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The identification of compounds for dissecting biological functions and the development of novel drug molecules are central tasks that often require screening campaigns. However, the required architecture is cost‐ and time‐intensive. Herein we describe the devices and technologies that comprise a Robotics‐Assisted Screening Platform for Efficient Ligand Discovery (RASPELD), which we set up in an academic laboratory. RASPELD provides semi‐automated high‐end screening, and it can be maintained by graduate students. ...

Transcription factors (TFs) constitute a diverse class of sequence-specific DNA-binding proteins, which are key to the modulation of gene expression. TFs have been associated with human diseases, including cancer, Alzheimer's and other neurodegenerative diseases, which makes this class of proteins attractive targets for chemical biology and medicinal chemistry research. ...

PIK‐75 is a phosphoinositide‐3‐kinase (PI3K) α‐isoform‐selective inhibitor with high potency. Although published structure–activity relationship data show the importance of the NO2 and the Br substituents in PIK‐75, none of the published studies could correctly determine the underlying reason for their importance. In this publication, we report the first X‐ray crystal structure of PIK‐75 in complex with the kinase GSK‐3β. ...

European Workshop in Drug Synthesis in Siena, Italy

Our promising PhD student Lisa Goebel won the Best Poster Award at the European Workshop in Drug Synthesis in Siena, Italy http://www.ewdsy.it/index.php . Congratulations!

The Molecular Basis of Kinase-Targeted Therapies and Drug Resistance in Non-Small Cell Lung Cancer

Jonas Lategahn, Marina Keul, and Daniel Rauh

The treatment of non-small cell lung cancer (NSCLC) is currently experiencing a revolution. Over the last decade, the Knowledge gained about the biochemical features of biomarkers and their predictive abilities has led to the development of targeted small-molecule Inhibitors that present an alternative to harsh chemotherapy. ...