Cravatt, B. F.; Kushner, S. A.; van der Stelt, M., Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474. Science 2017, 356 (6342), 1084-1087 DOI: 10.1126/science.aaf7497

2. van Rooden EJ, Florea BI, Deng H, Baggelaar MP, van Esbroeck ACM, Zhou J, Overkleeft HS, van der Stelt M. Mapping in vivo target interaction profiles of covalent inhibitors using chemical proteomics with label-free quantification. Nature Protoc. 2018, 13(4):752-767. doi: 10.1038/nprot.2017.159.

3. Punt JM, van der Vliet D, van der Stelt M. Chemical Probes to Control and Visualize Lipid Metabolism in the Brain. Acc Chem Res. 2022 Nov 15;55(22):3205-3217. doi: 10.1021/acs.accounts.2c00521.

4. Mock ED, Mustafa M, Gunduz-Cinar O, Cinar R, Petrie GN, Kantae V, Di X, Ogasawara D, Varga ZV, Paloczi J, Miliano C, Donvito G, van Esbroeck ACM, van der Gracht AMF, Kotsogianni I, Park JK, Martella A, van der Wel T, Soethoudt M, Jiang M, Wendel TJ, Janssen APA, Bakker AT, Donovan CM, Castillo LI, Florea BI, Wat J, van den Hurk H, Wittwer M, Grether U, Holmes A, van Boeckel CAA, Hankemeier T, Cravatt BF, Buczynski MW, Hill MN, Pacher P, Lichtman AH, van der Stelt M. Discovery of a NAPE-PLD inhibitor that modulates emotional behavior in mice. Nature Chem Biol. 2020, 16(6):667-675 DOI: 10.1038/s41589-020-0528-7

5. 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. Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition. Proc Natl Acad Sci U S A. 2016, 113(1):26-33. doi: 10.1073/pnas.1522364112.

6. 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. Highly Selective, Reversible Inhibitor Identified by Comparative Chemoproteomics Modulates Diacylglycerol Lipase Activity in Neurons. J Am Chem Soc. 2015, 137(27):8851-7. doi: 10.1021/jacs.5b04883.

7. Soethoudt, M.; Stolze, S. C.; Westphal, M. V.; van Stralen, L.; Martella, A.; van Rooden, E. J.; Guba, W.; Varga, Z. V.; Deng, H.; van Kasteren, S. I.; Grether, U.; AP, I. J.; Pacher, P.; Carreira, E. M.; Overkleeft, H. S.; Ioan-Facsinay, A.; Heitman, L. H.; van der Stelt, M., Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells. J Am Chem Soc 2018, 140 (19), 6067-6075 DOI: 10.1021/jacs.7b11281

8. Gagestein B, von Hegedus JH, Kwekkeboom JC, Heijink M, Blomberg N, van der Wel T, Florea BI, van den Elst H, Wals K, Overkleeft HS, Giera M, Toes REM, Ioan-Facsinay A, van der Stelt M. Comparative Photoaffinity Profiling of Omega-3 Signaling Lipid Probes Reveals Prostaglandin Reductase 1 as a Metabolic Hub in Human Macrophages. J Am Chem Soc. 2022, 144(41):18938-18947. doi: 10.1021/jacs.2c06827.

9. 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. Development of a Retinal-Based Probe for the Profiling of Retinaldehyde Dehydrogenases in Cancer Cells. ACS Cent Sci. 2019, 5(12):1965-1974. doi: 10.1021/acscentsci.9b01022.

10. van der Wel T, Hilhorst R, den Dulk H, van den Hooven T, Prins NM, Wijnakker JAPM, Florea BI, Lenselink EB, van Westen GJP, Ruijtenbeek R, Overkleeft HS, Kaptein A, Barf T, van der Stelt M. Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis. Nat Commun. 2020 Jun 25;11(1):3216. doi: 10.1038/s41467-020-17027-5.