Marc A. Grundl
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View article: Insights into the Identification of iPSC- and Monocyte-Derived Macrophage-Polarizing Compounds by AI-Fueled Cell Painting Analysis Tools
Insights into the Identification of iPSC- and Monocyte-Derived Macrophage-Polarizing Compounds by AI-Fueled Cell Painting Analysis Tools Open
Macrophage polarization critically contributes to a multitude of human pathologies. Hence, modulating macrophage polarization is a promising approach with enormous therapeutic potential. Macrophages are characterized by a remarkable functi…
View article: Interleukin‐1 receptor‐associated kinase 4 (IRAK4) is a critical regulator of inflammatory signalling through toll‐like receptors 4 and 7/8 in murine and human lungs
Interleukin‐1 receptor‐associated kinase 4 (IRAK4) is a critical regulator of inflammatory signalling through toll‐like receptors 4 and 7/8 in murine and human lungs Open
Background and Purpose Toll‐like receptors 4 (TLR4) and TLR7/TLR8 play an important role in mediating the inflammatory effects of bacterial and viral pathogens. Interleukin‐1 receptor‐associated kinase 4 (IRAK4) is an important regulator o…
View article: IRAK4 is a critical regulator of inflammatory signalling through Toll like receptors (TLR) 4 and 7/8 in murine and human lungs
IRAK4 is a critical regulator of inflammatory signalling through Toll like receptors (TLR) 4 and 7/8 in murine and human lungs Open
Background and purpose: Toll like receptors (TLR) 4 and 7/8 play an important role in mediating the inflammatory effects of bacterial and viral pathogens. IRAK4 is an important regulator of TLR signalling, and hence is a potential therapeu…
View article: Molecular basis of TASL recruitment by the peptide/histidine transporter 1, PHT1
Molecular basis of TASL recruitment by the peptide/histidine transporter 1, PHT1 Open
PHT1 is a histidine /oligopeptide transporter with an essential role in Toll-like receptor innate immune responses. It can act as a receptor by recruiting the adaptor protein TASL which leads to type I interferon production via IRF5. Persi…
View article: BI 1291583: a novel selective inhibitor of cathepsin C with superior in vivo profile for the treatment of bronchiectasis
BI 1291583: a novel selective inhibitor of cathepsin C with superior in vivo profile for the treatment of bronchiectasis Open
Background Airway inflammation in chronic inflammatory lung diseases (e.g. bronchiectasis) is partly mediated by neutrophil-derived serine protease (NSP)/antiprotease imbalance. NSPs are activated during neutrophil myelopoiesis in bone mar…
View article: Molecular basis of TASL recruitment by PHT1
Molecular basis of TASL recruitment by PHT1 Open
PHT1 is a histidine /oligopeptide transporter with an essential role in Toll-like receptor innate immune response. It can act as a receptor by recruiting the adaptor protein TASL which leads to type I interferon production via IRF5. Persis…
View article: BIreactive: Expanding the Scope of Reactivity Predictions to Propynamides
BIreactive: Expanding the Scope of Reactivity Predictions to Propynamides Open
We present the first comprehensive study on the prediction of reactivity for propynamides. Covalent inhibitors like propynamides often show improved potency, selectivity, and unique pharmacologic properties compared to their non-covalent c…
View article: Allosteric Activation of Striatal-Enriched Protein Tyrosine Phosphatase (STEP, PTPN5) by a Fragment-like Molecule
Allosteric Activation of Striatal-Enriched Protein Tyrosine Phosphatase (STEP, PTPN5) by a Fragment-like Molecule Open
Protein tyrosine phosphatase non-receptor type 5 (PTPN5, STEP) is a brain specific phosphatase that regulates synaptic function and plasticity by modulation of N-methyl-d-aspartate receptor (NMDAR) and α-amino-3-hydroxy-5-methyl-4-isoxazol…