Front Cover: Getting a Grip on the Undrugged: Targeting β‐Catenin with Fragment‐Based Methods (9/2021)

The Front Cover shows the discovered fragment in the process of binding to β‐catenin bound to the transcription factor TCF4 and co‐activator BCL9 (PDB ID: 2GL7). The electron density surrounding the ligand and the chemical shift perturbations observed in the fragment binding site represent the stron...

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Veröffentlicht in:ChemMedChem 2021-05, Vol.16 (9), p.1335-1335
Hauptverfasser: Kessler, Dirk, Mayer, Moriz, Zahn, Stephan K., Zeeb, Markus, Wöhrle, Simon, Bergner, Andreas, Bruchhaus, Jens, Ciftci, Tuncay, Dahmann, Georg, Dettling, Maike, Döbel, Sandra, Fuchs, Julian E., Geist, Leonhard, Hela, Wolfgang, Kofink, Christiane, Kousek, Roland, Moser, Franziska, Puchner, Teresa, Rumpel, Klaus, Scharnweber, Maximilian, Werni, Patrick, Wolkerstorfer, Bernhard, Breitsprecher, Dennis, Baaske, Philipp, Pearson, Mark, McConnell, Darryl B., Böttcher, Jark
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Sprache:eng
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Zusammenfassung:The Front Cover shows the discovered fragment in the process of binding to β‐catenin bound to the transcription factor TCF4 and co‐activator BCL9 (PDB ID: 2GL7). The electron density surrounding the ligand and the chemical shift perturbations observed in the fragment binding site represent the strong biophysical validation. The outreaching arm represents the prospective utility of this discovery to be used as a handle for proteolysis targeting chimeras (PROTACs) upon further optimization. More information can be found in the Communication by Dirk Kessler, Jark Böttcher et al. Cover art created by Mila Böttcher, Jark Böttcher, and Darryl B. McConnell.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.202100271