Publications by authors named "Olaf Kinzel"

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Optimization and Chemoproteomic Profiling of a Selective, Covalent Bfl-1-Targeting Cellular Tool.
J Henry Blackwell, Simon C C Lucas, Giovanni Battocchio, Ulf Börjesson, Mark J Bostock, Olaf Kinzel

J Med Chem· December 2025

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Identification of JNJ-61803534, a RORγt Inverse Agonist for the Treatment of Psoriasis.
Olaf Kinzel, Steven D Goldberg, Maxwell D Cummings, Christian Gege, Christoph Steeneck

J Med Chem· April 2025

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Structure-Based Discovery of a Series of Covalent, Orally Bioavailable, and Selective BFL1 Inhibitors.
Adeline Palisse, Tony Cheung, Aileen Blokhuis, Thomas Cogswell, Bruna S Martins, Olaf Kinzel

J Med Chem· December 2024

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Structure-Based Optimization of a Series of Covalent, Cell Active Bfl-1 Inhibitors.
Simon C C Lucas, J Henry Blackwell, Ulf Börjesson, David Hargreaves, Alexander G Milbradt, Olaf Kinzel

J Med Chem· September 2024

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Identification and Evaluation of Reversible Covalent Binders to Cys55 of Bfl-1 from a DNA-Encoded Chemical Library Screen.
Simon C C Lucas, J Henry Blackwell, Ulf Börjesson, David Hargreaves, Alexander G Milbradt, Olaf Kinzel

ACS Med Chem Lett· June 2024

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Development of Cilofexor, an Intestinally-Biased Farnesoid X Receptor Agonist, for the Treatment of Fatty Liver Disease.
David Hollenback, Eva Hambruch, Gero Fink, Manfred Birkel, Andreas Schulz, Olaf Kinzel

J Pharmacol Exp Ther· March 2024

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Author Correction: Preclinical and clinical characterization of the RORγt inhibitor JNJ-61803534.
Xiaohua Xue, Aimee De Leon-Tabaldo, Rosa Luna-Roman, Glenda Castro, Michael Albers, Olaf Kinzel

Sci Rep· April 2022

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Preclinical and clinical characterization of the RORγt inhibitor JNJ-61803534.
Xiaohua Xue, Aimee De Leon-Tabaldo, Rosa Luna-Roman, Glenda Castro, Michael Albers, Olaf Kinzel

Sci Rep· May 2021

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Discovery of highly potent heme-displacing IDO1 inhibitors based on a spirofused bicyclic scaffold.
Olaf Kinzel, Christoph Steeneck, Simon Anderhub, Martin Hornberger, Sheena Pinto

Bioorg Med Chem Lett· February 2021

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Discovery and optimization of substituted oxalamides as novel heme-displacing IDO1 inhibitors.
Christoph Steeneck, Olaf Kinzel, Simon Anderhub, Martin Hornberger, Sheena Pinto

Bioorg Med Chem Lett· February 2021

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Discovery and optimization of new oxadiazole substituted thiazole RORγt inverse agonists through a bioisosteric amide replacement approach.
Christoph Steeneck, Christian Gege, Olaf Kinzel, Michael Albers, Gerald Kleymann

Bioorg Med Chem Lett· June 2020

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Optimization and biological evaluation of thiazole-bis-amide inverse agonists of RORγt.
Christian Gege, Michael Albers, Olaf Kinzel, Gerald Kleymann, Thomas Schlüter

Bioorg Med Chem Lett· June 2020

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Discovery of Hydroxyamidine Based Inhibitors of IDO1 for Cancer Immunotherapy with Reduced Potential for Glucuronidation.
Christoph Steeneck, Olaf Kinzel, Simon Anderhub, Martin Hornberger, Sheena Pinto

ACS Med Chem Lett· February 2020

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Nonsteroidal FXR Ligands: Current Status and Clinical Applications.
Christian Gege, Eva Hambruch, Nina Hambruch, Olaf Kinzel, Claus Kremoser

Handb Exp Pharmacol· September 2019

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Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Christian Gege, Maxwell D Cummings, Michael Albers, Olaf Kinzel, Gerald Kleymann

Bioorg Med Chem Lett· May 2018

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Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties.
Olaf Kinzel, Christoph Steeneck, Thomas Schlüter, Andreas Schulz, Christian Gege

Bioorg Med Chem Lett· August 2016

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Knocking on FXR's door: the "hammerhead"-structure series of FXR agonists - amphiphilic isoxazoles with potent in vitro and in vivo activities.
Christian Gege, Olaf Kinzel, Christoph Steeneck, Andreas Schulz, Claus Kremoser

Curr Top Med Chem· July 2015

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The nuclear bile acid receptor FXR controls the liver derived tumor suppressor histidine-rich glycoprotein.
Ulrich Deuschle, Manfred Birkel, Eva Hambruch, Martin Hornberger, Olaf Kinzel

Int J Cancer· June 2015

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FXR controls the tumor suppressor NDRG2 and FXR agonists reduce liver tumor growth and metastasis in an orthotopic mouse xenograft model.
Ulrich Deuschle, Julia Schüler, Andreas Schulz, Thomas Schlüter, Olaf Kinzel

PLoS One· April 2013

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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.
Eva Hambruch, Shinobu Miyazaki-Anzai, Ulrike Hahn, Silke Matysik, Alfred Boettcher, Olaf Kinzel

J Pharmacol Exp Ther· December 2012

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Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 2.
Olaf Kinzel, Anna Alfieri, Sergio Altamura, Mirko Brunetti, Simone Bufali

Bioorg Med Chem Lett· August 2011

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Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydroimid azo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 1.
Savina Malancona, Sergio Altamura, Gessica Filocamo, Olaf Kinzel, Jose Ignacio Martin Hernando

Bioorg Med Chem Lett· August 2011

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Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Ulrich Abel, Thomas Schlüter, Andreas Schulz, Eva Hambruch, Christoph Steeneck, Olaf Kinzel

Bioorg Med Chem Lett· August 2010

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Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.
Federica Ferrigno, Danila Branca, Olaf Kinzel, Samuele Lillini, Laura Llauger Bufi

Bioorg Med Chem Lett· February 2010

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Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).
Giovanna Pescatore, Danila Branca, Fabrizio Fiore, Olaf Kinzel, Laura Llauger Bufi

Bioorg Med Chem Lett· February 2010

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