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New Platform for Target-to-Hit: From Fragment Screen to Structure-based Drug Discovery

Modern Structure-based Drug Discovery (SBDD) is a core component of the Target-to-Hit platform at WuXi AppTec HitS. A tailored screening approach is preferred, employing a potential combination of fragment or DNA-encoded library screening. X-ray crystallography is also an important tool for target identification and validation, target evaluation (ligandability/druggability assessment), hit identification (e.g. fragment screening), and acceleration of the latter medicinal chemistry hit-to-lead process. NMR and Cryo-EM allow for structure determination of the samples that are unamenable to crystallization. Closely interwoven with a state-of-the art biophysical platform (as illustrated by a case study employing STING), SBDD enables shorter timelines for target-to-hit and hit-to-lead campaigns.

Who should attend
  • Academics interested in fragment screening, structure-based drug discovery and biophysics.
  • Industry scientist interested in expanding the tool box of target-to-hit processes.
What will be learned
  • Advantages and limitations of fragment-based and structure-based drug discovery
  • The importance of protein quality and protein construct for the successful screening campaigns
  • Advantages and limitations of biophysical approaches (e.g., SPR, MST, TRIC/Dianthus, nanoDSF, ITC).
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Nuska Tschammer

Nuska Tschammer

Head of DEL Lab Operations, WuXi AppTec HitS/Crelux

Dr. habil. Nuska Tschammer is Head of DEL Lab Operations at WuXi AppTecĀ“s HitS/Crelux in Munich, Germany. Prior to this role, she was Subject Matter Expert at Crelux. Before that she was Head of Research and Development Biochemistry at NanoTemper Technologies, where she developed new generation of dyes for the MicroScale Thermophoresis (MST) and Dianthus (TRIC). During the habilitation in Medicinal Chemistry at Friedrich-Alexander University, Erlangen, Germany, her research on the allosteric modulation of GPRCs was funded by several grants of German Research Foundation (DFG), which led to many publications and patents. She received various prizes and awards, among them Innovation Award in Medicinal Chemistry, which is jointly awarded by Society of German Chemists (GDCh) and German Pharmaceutical Society (DPhG).

Arsalan Arif

arsalan arif

Founder & Publisher, Endpoints News

Arsalan Arif is a news media entrepreneur who set out in 2015 to build his vision of an independent biotech news company at Endpoints News.