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A Highly Potent and Cellularly Active β‐Peptidic Inhibitor of the p53/hDM2 Interaction |
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| Authors: | Martin Hintersteiner Dr. Thierry Kimmerlin Dr. Geraldine Garavel Dr. Thorsten Schindler Dr. Roman Bauer Dr. Nicole‐Claudia Meisner Dr. Jan‐Marcus Seifert Dr. Volker Uhl Dr. Manfred Auer Prof. Dr. |
| Affiliation: | 1. The University of Edinburgh, Centre for Translational and Chemical Biology, Michael Swann Building, 3.34, The King's Buildings, Mayfield Road, Edinburgh, EH9 3JR (UK);2. Affiliation when work was performed: Innovative Screening Technologies Unit, Novartis Institutes for BioMedical Research (NIBR), Brunnerstrasse 59, 1235 Vienna (Austria) |
| Abstract: | New and improved : The incorporation of a 6‐chlorotryptophan (6‐Cl‐Trp) into a β‐peptide (M)‐314 helix leads to a high‐affinity hDM2 inhibitor, as demonstrated by fluorescence fluctuation analysis at single molecule resolution. When conjugated to penetratin, the newly derived hDM2 binder specifically inhibits tumour cell growth in vitro.  |
| Keywords: | antitumor agents beta‐peptides hDM2 inhibitors p53 protein– protein interactions |