The BSF helped to develop a screen of a macrocyclic compound library
© 2022 EPFL
The Biomolecular Screening Facility (BSF) helped to develop a high-speed miniaturized screen of a macrocyclic compound library.
As a part of a long-lasting collaboration with the group of Professor Christian Heinis at EPFL’s School of Basic Sciences, the BSF team helped to develop a new approach for efficient screening of a large and customized collection of macrocycles. The BSF team provided expertise and instruments for miniaturization and automatization of synthesis validation and screening of libraries of macrocycles. This allowed preparation and screening of a combinatorial customized macrocyclic compound library leading to the identification of thrombin and MDM2:p53 protein-protein interaction-inhibiting macrocycles.
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Sevan Habeshian, Manuel Leonardo Merz, Gontran Sangouard, Ganesh Kumar Mothukuri, Mischa Schüttel, Zsolt Bognar, Cristina Díaz-Perlas, Jonathan Vesin, Julien Bortoli Chapalay, Gerardo Turcatti, Laura Cendron, Alessandro Angelini, Christian Heinis. Synthesis and direct assay of large macrocycle diversities by combinatorial late-stage modification at picomole scale. Nature Communications 13, Article number: 3823 (02 July 2022).
DOI: 10.1038/s41467-022-31428-8