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The Ser/Thr Kinase Akt (Protein Kinase B/PKB) is a master switch in cellular signal transduction pathways. Ist downstream signaling influences cell proliferation, cell growth, and apoptosis, rendering Akt a prominent drug target. The unique activation mechanism of Akt involves a change of the relative orientation of its N-terminal pleckstrin homology (PH) and the kinase domain and makes this kinase suitable for highly specific allosteric modulation. Here we present...

Thirty researchers of the DDHD consortium gathered at TU Dortmund University to enjoy an afternoon of excellent science and fruitful discussions.

Universität eröffnet mit sieben Partnern Drug Discovery Hub Dortmund

Ein neues Kapitel in der außergewöhnlichen Erfolgsgeschichte der Dortmunder Wirkstoffforschung hat die TU Dortmund am Montag, 17. September, aufgeschlagen: In einer Feierstunde eröffneten Prof. Daniel Rauh, Koordinator des DDHD und Professor für Chemische Biologie und Medizinische Chemie an der TU Dortmund und Prof. Ursula Gather, Rektorin der TU Dortmund, den Drug Discovery Hub Dortmund (DDHD). ...

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. ...