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Using a β‐Hairpin To Mimic an α‐Helix: Cyclic Peptidomimetic Inhibitors of the p53–HDM2 Protein–Protein Interaction
Author(s) -
Fasan Rudi,
Dias Ricardo L. A.,
Moehle Kerstin,
Zerbe Oliver,
Vrijbloed Jan W.,
Obrecht Daniel,
Robinson John A.
Publication year - 2004
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.200353242
Subject(s) - peptidomimetic , suppressor , chemistry , protein structure , epitope , protein–protein interaction , helix (gastropod) , biophysics , biochemistry , microbiology and biotechnology , computational biology , stereochemistry , biology , peptide , genetics , antibody , gene , ecology , snail
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.