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Updated: May 20, 2025

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
Published on: May 15, 2019
Design and synthesis of a clickable cell-permeable pseudopeptide Pin1 inhibitor with antiproliferative effects on
Lorenzo Meneghelli1,2, Stephanie Davidson3, Anthony Gineste1,2
1BioCIS, UMR 8076, CY Cergy Paris Université, CNRS, 95000 Cergy Pontoise, France. chiara.zanato@cyu.fr.
Abstract:
The synthesis of a library of minimal-backbone, cell-permeable, clickable pseudopeptide Pin1 ligands with potential applications in drug development and biochemical studies is reported. The ligands' affinity constants were evaluated using NMR. The lead compound 4b, demonstrated effective cell permeability, inhibitory activity, and an antiproliferative effect on a multiple myeloma cell line.
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