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Structural basis of species-selective antagonist binding to the succinate receptor.

Haffke M, Fehlmann D, Rummel G, Boivineau J, Duckely M, Gommermann N, Cotesta S, Sirockin F, Freuler F, Littlewood-Evans A, Kaupmann K, Jaakola VP.

Nature. 2019 Oct;574(7779):581-585. doi: 10.1038/s41586-019-1663-8. Epub 2019 Oct 23.


Antagonizing Retinoic Acid-Related-Orphan Receptor Gamma Activity Blocks the T Helper 17/Interleukin-17 Pathway Leading to Attenuated Pro-inflammatory Human Keratinocyte and Skin Responses.

Ecoeur F, Weiss J, Kaupmann K, Hintermann S, Orain D, Guntermann C.

Front Immunol. 2019 Mar 26;10:577. doi: 10.3389/fimmu.2019.00577. eCollection 2019.


Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model.

Carcache DA, Vulpetti A, Kallen J, Mattes H, Orain D, Stringer R, Vangrevelinghe E, Wolf RM, Kaupmann K, Ottl J, Dawson J, Cooke NG, Hoegenauer K, Billich A, Wagner J, Guntermann C, Hintermann S.

J Med Chem. 2018 Aug 9;61(15):6724-6735. doi: 10.1021/acs.jmedchem.8b00529. Epub 2018 Jul 24.


PET Imaging of T Cells: Target Identification and Feasibility Assessment.

Auberson YP, Briard E, Rudolph B, Kaupmann K, Smith P, Oberhauser B.

ChemMedChem. 2018 Aug 10;13(15):1566-1579. doi: 10.1002/cmdc.201800241. Epub 2018 Jul 2.


Pharmacological inhibition of RORγt suppresses the Th17 pathway and alleviates arthritis in vivo.

Guendisch U, Weiss J, Ecoeur F, Riker JC, Kaupmann K, Kallen J, Hintermann S, Orain D, Dawson J, Billich A, Guntermann C.

PLoS One. 2017 Nov 20;12(11):e0188391. doi: 10.1371/journal.pone.0188391. eCollection 2017.


Structural States of RORγt: X-ray Elucidation of Molecular Mechanisms and Binding Interactions for Natural and Synthetic Compounds.

Kallen J, Izaac A, Be C, Arista L, Orain D, Kaupmann K, Guntermann C, Hoegenauer K, Hintermann S.

ChemMedChem. 2017 Jul 6;12(13):1014-1021. doi: 10.1002/cmdc.201700278. Epub 2017 Jun 20.


Retinoic-acid-orphan-receptor-C inhibition suppresses Th17 cells and induces thymic aberrations.

Guntermann C, Piaia A, Hamel ML, Theil D, Rubic-Schneider T, Del Rio-Espinola A, Dong L, Billich A, Kaupmann K, Dawson J, Hoegenauer K, Orain D, Hintermann S, Stringer R, Patel DD, Doelemeyer A, Deurinck M, Schümann J.

JCI Insight. 2017 Mar 9;2(5):e91127. doi: 10.1172/jci.insight.91127.


Blunted 5-HT1A receptor-mediated responses and antidepressant-like behavior in mice lacking the GABAB1a but not GABAB1b subunit isoforms.

Jacobson LH, Hoyer D, Fehlmann D, Bettler B, Kaupmann K, Cryan JF.

Psychopharmacology (Berl). 2017 May;234(9-10):1511-1523. doi: 10.1007/s00213-016-4521-5. Epub 2017 Jan 9.


Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine RORγt Inverse Agonists.

Hintermann S, Guntermann C, Mattes H, Carcache DA, Wagner J, Vulpetti A, Billich A, Dawson J, Kaupmann K, Kallen J, Stringer R, Orain D.

ChemMedChem. 2016 Dec 16;11(24):2640-2648. doi: 10.1002/cmdc.201600500. Epub 2016 Nov 30.


Differential roles of GABAB1 subunit isoforms on locomotor responses to acute and repeated administration of cocaine.

Jacobson LH, Sweeney FF, Kaupmann K, O'Leary OF, Gassmann M, Bettler B, Cryan JF.

Behav Brain Res. 2016 Feb 1;298(Pt B):12-6. doi: 10.1016/j.bbr.2015.10.039. Epub 2015 Oct 27.


Chemical genetic approach identifies microtubule affinity-regulating kinase 1 as a leucine-rich repeat kinase 2 substrate.

Krumova P, Reyniers L, Meyer M, Lobbestael E, Stauffer D, Gerrits B, Muller L, Hoving S, Kaupmann K, Voshol J, Fabbro D, Bauer A, Rovelli G, Taymans JM, Bouwmeester T, Baekelandt V.

FASEB J. 2015 Jul;29(7):2980-92. doi: 10.1096/fj.14-262329. Epub 2015 Apr 8.


Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior.

Gee CE, Peterlik D, Neuhäuser C, Bouhelal R, Kaupmann K, Laue G, Uschold-Schmidt N, Feuerbach D, Zimmermann K, Ofner S, Cryan JF, van der Putten H, Fendt M, Vranesic I, Glatthar R, Flor PJ.

J Biol Chem. 2014 Apr 18;289(16):10975-87. doi: 10.1074/jbc.M113.542654. Epub 2014 Mar 4.


A screen for enhancers of clearance identifies huntingtin as a heat shock protein 90 (Hsp90) client protein.

Baldo B, Weiss A, Parker CN, Bibel M, Paganetti P, Kaupmann K.

J Biol Chem. 2012 Jan 6;287(2):1406-14. doi: 10.1074/jbc.M111.294801. Epub 2011 Nov 28.


LRRK2 protein levels are determined by kinase function and are crucial for kidney and lung homeostasis in mice.

Herzig MC, Kolly C, Persohn E, Theil D, Schweizer T, Hafner T, Stemmelen C, Troxler TJ, Schmid P, Danner S, Schnell CR, Mueller M, Kinzel B, Grevot A, Bolognani F, Stirn M, Kuhn RR, Kaupmann K, van der Putten PH, Rovelli G, Shimshek DR.

Hum Mol Genet. 2011 Nov 1;20(21):4209-23. doi: 10.1093/hmg/ddr348. Epub 2011 Aug 9.


Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor.

Hintermann S, Hurth K, Nozulak J, Tintelnot-Blomley M, Aichholz R, Blanz J, Kaupmann K, Mosbacher J.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1523-6. doi: 10.1016/j.bmcl.2010.12.107. Epub 2010 Dec 28.


Both GABA(B) receptor activation and blockade exacerbated anhedonic aspects of nicotine withdrawal in rats.

Vlachou S, Paterson NE, Guery S, Kaupmann K, Froestl W, Banerjee D, Finn MG, Markou A.

Eur J Pharmacol. 2011 Mar 25;655(1-3):52-8. doi: 10.1016/j.ejphar.2011.01.009. Epub 2011 Jan 22.


Reduction of alcohol's reinforcing and motivational properties by the positive allosteric modulator of the GABA(B) receptor, BHF177, in alcohol-preferring rats.

Maccioni P, Carai MA, Kaupmann K, Guery S, Froestl W, Leite-Morris KA, Gessa GL, Colombo G.

Alcohol Clin Exp Res. 2009 Oct;33(10):1749-56. doi: 10.1111/j.1530-0277.2009.01012.x. Epub 2009 Jul 1.


The sushi domains of secreted GABA(B1) isoforms selectively impair GABA(B) heteroreceptor function.

Tiao JY, Bradaia A, Biermann B, Kaupmann K, Metz M, Haller C, Rolink AG, Pless E, Barlow PN, Gassmann M, Bettler B.

J Biol Chem. 2008 Nov 7;283(45):31005-11. doi: 10.1074/jbc.M804464200. Epub 2008 Sep 2.


Roles of GABAB receptor subtypes in presynaptic auto- and heteroreceptor function regulating GABA and glutamate release.

Waldmeier PC, Kaupmann K, Urwyler S.

J Neural Transm (Vienna). 2008 Oct;115(10):1401-11. doi: 10.1007/s00702-008-0095-7. Epub 2008 Jul 30.


Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats.

Paterson NE, Vlachou S, Guery S, Kaupmann K, Froestl W, Markou A.

J Pharmacol Exp Ther. 2008 Jul;326(1):306-14. doi: 10.1124/jpet.108.139204. Epub 2008 Apr 29.


Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors.

Guery S, Floersheim P, Kaupmann K, Froestl W.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6206-11. Epub 2007 Sep 8.


Specific roles of GABA(B(1)) receptor isoforms in cognition.

Jacobson LH, Kelly PH, Bettler B, Kaupmann K, Cryan JF.

Behav Brain Res. 2007 Jul 19;181(1):158-62. Epub 2007 Apr 5.


GABAB receptor-positive modulation-induced blockade of the rewarding properties of nicotine is associated with a reduction in nucleus accumbens DeltaFosB accumulation.

Mombereau C, Lhuillier L, Kaupmann K, Cryan JF.

J Pharmacol Exp Ther. 2007 Apr;321(1):172-7. Epub 2007 Jan 10.


Behavioral evaluation of mice deficient in GABA(B(1)) receptor isoforms in tests of unconditioned anxiety.

Jacobson LH, Bettler B, Kaupmann K, Cryan JF.

Psychopharmacology (Berl). 2007 Mar;190(4):541-53. Epub 2006 Dec 15.


GABAB1 receptor subunit isoforms exert a differential influence on baseline but not GABAB receptor agonist-induced changes in mice.

Jacobson LH, Bettler B, Kaupmann K, Cryan JF.

J Pharmacol Exp Ther. 2006 Dec;319(3):1317-26. Epub 2006 Sep 21.


GABA(B(1)) receptor isoforms differentially mediate the acquisition and extinction of aversive taste memories.

Jacobson LH, Kelly PH, Bettler B, Kaupmann K, Cryan JF.

J Neurosci. 2006 Aug 23;26(34):8800-3.


Generalization of amygdala LTP and conditioned fear in the absence of presynaptic inhibition.

Shaban H, Humeau Y, Herry C, Cassasus G, Shigemoto R, Ciocchi S, Barbieri S, van der Putten H, Kaupmann K, Bettler B, Lüthi A.

Nat Neurosci. 2006 Aug;9(8):1028-35. Epub 2006 Jul 2.


GABA(B) receptor-positive modulation decreases selective molecular and behavioral effects of cocaine.

Lhuillier L, Mombereau C, Cryan JF, Kaupmann K.

Neuropsychopharmacology. 2007 Feb;32(2):388-98. Epub 2006 May 17.


Differential compartmentalization and distinct functions of GABAB receptor variants.

Vigot R, Barbieri S, Bräuner-Osborne H, Turecek R, Shigemoto R, Zhang YP, Luján R, Jacobson LH, Biermann B, Fritschy JM, Vacher CM, Müller M, Sansig G, Guetg N, Cryan JF, Kaupmann K, Gassmann M, Oertner TG, Bettler B.

Neuron. 2006 May 18;50(4):589-601.


Hyperdopaminergia and altered locomotor activity in GABAB1-deficient mice.

Vacher CM, Gassmann M, Desrayaud S, Challet E, Bradaia A, Hoyer D, Waldmeier P, Kaupmann K, Pévet P, Bettler B.

J Neurochem. 2006 May;97(4):979-91. Epub 2006 Apr 5.


Subtype-selective interaction with the transcription factor CCAAT/enhancer-binding protein (C/EBP) homologous protein (CHOP) regulates cell surface expression of GABA(B) receptors.

Sauter K, Grampp T, Fritschy JM, Kaupmann K, Bettler B, Mohler H, Benke D.

J Biol Chem. 2005 Sep 30;280(39):33566-72. Epub 2005 Aug 4.


The RXR-type endoplasmic reticulum-retention/retrieval signal of GABAB1 requires distant spacing from the membrane to function.

Gassmann M, Haller C, Stoll Y, Abdel Aziz S, Biermann B, Mosbacher J, Kaupmann K, Bettler B.

Mol Pharmacol. 2005 Jul;68(1):137-44. Epub 2005 Apr 1.


Altered anxiety and depression-related behaviour in mice lacking GABAB(2) receptor subunits.

Mombereau C, Kaupmann K, Gassmann M, Bettler B, van der Putten H, Cryan JF.

Neuroreport. 2005 Feb 28;16(3):307-10.


Don't worry 'B' happy!: a role for GABA(B) receptors in anxiety and depression.

Cryan JF, Kaupmann K.

Trends Pharmacol Sci. 2005 Jan;26(1):36-43. Review.


Determination of the minimal functional ligand-binding domain of the GABAB1b receptor.

Deriu D, Gassmann M, Firbank S, Ristig D, Lampert C, Mosbacher J, Froestl W, Kaupmann K, Bettler B, Grütter MG.

Biochem J. 2005 Mar 15;386(Pt 3):423-31.


Altered hippocampal expression of calbindin-D-28k and calretinin in GABA(B(1))-deficient mice.

Rüttimann E, Vacher CM, Gassmann M, Kaupmann K, Van der Putten H, Bettler B.

Biochem Pharmacol. 2004 Oct 15;68(8):1613-20.


Altered response to benzodiazepine anxiolytics in mice lacking GABA B(1) receptors.

Mombereau C, Kaupmann K, van der Putten H, Cryan JF.

Eur J Pharmacol. 2004 Aug 16;497(1):119-20.


Independent maturation of the GABA(B) receptor subunits GABA(B1) and GABA(B2) during postnatal development in rodent brain.

Fritschy JM, Sidler C, Parpan F, Gassmann M, Kaupmann K, Bettler B, Benke D.

J Comp Neurol. 2004 Sep 20;477(3):235-52.


Molecular structure and physiological functions of GABA(B) receptors.

Bettler B, Kaupmann K, Mosbacher J, Gassmann M.

Physiol Rev. 2004 Jul;84(3):835-67. Review.


Redistribution of GABAB(1) protein and atypical GABAB responses in GABAB(2)-deficient mice.

Gassmann M, Shaban H, Vigot R, Sansig G, Haller C, Barbieri S, Humeau Y, Schuler V, Müller M, Kinzel B, Klebs K, Schmutz M, Froestl W, Heid J, Kelly PH, Gentry C, Jaton AL, Van der Putten H, Mombereau C, Lecourtier L, Mosbacher J, Cryan JF, Fritschy JM, Lüthi A, Kaupmann K, Bettler B.

J Neurosci. 2004 Jul 7;24(27):6086-97.


Behavioral characterization of the novel GABAB receptor-positive modulator GS39783 (N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine): anxiolytic-like activity without side effects associated with baclofen or benzodiazepines.

Cryan JF, Kelly PH, Chaperon F, Gentsch C, Mombereau C, Lingenhoehl K, Froestl W, Bettler B, Kaupmann K, Spooren WP.

J Pharmacol Exp Ther. 2004 Sep;310(3):952-63. Epub 2004 Apr 27.


Genetic and pharmacological evidence of a role for GABA(B) receptors in the modulation of anxiety- and antidepressant-like behavior.

Mombereau C, Kaupmann K, Froestl W, Sansig G, van der Putten H, Cryan JF.

Neuropsychopharmacology. 2004 Jun;29(6):1050-62.


Selected amino acids, dipeptides and arylalkylamine derivatives do not act as allosteric modulators at GABAB receptors.

Urwyler S, Gjoni T, Kaupmann K, Pozza MF, Mosbacher J.

Eur J Pharmacol. 2004 Jan 12;483(2-3):147-53.


Specific gamma-hydroxybutyrate-binding sites but loss of pharmacological effects of gamma-hydroxybutyrate in GABA(B)(1)-deficient mice.

Kaupmann K, Cryan JF, Wellendorph P, Mombereau C, Sansig G, Klebs K, Schmutz M, Froestl W, van der Putten H, Mosbacher J, Bräuner-Osborne H, Waldmeier P, Bettler B.

Eur J Neurosci. 2003 Nov;18(10):2722-30.


Recognition molecule associated carbohydrate inhibits postsynaptic GABA(B) receptors: a mechanism for homeostatic regulation of GABA release in perisomatic synapses.

Saghatelyan AK, Snapyan M, Gorissen S, Meigel I, Mosbacher J, Kaupmann K, Bettler B, Kornilov AV, Nifantiev NE, Sakanyan V, Schachner M, Dityatev A.

Mol Cell Neurosci. 2003 Oct;24(2):271-82.


N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function.

Urwyler S, Pozza MF, Lingenhoehl K, Mosbacher J, Lampert C, Froestl W, Koller M, Kaupmann K.

J Pharmacol Exp Ther. 2003 Oct;307(1):322-30. Epub 2003 Sep 3.


Nogo-A inhibits neurite outgrowth and cell spreading with three discrete regions.

Oertle T, van der Haar ME, Bandtlow CE, Robeva A, Burfeind P, Buss A, Huber AB, Simonen M, Schnell L, Brösamle C, Kaupmann K, Vallon R, Schwab ME.

J Neurosci. 2003 Jul 2;23(13):5393-406.


Characterization of two novel proteins, NgRH1 and NgRH2, structurally and biochemically homologous to the Nogo-66 receptor.

Pignot V, Hein AE, Barske C, Wiessner C, Walmsley AR, Kaupmann K, Mayeur H, Sommer B, Mir AK, Frentzel S.

J Neurochem. 2003 May;85(3):717-28.

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