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Back Cover: Bicyclic β‐Sheet Mimetics that Target the Transcriptional Coactivator β‐Catenin and Inhibit Wnt Signaling (Angew. Chem. Int. Ed. 25/2021)
Author(s) -
Wendt Mathias,
Bellavita Rosa,
Gerber Alan,
Efrém NinaLouisa,
Ramshorst Thirza,
Pearce Nicholas M.,
Davey Paul R. J.,
Everard Isabel,
VazquezChantada Mercedes,
Chiarparin Elisabetta,
Grieco Paolo,
Hennig Sven,
Grossmann Tom N.
Publication year - 2021
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.202104892
Subject(s) - bicyclic molecule , coactivator , wnt signaling pathway , peptidomimetic , chemistry , subfamily , stereochemistry , microbiology and biotechnology , computational biology , biochemistry , biology , signal transduction , transcription factor , peptide , gene
Bicyclic peptidomimetics bind the transcriptional coactivator β‐catenin. A structure‐based design strategy has been applied to minimize a 52 amino acid binding motif into bicyclic 16‐mer β‐sheet mimetics. The biologically most active mimetic exhibits robust cellular uptake and inhibits Wnt signaling in a cell‐based assay, as reported by Tom N. Grossmann and co‐workers in their Research Article on page 13937.