Article
Structure Based Design of Bicyclic Peptide Inhibitors of RbAp48.
Angewandte Chemie (International ed. in English) - 25 Jan 2021
Hart Peter 't, Hommen Pascal, Noisier Anaïs, Krzyzanowski Adrian, Schüler Darijan, Porfetye Arthur T, Akbarzadeh Mohammad, Vetter Ingrid R, Adihou Hélène, Waldmann Herbert
Abstract excerpt
The scaffolding protein RbAp48 is part of several epigenetic regulation complexes and is overexpressed in a variety of cancers. In order to develop tool compounds for the study of RbAp48 function, we have developed peptide inhibitors targeting the protein-protein interaction interface between RbAp48 and the scaffold protein MTA1. Based on a MTA1-derived linear peptide with low micromolar affinity and informed by...
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