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Design of β‐Hairpin Peptidomimetics That Inhibit Binding of α‐Helical HIV‐1 Rev Protein to the Rev Response Element RNA
Author(s) -
Moehle Kerstin,
Athanassiou Zafiria,
Patora Krystyna,
Davidson Amy,
Varani Gabriele,
Robinson John A.
Publication year - 2007
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.200702801
Subject(s) - peptidomimetic , chemistry , library science , human immunodeficiency virus (hiv) , stereochemistry , medicine , biochemistry , computer science , family medicine , peptide
Bound to please : Binding of the Rev protein to HIV‐1 RRE RNA is essential for virus replication. A strategy for the discovery of Rev‐RRE inhibitors, based on the use of protein epitope mimetics, is described. Template‐bound β‐hairpin peptidomimetics (see picture, orange) are designed that mimic the Rev helical epitope (green). The mimetics bind with high affinity and selectivity to the target RNA, and have potential for development into novel anti‐viral drugs.