Marion Kamke

Discovery of NP3-253, a Potent Brain Penetrant Inhibitor of the NLRP3 Inflammasome

Angela Mackay, Juraj Velcicky, Nina Gommermann, Henri Mattes et autres

Activation of the NLRP3 inflammasome in response to danger signals is a key innate immune mechanism and results in the production of the pro-inflammatory cytokines interleukin-1β (IL-1β) and interleukin-18 (IL-18) as well as pyroptotic cell death. Aberrant NLRP3 activation has been linked …

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Evaluation of protein kinase D auto-phosphorylation as biomarker for NLRP3 inflammasome activation

Diane Heiser, Joëlle Rubert, Adeline Unterreiner, Claudine Maurer et autres

BACKGROUND: The NLRP3 inflammasome is a critical component of sterile inflammation, which is involved in many diseases. However, there is currently no known proximal biomarker for measuring NLRP3 activation in pathological conditions. Protein kinase D (PKD) has emerged as an important NLRP3 …

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Evaluation of protein kinase D auto-phosphorylation as biomarker for NLRP3 inflammasome activation

Diane Heiser, Joëlle Rubert, Adeline Unterreiner, Claudine Maurer et autres

Abstract Background The NLRP3 inflammasome is a critical component of sterile inflammation, which is involved in many diseases. However, there is currently no known proximal biomarker for measuring NLRP3 activation in pathological conditions. Protein kinase D (PKD) has emerged as an important …

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Identification of SPPL2a Inhibitors by Multiparametric Analysis of a High-Content Ultra-High-Throughput Screen

Xian Zhang, Marjo Götte, Yvonne Ibig-Rehm, Ansgar Schuffenhauer et autres

The intramembrane protease signal peptide peptidase-like 2a (SPPL2a) is a potential drug target for the treatment of autoimmune diseases due to an essential role in B cells and dendritic cells. To screen a library of 1.4 million compounds for inhibitors of SPPL2a, …

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Multiparametric analysis of a high-content ultra-high-throughput screen identifies inhibitors of the intramembrane protease SPPL2a

Xian Zhang, Marjo Goette, Yvonne Ibig-Rehm, Marion Kamke et autres

The intramembrane protease SPPL2a (signal peptide peptidase-like 2a) is a potential drug target for the treatment of autoimmune diseases due to its essential role in B cells and dendritic cells. To screen a library of 1.4 million compounds for inhibitors of SPPL2a, …

A macrocyclic HCV NS3/4A protease inhibitor interacts with protease and helicase residues in the complex with its full-length target

Nikolaus Schiering, Allan D'Arcy, Frédéric Villard, Oliver Simić et autres

Hepatitis C virus (HCV) infection is a global health burden with over 170 million people infected worldwide. In a significant portion of patients chronic hepatitis C infection leads to serious liver diseases, including fibrosis, cirrhosis, and hepatocellular carcinoma. The HCV NS3 protein …

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