Modern medicinal chemistry requires strategies that accelerate the discovery of chemical probes from initial ligand identification to advanced pharmacological modalities. Using conformationally constrained adenosine mimetics, we identified ligands for the Mac1 macro domain of MERS-CoV and, through structure-guided optimization and virtual screening, developed distinct inhibitor series with submicromolar potency. Complementing these approaches, we established a miniaturized direct-to-biology (D2B) platform based on copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC), enabling parallel synthesis and biological evaluation without prior purification. Initially applied to PROTAC discovery, this modular click-chemistry approach provides opportunities for rapid chemical-space exploration across different modalities, including targeted protein degraders and inhibitors.
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Professor Dr. Alexandra K. Kiemer
Vorsitzende der DPhG Landesgruppe Saar
Kontakt: pharm.bio.kiemer@uni-saarland.de
