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Overcoming EGFRG724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors
The emergence of acquired resistance against targeted drugs remains a major clinical challenge in lung adenocarcinoma patients. In a subgroup of these patients we identified an association between selection of EGFRT790M-negative but EGFRG724S-positive subclones and osimertinib resistance. We demonstrate that EGFRG724S limits the activity of third-generation EGFR inhibitors both in vitro and in vivo. Structural analyses and computational modeling indicate that...
TU Dortmund schlägt neues Kapitel in der Erfolgsgeschichte der Wirkstoffforschung auf
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). …
Read more … TU Dortmund schlägt neues Kapitel in der Erfolgsgeschichte der Wirkstoffforschung auf
RASPELD to Perform High‐End Screening in an Academic Environment toward the Development of Cancer Therapeutics
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. ...