S P A C E R

 WELCOME TO OUR LABORATORY 

We study the molecular mechanisms of action of small organic compounds and use them as tools to understand biochemical processes. We are interested in molecular pharmacology and the mechanistic role of the endocannabinoid system (ECS) in inflammation. In particular, we study how endogenous and potentially therapeutic ligands modulate cellular processes, with a focus on drug discovery.

To study the function of the ECS we are using biologically active small  molecules, e.g. natural product-derived molecular scaffolds, for the development of novel modulators of cellular systems. Such molecules may serve both as tools and potential leads for drug development.

We work on the assay development and in vitro screening related to different membrane transporters within the NCCR TransCure, a transdisciplinary consortium in Switzerland dedicated to target transport mechanisms in order to discover new therapeutic principles.

Our research is sponsored by:

SWISS NATIONAL SCIENCE FOUNDATION	NOVARTIS FOUNDATION
COST ACTION	University of Bern Research Foundation

Selected Publications (for full list see 2002-2011)

    Brit J Pharmacol. 2012; accepted. The antinociceptive triterpene β-amyrin inhibits 2-arachidonoylglycerol (2-AG) hydrolysis without directly targeting CB receptors . Chicca A, Marazzi J, Gertsch J. 

    Biochem Pharmacol. 2012; 83(10):1393-412. Cannabinoid receptor trafficking in peripheral cells is dynamically regulated by a binary biochemical switch. Kleyer J, Nicolussi S; Taylor P, Simonelli D, Furger E, Anderle P, Gertsch J.  

    Nature Neurosci. 2012; 15(4):558-64. Mitochondrial CB1 receptors regulate  neuronal energy metabolism. Bénard G, Massa F, Puente N, JLourenço J, Bellocchio L, Soria-Gómez E, Matias I, Delamarre A, Metna-Laurent M, Cannich A, Hebert-Chatelain E, Mulle C, Ortega-Gutiérrez S, Martín-Fontecha M, Klugmann M, Guggenhuber S, Lutz B, Gertsch J, Chaouloff J, López-Rodríguez ML, Grandes P, Rodrigue Rossignol R, Marsicano G 

    Free Rad Biol Med. 2012; 52(8):1325-33. Beta-Caryophyllene ameliorates cisplatin-induced nephrotoxicity in a cannabinoid 2 receptor-dependent manner.  Horvath B, Mukhophadyay P, Kechrid M; Patel V, Tanashian G, Wink Da, Gertsch J, Pacher P.

    J Biol Chem. 2011; 287(1):91-104. Modulation of L-alpha-lysophosphatitylinositol / GPR55 MAK kinase signalling by cannabinoids.  Anavi-Goffer S, Baillie G, Irving AJ; Gertsch J, Greig IR, Pertwee RG, Ross RA.  

    Proc Natl Acad Sci USA (PNAS); 2011; 108(44):18150-5. The major central endocannabinoid directly acts at GABA_A receptors.  Sigel E, Baur R, Racz I, Marazzi J, Smart T, Zimmer A,  Gertsch J. 

    J Immunol. Methods 2011; 373(1-2):219-28. Endocannabinoid content in  fetal bovine sera - unexpected effects on mononuclear cells and osteoclastogenesis.  Marazzi J, Kleyer J, Viveros-Paredes JM, Gertsch J.

J Immunol. 2011; 187(8):4140-50. Ginger phenylpropanoids inhibit IL-1β and prostanoid secretion and disrupt arachidonate-phospholipid remodeling by targeting phospholipases A2. Nievergelt  A, Marazzi J, Schoop R, Altmann K-H, Gertsch J.

    Chem Biol. 2011; 18(8), 1053-1064. Mechanisms of Osteoclastogenesis Inhibition by a Novel Class of Biphenyl-type Cannabinoid CB2 Receptor Inverse Agonists. Schuhly W, Viveros Paredes JM, Kleyer J, Huefner A, Anavi-Goffer S, Raduner S, Altmann, KH, Gertsch J.

    Curr Drug Targ. 2011; 12(11),1513-1514. Natural Products in Chemical Biology. Gertsch J

    Curr Drug Targ. 2011; 12(11), 1515-1530. Biodiversity and Chemodiversity: Future Perspectives in Bioprospecting. Ramesha BT, Gertsch J, Ravikanth G, Priti V, Ganeshaiah KN, Shaanker UR

    Int Immunopharmacol. 2011; 11(9):1303-1310. Mutagenesis and Computer Modeling Studies of A GPCR Conserved Residue W5.43(194) in Ligand Recognition and Signal Transduction For CB2 Receptor. Zhang Y, Xie Z, Wang L, Schreiter B, Lazo J, Gertsch J, Xie X-Q.

    Brit J Pharmacol. 2011, 165(8):2479-84. The Cannabinoid Receptor CB1 Antagonist Rimonabant (SR141716) and AM251 directly potentiate GABA(A) receptors. Baur R, Gertsch J, Sigel E

Planta Med. 2011; 77(11):1086-1098. Botanical Drugs, Synergy, and Network Pharmacology: Forth and Back to Intelligent Mixtures. Gertsch J

    Org Lett. 2010; 12(10):2302-5. Synthesis of (-)-dactylolide and 13-desmethylene- (-)dactylolide and their effects on tubulin. Zurwerra D, Gertsch, J, Altmann, KH

    Angew Chem Int Ed Engl., 2010, 49(33):5767-5770. Catalytic selective cyclizations of aminocylcopropanes: formal synthesis of aspidospermine and total synthesis of goniomitine. De Simone F, Gertsch J, Waser J

    Bioorg Med Chem. 2010; 18(9):3345-51. Identification of Serotonin 5HT1A Receptor Partial Agonists in Ginger. Nievergelt A, Huonker P, Schoop R, Altmann KH, Gertsch J

    Brit J Pharmacol. 2010; 160(3):523-529. Phytocannabinoids Beyond the Cannabis Plant - do they Exist? Gertsch, J, Pertwee RG, Di Marzo, V

    Biochem Pharmacol. 2010; 79(12):1815-1826. Falcarinol is a covalent CB1 receptor antagonist and induces pro-allergic effects in skin. Leonti M, Casu L, Raduner S, Cottiglia F, Altmann K-H, Gertsch J

    ChemBiochem. 2009; 10(15):2513-21. Making epothilones fluoresce: design, synthesis, and biological characerization of a fluorescent N-12-aza-epothilone (azathilone). Gertsch J, Feyen F, Bützberger A, Gerber B, Pfeiffer B, Altmann K-H

J Pharm Pharmacol. 2009;61(7):839-53. Cannabinoid receptor ligands as potential anticancer agents - high hopes for new therapies? Oesch S & Gertsch J

J. Ethnopharmacol. 2009; 122(2):177-183. How scientific is the science in ethnopharmacology? Historical perspectives and epistemological problems. Gertsch J

    J Med Chem. 2009;52(2):369-78. Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow. Markt P, Feldmann C, Rollinger JM, Raduner S, Schuster D, Kirchmair J, Distinto S, Spitzer GM, Wolber G, Laggner C, Altmann KH, Langer T, Gertsch J

    ChemBiochem. 2009;10(1):166-75. Differential effects of natural product microtubule stabilizers on microtubule assembly; single agent and combination studies with taxol, epothilone B, and discodermolide. Gertsch J, Meier S, Müller M, Altmann KH

Proc Natl Acad Sci USA (PNAS). 2008;105(26):9099-104. Beta-caryophyllene is a dietary cannabinoid. Gertsch J*, Leonti M, Raduner S, Racz I, Chen JZ, Xie XQ, Altmann KH, Karsak M, Zimmer A

    Planta Med. 2008;74(6):638-50. Immunomodulatory lipids in plants: plant fatty acid amides and the human endocannabinoid system. Gertsch J

    J Nat Prod. 2007;70(6):1010-5. Self-assembling cannabinomimetics: supramolecular structures of N-alkyl amides. Raduner S, Bisson W, Abagyan R, Altmann KH, Gertsch J

    Nat Prod Rep. 2007;24(2):327-57. Anticancer drugs from nature - natural products as a unique source of new microtubule-stabilizing agents. Altmann KH, Gertsch J

    J Recept Signal Transduct Res. 2006;26(5-6):709-30. New natural noncannabinoid ligands fro cannabinoid type-2 (CB2) receptors. Gertsch J, Raduner S, Altmann KH

J Biol Chem. 2006;281(20):14192-206. Alkylamides from Echinacea are a new class of cannabinomimetics. Cannabinoid type-2 receptor-dependent and -independent immunomodulatory effects. Raduner S, Majewska A, Chen JZ, Xie XQ, Hamon J, Faller B, Altmann KH, Gertsch J

    Angew Chem Int Ed Engl. 2006;45(35):5880-5. Design and synthesis of 12-aza-epothilones (azathilones) - non-natural natural products with potent anticancer activity. Feyen F, Gertsch J, Wartmann M, Altmann KH

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