Sandra Koska
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View article: Identification of Natural Killer Cell Enhancers Through Mimicking of the Tumor Microenvironment
Identification of Natural Killer Cell Enhancers Through Mimicking of the Tumor Microenvironment Open
The tumor microenvironment (TME) is a pro‐cancerous niche harboring immunosuppressive factors that are secreted by cancer cells and the surrounding cancer‐supportive tissue, such as kynurenine, prostaglandin E2 and transforming growth fact…
View article: Alternating binding and p97-mediated dissociation of SDS22 and I3 recycles active PP1 between holophosphatases
Alternating binding and p97-mediated dissociation of SDS22 and I3 recycles active PP1 between holophosphatases Open
Protein phosphatase-1 catalytic subunit (PP1) joins diverse targeting subunits to form holophosphatases that regulate many cellular processes. Newly synthesized PP1 is known to be transiently sequestered in an inhibitory complex with Suppr…
View article: Detection of a Mitochondrial Fragmentation and Integrated Stress Response Using the Cell Painting Assay
Detection of a Mitochondrial Fragmentation and Integrated Stress Response Using the Cell Painting Assay Open
Mitochondria are cellular powerhouses and are crucial for cell function. However, they are vulnerable to internal and external perturbagens that may impair mitochondrial function and eventually lead to cell death. In particular, small mole…
View article: Illuminating Dark Chemical Matter Using the Cell Painting Assay
Illuminating Dark Chemical Matter Using the Cell Painting Assay Open
Screening for small-molecule modulators of disease-relevant targets and phenotypes is the first step on the way to new drugs. Large compound libraries have been synthesized by academia and, particularly, pharmaceutical companies to meet th…
View article: Detection of a Mitochondrial Stress Phenotype using the Cell Painting Assay
Detection of a Mitochondrial Stress Phenotype using the Cell Painting Assay Open
Mitochondria are cellular powerhouses and crucial for cell function. However, these organelles are vulnerable to internal and external perturbagens that may impair mitochondrial function and eventually lead to cell death. In particular, sm…
View article: Inducin Triggers LC3‐Lipidation and ESCRT‐Mediated Lysosomal Membrane Repair
Inducin Triggers LC3‐Lipidation and ESCRT‐Mediated Lysosomal Membrane Repair Open
Lipidation of the LC3 protein has frequently been employed as a marker of autophagy. However, LC3‐lipidation is also triggered by stimuli not related to canonical autophagy. Therefore, characterization of the driving parameters for LC3 lip…
View article: Synthetic Matching of Complex Monoterpene Indole Alkaloid Chemical Space
Synthetic Matching of Complex Monoterpene Indole Alkaloid Chemical Space Open
Monoterpene indole alkaloids (MIAs) are endowed with high structural and spatial complexity and characterized by diverse biological activities. Given this complexity‐activity combination in MIAs, rapid and efficient access to chemical matt…
View article: Illuminating Dark Chemical Matter using the Cell Painting Assay
Illuminating Dark Chemical Matter using the Cell Painting Assay Open
The identification of bioactive small molecules is at the heart of chemical biology and medicinal research. The screening for modulators of disease-relevant targets and phenotypes is the first step on the way to new drugs. Therefore, large…
View article: Addressing the Osimertinib Resistance Mutation EGFR-L858R/C797S with Reversible Aminopyrimidines
Addressing the Osimertinib Resistance Mutation EGFR-L858R/C797S with Reversible Aminopyrimidines Open
Drug resistance mutations emerging during the treatment of non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) inhibitors represent a major challenge in personalized cancer treatment and require constant develop…
View article: Targeting oncogenic KRasG13C with nucleotide-based covalent inhibitors
Targeting oncogenic KRasG13C with nucleotide-based covalent inhibitors Open
Mutations within Ras proteins represent major drivers in human cancer. In this study, we report the structure-based design, synthesis, as well as biochemical and cellular evaluation of nucleotide-based covalent inhibitors for KRasG13C, an …
View article: Targeting oncogenic KRasG13C with nucleotide-based covalent inhibitors
Targeting oncogenic KRasG13C with nucleotide-based covalent inhibitors Open
Mutations within Ras proteins represent major drivers in human cancer. In this study, we report the structure-based design, synthesis, as well as biochemical and cellular evaluation of nucleotide-based covalent inhibitors for KRasG13C, an …