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Front Cover: Getting a Grip on the Undrugged: Targeting β‐Catenin with Fragment‐Based Methods (9/2021)
Author(s) -
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
Publication year - 2021
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202100271
Subject(s) - front cover , protein data bank (rcsb pdb) , fragment (logic) , transcription factor , catenin , cover (algebra) , transcription (linguistics) , chemistry , computational biology , biology , stereochemistry , computer science , biochemistry , algorithm , signal transduction , philosophy , gene , engineering , mechanical engineering , wnt signaling pathway , linguistics
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.