Publications & Posters

Publications

Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Gege C, Cummings MD, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Nelen MI, Milligan C, Spurlino J, Xue X, Leonard K, Edwards JP, Fourie A, Goldberg SD, Hoffmann T.
Bioorg Med Chem Lett. 2018 May 15;28(9):1446-1455. Epub 2018 Apr 3.
Intestinal Farnesoid X Receptor Controls Transintestinal Cholesterol Excretion in Mice.
de Boer JF, Schonewille M, Boesjes M, Wolters H, Bloks VW, Bos T, van Dijk TH, Jurdzinski A, Boverhof R, Wolters JC, Kuivenhoven JA, van Deursen JM, Oude Elferink RPJ, Moschetta A, Kremoser C, Verkade HJ, Kuipers F, Groen AK.
Gastroenterology. 2017 Apr;152(5):1126-1138. Epub 2017 Jan 5.
The FXR agonist PX20606 ameliorates portal hypertension by targeting vascular remodelling and sinusoidal dysfunction.
Schwabl P, Hambruch E, Seeland BA, Hayden H, Wagner M, Garnys L, Strobel B, Schubert TL, Riedl F, Mitteregger D, Burnet M, Starlinger P, Oberhuber G, Deuschle U, Rohr-Udilova N, Podesser BK, Peck-Radosavljevic M, Reiberger T, Kremoser C, Trauner M.
J Hepatol. 2017 Apr;66(4):724-733. Epub 2016 Dec 18.
Pharmacologic modulation of RORγt translates to efficacy in preclinical and translational models of psoriasis and inflammatory arthritis.
Xue X, Soroosh P, De Leon-Tabaldo A, Luna-Roman R, Sablad M, Rozenkrants N, Yu J, Castro G, Banie H, Fung-Leung WP, Santamaria-Babi L, Schlüter T, Albers M, Leonard K, Budelsky AL, Fourie AM.
Sci Rep. 2016 Dec 1;6:37977.
Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties.
Kinzel O, Steeneck C, Schlüter T, Schulz A, Gege C, Hahn U, Hambruch E, Hornberger M, Spalwisz A, Frick K, Perovic-Ottstadt S, Deuschle U, Burnet M, Kremoser C.
Bioorg Med Chem Lett. 2016 Aug 1;26(15):3746-53. Epub 2016 May 24.
The nuclear bile acid receptor FXR controls the liver derived tumor suppressor histidine-rich glycoprotein.
Deuschle U, Birkel M, Hambruch E, Hornberger M, Kinzel O, Perovic-Ottstadt S, Schulz A, Hahn U, Burnet M, Kremoser C.
Int J Cancer. 2015 Jun 1;136(11):2693-704. Epub 2014 Nov 13.
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
Gege C, Schlüter T, Hoffmann T.
Bioorg Med Chem Lett. 2014 Nov 15;24(22):5265-7. Epub 2014 Sep 28.
Knocking on FXR's door: the "hammerhead"-structure series of FXR agonists - amphiphilic isoxazoles with potent in vitro and in vivo activities.
Gege C, Kinzel O, Steeneck C, Schulz A, Kremoser C.
Curr Top Med Chem. 2014;14(19):2143-58. Review.
FXR controls the tumor suppressor NDRG2 and FXR agonists reduce liver tumor growth and metastasis in an orthotopic mouse xenograft model.
Deuschle U, Schüler J, Schulz A, Schlüter T, Kinzel O, Abel U, Kremoser C.
PLoS One. 2012;7(10):e43044
Synthetic farnesoid x receptor agonists induce high-density lipoprotein-mediated transhepatic cholesterol efflux in mice and monkeys and prevent atherosclerosis in cholesteryl ester transfer protein transgenic low-density lipoprotein receptor (-/-) mice.
Hambruch E, Miyazaki-Anzai S, Hahn U, Matysik S, Boettcher A, Perovic-Ottstadt S, Schlüter T, Kinzel O, Krol HD, Deuschle U, Burnet M, Levi M, Schmitz G, Miyazaki M, Kremoser C.
J Pharmacol Exp Ther. 2012 Dec;343(3):556-67
Synthesis and pharmacological validation of a novel series of non-steroidal
FXR agonists
.
Abel U, Schlüter T, Schulz A, Hambruch E, Steeneck C, Hornberger M, Hoffmann T,
Perović-Ottstadt S, Kinzel O, Burnet M, Deuschle U, Kremoser C.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4911-7
Panning for SNuRMs: using cofactor profiling for the rational discovery of selective nuclear receptor modulators.
Kremoser C, Albers M, Burrris TP, Deusche U, Koegl M.
Drug Discov Today. 2007 Oct;12(19-20):860-9. Epub 2007 Sep 19.
A Novel Principle for Partial Agonism of Liver X Receptor Ligands: COMPETITIVE RECRUITMENT OF ACTIVATORS AND REPRESSORS.
Albers M, Blume B, Schlueter T, Wright MB,
Kober I, Kremoser C, Deuschle U, Koegl M.

J Biol Chem. 2006 Feb 24;281(8):4920-30. Epub 2005 Dec 13.
Automated yeast two-hybrid screening for nuclear receptor-interacting proteins.
Albers M, Kranz H, Kober I, Kaiser C, Klink M, Suckow J, Kern R, Koegl M.
Mol Cell Proteomics. 2005 Feb;4(2):205-13. Epub 2004 Dec 15.

Posters

Identification and Profiling of PX-D26116, a potent Hydroxyamidine-based IDO1 Inhibitor.PDF
CIMT 2018 Annual Meeting, May 15-17, 2018, Mainz, Germany
A novel aryl hydrocarbon receptor antagonist (PX-A24590) with anti-tumor activity in a syngeneic mouse pancreatic cancer model.PDF
CIMT 2018 Annual Meeting, May 15-17, 2018, Mainz, Germany
LXR inverse agonists inhibit de novo lipogenesis and reduce intestinal lipid and cholesterol absorption in a NAFLD mouse model.PDF
European Association for the Study of the Liver: “The International Liver Congress™ 2018”, April 11-15, 2018, Paris, France
LXR inverse agonists inhibit de novo lipogenesis and reduce intestinal lipid and cholesterol absorption in a NAFLD mouse model.PDF
NASH tag conference 2018, January 4-5, Utah, USA
LXR inverse agonists demonstrate liver lipid lowering effects through multiple mechanisms in rodent models of NASH and in human hepatocytesPDF
European Association for the Study of the Liver: “The International Liver Congress™ 2017”, April 19-23, 2017, Amsterdam, Netherlands
LXR inverse agonists demonstrate liver lipid lowering effects through multiple mechanisms in rodent models of NASH and in human hepatocytes.PDF
NASH tag conference 2017, January 5-7, Utah, USA
Novel LXR inverse agonists demonstrate anti-steatotic effects in human hepatocytes and in rodent models of NAFLD.PDF
American Association for the Study of the Liver Diseases: “The Liver Meeting™ 2016”, November 11-15, 2016 Boston, USA
From mice to men - Plasma and fecal bile acid composition as sensitive markers of pharmacological FXR activation: Results from animal and human phase I studies using the potent and selective FXR agonist PX20606.PDF
European Association for the Study of the Liver: “The International Liver Congress™ 2016”, April 13-17, 2016, Barcelona, Spain
Novel LXR inverse agonists demonstrate anti-steatotic effects in human hepatocytes and in rodent models of NAFLD.PDF
Falk Symposium 194: “XXIII International Bile. Acid Meeting: Bile Acids as Signal Integrators and. Metabolic Modulators”, October 89, 2014 Freiburg, Germany
FXR controls the tumor suppressor Histidine Rich Glycoprotein (HRG).PDF
Falk Symposium 194: “XXIII International Bile. Acid Meeting: Bile Acids as Signal Integrators and. Metabolic Modulators”, October 89, 2014 Freiburg, Germany
FXR agonist Px-102 improves hepatic steatosis in NAFLD mouse models. PDF
The Asian Pacific Association for the Study of the Liver: "APASL Liver week", Juni 6-10, 2013 Singapore, Malysia
Synthetic Farnesoid X Receptor agonist PX20606 demonstrates anti-atherosclerotic effects and lowers cholesterol in HDL2 but not in HDL3 subfractions.PDF
DKFZ-ZMBH Alliance Forum: "Metabolism 2012 From Signaling to Disease", November 15-16, 2012 Heidelberg, Germany
Strong anti-steatotic and anti-fibrotic effects of novel FXR agonists in a murine NASH model that resembles human NASH.PDF
The 9th JSH Single Topic Conference :"NASH 2010" November 18-19, 2010 Tokyo, Japan