Marian Raschke

Quantitative Systems Toxicology Identifies Independent Mechanisms for Hepatotoxicity and Bilirubin Elevations Due to AKR1C3 Inhibitor BAY1128688

Antje Rottmann, Paul Brent Watkins, Esther Groettrup‐Wolfers, Christina Battista et autres

BAY1128688 is a selective inhibitor of AKR1C3, investigated recently in a trial that was prematurely terminated due to drug-induced liver injury. These unexpected observations prompted use of the quantitative systems toxicology model, DILIsym, to determine possible mechanisms of hepatotoxicity. Using mechanistic in …

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Predicting in vitro assays related to liver function using probabilistic machine learning

Flavio M. Morelli, Marian Raschke, Natalia A. Jungmann, Michaela Bairlein et autres

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Predicting Liver-Related In Vitro Endpoints with Machine Learning to Support Early Detection of Drug-Induced Liver Injury

Marina García de Lomana, Domenico Gadaleta, Marian Raschke, Robert E. Fricke et autres

Drug-induced liver injury (DILI) is a major cause of drug development failures and postmarket drug withdrawals, posing significant challenges to public health and pharmaceutical research. The biological mechanisms leading to DILI are highly complex and the adverse reaction is often difficult to …

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Biology-inspired dynamic microphysiological system approaches to revolutionize basic research, healthcare and animal welfare

Uwe Marx, Sonja Beken, Zaozao Chen, Eva‐Maria Dehne et autres

The regular t4 workshops on biology-inspired microphysiological systems (MPS) have become a reliable benchmark for assessing fundamental scientific, industrial, and regulatory trends in the MPS field. The 2023 workshop participants concluded that MPS technology as used in academia has matured significantly, as …

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Discovery of BAY-405: An Azaindole-Based MAP4K1 Inhibitor for the Enhancement of T-Cell Immunity against Cancer

Jeffrey Mowat, Rafael Carretero, Gabriele Leder, Núria Aiguabella Font et autres

High Resolution Image Download MS PowerPoint Slide Mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1) is a serine/threonine kinase that acts as an immune checkpoint downstream of T-cell receptor stimulation. MAP4K1 activity is enhanced by prostaglandin E2 (PGE2) and transforming growth factor …

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P01-39 Mitochondrial toxicity screening to support the R&D crop protection pipeline

Caroline Hilmi, Marian Raschke, Virginie Lempereur, Sven Geibel et autres

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P16-33: Identifying and characterizing toxicity liabilities of pharmaceuticals using ToxProfiler: A blinded case study with the ITLF consortium

Bas ter Braak, Liesanne Wolters, Kim Elbertse, Mario Beilmann et autres

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Quantitative Systems Toxicology Identifies Independent Mechanisms for Hepatotoxicity and Bilirubin Elevations Due to AKR1C3 Inhibitor BAY1128688

Christina Battista, Lisl K.M. Shoda, Paul Brent Watkins, Esther Groettrup‐Wolfers et autres

BAY1128688 is a selective inhibitor of AKR1C3, investigated recently in a trial that was prematurely terminated due to drug‐induced liver injury. These unexpected observations prompted use of the quantitative systems toxicology model, DILIsym, to determine possible mechanisms of hepatotoxicity. Using mechanistic in …

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New Generation of sGC Stimulators: Discovery of Imidazo[1,2-a]pyridine Carboxamide BAY 1165747 (BAY-747), a Long-Acting Soluble Guanylate Cyclase Stimulator for the Treatment of Resistant Hypertension

Alexandros Vakalopoulos, Frank Wunder, Ingo Volker Hartung, Gorden Redlich et autres

Herein, we describe the identification, chemical optimization, and preclinical characterization of novel soluble guanylate cyclase (sGC) stimulators. Given the very broad therapeutic opportunities for sGC stimulators, new tailored molecules for distinct indications with specific pharmacokinetics, tissue distribution, and physicochemical properties will be …

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Suppl. Figure 4 from Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity

Antje Margret Wengner, Gerhard Siemeister, Marcus Koppitz, Volker Schulze et autres

Effect of BAY 1217389 in monotherapy and combination therapy with paclitaxel on total KNL1 in A2780Cis tumors in nude mice

Supplementary Materials and Methods; Supplementary Tables 1-6; and Supplementary Figure Legends from Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity

Antje Margret Wengner, Gerhard Siemeister, Marcus Koppitz, Volker Schulze et autres

Additional data showing pharmacological characterization of Mps1 Inhibitors BAY 1161909 and BAY 1217389; Suppl. Table 1: Kinase selectivity profile of BAY 1161909; Suppl. Table 2: Kinase selectivity profile of BAY 1217389; Suppl. Table 3: Kinase selectivity profiles of BAY 1161909 compared to …

Suppl. Figure 1 from Novel Mps1 Kinase Inhibitors with Potent Antitumor Activity

Antje Margret Wengner, Gerhard Siemeister, Marcus Koppitz, Volker Schulze et autres

Multinuclearity in U2OS cells induced by Mps1 inhibition