Using a β-Hairpin To Mimic an α-Helix: Cyclic Peptidomimetic Inhibitors of the p53-HDM2 Protein-Protein Interaction

Inhibition of crucial protein–protein interactions, for example, between the p53 tumor suppressor (red in structure) and HDM2, a protein overexpressed in tumor cells, is possible with peptidomimetics having a β‐hairpin structure (yellow) mimicking the α‐helical protein epitope. These mimetics might...

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Veröffentlicht in:Angewandte Chemie International Edition 2004-04, Vol.43 (16), p.2109-2112
Hauptverfasser: Fasan, Rudi, Dias, Ricardo L. A., Moehle, Kerstin, Zerbe, Oliver, Vrijbloed, Jan W., Obrecht, Daniel, Robinson, John A.
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Sprache:eng
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Zusammenfassung:Inhibition of crucial protein–protein interactions, for example, between the p53 tumor suppressor (red in structure) and HDM2, a protein overexpressed in tumor cells, is possible with peptidomimetics having a β‐hairpin structure (yellow) mimicking the α‐helical protein epitope. These mimetics might be of direct value in the search for novel agents with tumor‐suppressor activity.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200353242