The Gertsch Lab
Transdisciplinary Molecular Research
Institute of Biochemistry and Molecular Medicine, University of Bern
IBMM
Research Mission
We study the molecular mechanisms of action of small organic molecules and use them as tools to understand biochemical and biological processes. We are interested in molecular pharmacology and the role of the endocannabinoid system in inflammation and stress (HPA and sympathoadrenal axes). Our lab is specialized on lipids and highly apolar membrane constituents. The transdisciplinary research in the Gertsch lab involves chemical biology, animal studies, biochemistry and molecular biology (transgenic animal models), as well as high-end LC-MS/MS and GC-MS analytics. Our research is dedicated to translational aspects related drug discovery and biochemical processes in diseases. We have a strong interest in neuropharmacology and natural products as source of bioactive molecules and study their convergent evolution in different organisms like mammals, plants and Trypanosma cruzi.
Current Research Projects
News & Recent Publications
Examplary Research Papers
Unovering the psychoactivity of a cannabinoid from liverworts associated with a legal high. Chicca A, Schafroth M, Reynoso-Moreno I, Erni E, Petrucci V, Carreira EM, Gertsch J. Science Advances, 2018, 4, 10, eaat2166.
Chemical probes to potently and selectively inhibit endocannabinoid reuptake. Chicca A, Nicolussi S, Bartholomäus R, Blunder M, Aparisi Rey A, Petrucci V, Reynoso-Moreno IDC, Viveros-Paredes JM, Dalghi Gens M, Lutz B, Schiöth HB, Soeberdt M, Abels C, Charles RP, Altmann KH, Gertsch J. PNAS, 2017, 114(25):E5006-E5015.
Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity. Soethoudt M, ... Di Marzo V, Gertsch J, Lichtman AH, Maccarrone M,Pacher P, Glass M, van der Stelt M. Nature Com., 2017, 3;8:13958.
Targeted metabolomics shows plasticity in the evolution of signaling lipids and uncovers old and new endocannabinoids in the plant kingdom. Gachet MS, Schubert, A, Calarco S, Boccard J, Gertsch J.
Scientific Reports, 2017, 7:41177.
Localization and production of peptide endocannabinoids in the rodent CNS and adrenal medulla. Hofer SC, Ralvenius WT, Gachet MS, Fritschy JM, Zeilhofer HU, Gertsch J. Neuropharmacology 2015, 98:78-89.
The major central endo-cannabinoid directly acts at GABA(A) receptors. Sigel E, Baur R, Rácz I, Marazzi J, Smart TG, Zimmer A, Gertsch J. PNAS, 2011,108(44):18150-5.
Beta-caryophyllene is a dietary cannabinoid. Gertsch J, Leonti M, Raduner S, Racz I, Chen JZ, Xie XQ, Altmann KH, Karsak M, Zimmer A. PNAS 2008, 105(26):9099-104.
Recent Collaborative Research Papers
Association of endocannabinoids with pain in endometriosis. Andrieu T, Chicca A, Pellegata D, Bersinger NA, Imboden S, Nirgianakis K, Gertsch J, Mueller MD. Pain. 2021, doi: 10.1097/j.pain.0000000000002333.
Diacylglycerol lipase alpha in astrocytes is involved in maternal care and affective behaviors. Schuele LL, Glasmacher S, Gertsch J, Roggan MD, Transfeld JL, Bindila L, Lutz B, Kolbe CC, Bilkei-Gorzo A, Zimmer A, Leidmaa E. Glia. 2021, 69(2):377-391.
Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors. Granchi C, Bononi G, Ferrisi R, Gori E, Mantini G, Glasmacher S, Poli G, Palazzolo S, Caligiuri I, Rizzolio F, Canzonieri V, Perin T, Gertsch J, Sodi A, Giovannetti E, Macchia M, Minutolo F, Tuccinardi T, Chicca A. Eur J Med Chem. 2021, 209:112857.
Salm A, Krishnan SR et al. Phylobioactive hotspots in plant resources used to treat Chagas disease
iScience, https://doi.org/10.1016/j.isci.2021.102310
Globally, more than six million people are infected with Trypanosoma cruzi, the causative protozoan parasite of the vector-borne Chagas disease. We conducted a cross-sectional ethnopharmacological field study in Bolivia among different ethnic groups where CD is hyperendemic. A total of 775 extracts of botanical drugs used in Bolivia in the context of CD and botanical drugs from unrelated indications from the Mediterranean De Materia Medica compiled by Dioscorides two thousand years ago were profiled in a multidimensional assay uncovering different antichagasic natural product classes. Intriguingly, the phylobioactive anthraquinone hotspot matched the antichagasic activity of Senna chloroclada, the taxon with the strongest ethnomedical consensus for treating CD among the Izoceño-Guaraní. Testing common 9,10-anthracenedione derivatives in T. cruzi cellular infection assays demarcates hydroxyanthraquinone as potential antichagasic lead scaffold. Our study systematically uncovers in vitro antichagasic phylogenetic hotspots in the plant kingdom as a potential resource for drug discovery based on ethnopharmacological hypotheses.
Recent Papers
Adv Biol Regul, 2021, in press. Characterization of pepcan-23 as pro-peptide of RVD-hemopressin (pepcan-12) and stability of hemopressins in mice. Glasmacher S, Gertsch J.
Cell Discovery, 2021, 7(1), 16. Mechanism of substrate transport and inhibition of the human LAT1-4F2hc amino acid transporter. Yan R, Li Y, Müller J, Zhang Y, Singer S, Xia L, Zhong X, Gertsch J, Altmann KH, Zhou Q.
ACS Pharmacol Transl Sci, 2021. in press. Selective endocannabinoid reuptake inhibitor WOBE437 reduces disease progression in a mouse model of multiple sclerosis. Reynoso Moreno I., Tietz S, Vallini E, Engelhardt B, Gertsch J, Chicca A.
Glia, 2021, 69, 377-391. Diacylgylcerol lipase alpha in astrocytes is involved in maternal care and affective behaviors. Schuele LL, Glasmacher S, Gertsch J, Roggan MD, Transfeld JL, Bindila L, Lutz B, Kolbe CC, Bilkei-Gorzo A, Zimmer A, Leidmann E.
Eur J Med Chem. 2021, 209:112857. Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors. Granchi C, Bononi G, Ferrisi R, Gori E, Mantini G, Glasmacher S, Poli G, Palazzolo S, Caligiuri I, Rizzolio F, Canzonieri V, Perin T, Gertsch J, Sodi A, Giovannetti E, Macchia M, Minutolo F, Tuccinardi T, Chicca A.
Food Res Int. 2021, 141:110123. LC-HRMS/MS-based phytochemical profiling of Piper spices: Global association of piperamides with endocannabinoid system modulation. Luca SV, Minceva M, Gertsch J, Skalicka-Woźniak K.
Chemistry, 2020, in press. Synthesis of morpholine-based analogs of (-)-zampanolide and their biological activity. Altmann, KH, Bold, CP, Schürmann, J, Lucena Agell D, Diaz JF, Gertsch J.
ChemMedChem, 2021,16(1):145-154. Synthesis and Biological Evaluation of Endocannabinoid Uptake Inhibitors Derived from WOBE437. Mäder P., Barthalomäus R., Nicolussi S., Baumann A., Weis M., Chicca A., Rau M., Simao AC., Gertsch J., Altmann KH.
Oncogene, 2020, 39(14), 2948-2960. The ACSL3-LPIAT1 signaling drives prostaglandin synthesis in non-small lung cancer. Saliakoura M, Reynoso-Moreno I, Pozzato C, Rossi Sebastiano M, Galie M, Gertsch J, Konstandinidou G.
J. Am. Chem. Soc. 2020, 142(40):16953-16964. Development of high-specifitiy fluorescent probes to enable cannabinoid type 2 receptor studies in living cells. Sarrott R.C., et al.
Parasit Vectors 2019, 12(1):291. Cultural Perception of triatomine bugs and Chagas disease in Bolivia: A cross-sectional study. Salm, A., Gertsch J.
Nat. Chem. Biol. 2019, 15(5) 428-429. Scaffold and organism hopping with chemical probes. Gertsch J.
ChemMedChem, 2019, 14(17) 1590-1596.
Total Synthesis of the Endocannabinoid Uptake Inhibitor Guineensine and SAR Studies. Barthalomäus R., Nicolussi S., Baumann A., Rau M, Simao AC, Gertsch J, Altmann KH.
The Research Team 2021
Prof. Dr. Jürg Gertsch
Principle Investigator
Dr. Ines Reynoso-Moreno
Postdoc
Prof. Dr. Krystyna Skalicka
Lecturer/Visiting Scientist
Dr. Philip Förstner
Postdoc
Dr. Adonis Yiannakas
Postdoc
Simon Singer
Scientific Staff MSc
Sandhya R. Krishnan
PhD student
Daniele Pellegata
LC-MS/MS Specialist MSc
Tatiana Hofer
Lab Technician
Luis Fernando Quiñones
PhD student
Veronika Morozova
PhD student
Daniel Batora
PhD student
Jaap Roukens
PhD student
Linus Rechsteiner
MSc student
Nico M. Schütz
MSc student