Publications by authors named "Michael Kiffe"

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A cereblon-based glue degrader of NEK7 regulates NLRP3 inflammasome in a context-dependent manner.
Aude Sylvain, Natacha Stoehr, Fupeng Ma, Artiom Cernijenko, Martin Schröder, Michael Kiffe

Cell Chem Biol· July 2025

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Discovery of GJG057, a Potent and Highly Selective Inhibitor of Leukotriene C4 Synthase.
Gebhard Thoma, Wolfgang Miltz, Rudolf Waelchli, David Orain, Carsten Spanka, Michael Kiffe

J Med Chem· February 2025

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Structure-Guided Elaboration of a Fragment-Like Hit into an Orally Efficacious Leukotriene A4 Hydrolase Inhibitor.
Gebhard Thoma, Wolfgang Miltz, Honnappa Srinivas, Carlos A Penno, Michael Kiffe

J Med Chem· March 2024

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Discovery of Amino Alcohols as Highly Potent, Selective, and Orally Efficacious Inhibitors of Leukotriene A4 Hydrolase.
Gebhard Thoma, Christian Markert, Rainer Lueoend, Wolfgang Miltz, Carsten Spanka, Michael Kiffe

J Med Chem· December 2023

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Efficacy and safety of MAS825 (anti-IL-1β/IL-18) in COVID-19 patients with pneumonia and impaired respiratory function.
Alex D Hakim, Mustafa Awili, Hollis R O'Neal, Omar Siddiqi, Naseem Jaffrani, Michael Kiffe

Clin Exp Immunol· October 2023

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Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
Robin A Fairhurst, Pascal Furet, Patricia Imbach-Weese, Frédéric Stauffer, Heinrich Rueeger, Michael Kiffe

J Med Chem· June 2022

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Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies.
Ying Huang, Martin Sendzik, Jeff Zhang, Zhenting Gao, Yongfeng Sun, Michael Kiffe

J Med Chem· April 2022

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Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.
Ramulu Poddutoori, Kimberly Aardalen, Kiran Aithal, Sanjeev Surendranath Barahagar, Charamanna Belliappa, Michael Kiffe

J Med Chem· March 2022

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Preclinical pharmacokinetics and metabolism of MAK683, a clinical stage selective oral embryonic ectoderm development (EED) inhibitor for cancer treatment.
Ji Yue Jeff Zhang, Jiangwei Zhang, Michael Kiffe, Markus Walles, Yi Jin

Xenobiotica· January 2022

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Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Robin A Fairhurst, Thomas Knoepfel, Nicole Buschmann, Catherine Leblanc, Robert Mah, Michael Kiffe

J Med Chem· November 2020

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FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer.
Andreas Weiss, Flavia Adler, Alexandra Buhles, Christelle Stamm, Robin A Fairhurst, Michael Kiffe

Mol Cancer Ther· December 2019

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New Potent DOT1L Inhibitors for Evaluation in Mouse.
Frédéric Stauffer, Andreas Weiss, Clemens Scheufler, Henrik Möbitz, Christian Ragot, Michael Kiffe

ACS Med Chem Lett· December 2019

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Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived -Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies.
Magdalena Koziczak-Holbro, Dean F Rigel, Bérengère Dumotier, David A Sykes, Jeffrey Tsao, Michael Kiffe

J Pharmacol Exp Ther· May 2019

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Targeted inhibition of the COP9 signalosome for treatment of cancer.
Anita Schlierf, Eva Altmann, Jean Quancard, Anne B Jefferson, René Assenberg, Michael Kiffe

Nat Commun· October 2016

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Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
Chao Chen, Hugh Zhu, Frédéric Stauffer, Giorgio Caravatti, Susanne Vollmer, Michael Kiffe

ACS Med Chem Lett· August 2016

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Fixing clearance as early as lead optimization using high throughput in vitro incubations in combination with exact mass detection and automatic structure elucidation of metabolites.
Alfred Zimmerlin, Michael Kiffe

Drug Discov Today Technol· April 2014

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Cytostar-T plates--a valid alternative for microplate scintillation counting of low radioactivity in combination with high-performance liquid chromatography in drug metabolism studies?
Michael Kiffe, Robert Nufer, Markus Trunzer, Daniel Graf

J Chromatogr A· July 2007

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Comparison of a two-dimensional liquid chromatography/mass spectrometry approach with a chip-based nanoelectrospray device for structural elucidation of metabolites in a human ADME study using a quadrupole time-of-flight mass spectrometer.
Markus Trunzer, Daniel Graf, Michael Kiffe

Rapid Commun Mass Spectrom· May 2007

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Two-dimensional liquid chromatography/mass spectrometry set-up for structural elucidation of metabolites in complex biological matrices.
Michael Kiffe, Daniel Graf, Markus Trunzer

Rapid Commun Mass Spectrom· May 2007

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Characterization of cytotoxic and genotoxic effects of different compounds in CHO K5 cells with the comet assay (single-cell gel electrophoresis assay).
Michael Kiffe, Peter Christen, Peter Arni

Mutat Res· June 2003

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Combination of high-performance liquid chromatography and microplate scintillation counting for crop and animal metabolism studies: a comparison with classical on-line and thin-layer chromatography radioactivity detection.
Michael Kiffe, Andrea Jehle, Robert Ruembeli

Anal Chem· February 2003

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SAR and pH stability of cyano-substituted epothilones.
Alicia Regueiro-Ren, Kenneth Leavitt, Soong-Hoon Kim, Gerhard Höfle, Michael Kiffe

Org Lett· October 2002

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N-Oxidation of Epothilone A-C and O-Acyl Rearrangement to C-19- and C-21-Substituted Epothilones.
Gerhard Höfle, Nicole Glaser, Michael Kiffe, Hans-Jürgen Hecht, Florenz Sasse

Angew Chem Int Ed Engl· July 1999

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