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Structure‐Based Design of an RNA‐Binding p ‐Terphenylene Scaffold that Inhibits HIV‐1 Rev Protein Function
Author(s) -
GonzálezBulnes Luis,
Ibáñez Ignacio,
Bedoya Luis M.,
Beltrán Manuela,
Catalán Silvia,
Alcamí José,
Fustero Santos,
Gallego José
Publication year - 2013
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.201306665
Subject(s) - scaffold , scaffold protein , function (biology) , microbiology and biotechnology , rna , rna binding protein , chemistry , computational biology , human immunodeficiency virus (hiv) , computer science , biology , virology , biochemistry , signal transduction , programming language , gene
Rev(ersing) RNA binding : RNA‐binding inhibitors based on a bilaterally substituted p ‐terphenylene scaffold (green) project their substituents in a broad spatial angle and reproduce the interactions of a protein α‐helix (red) embedded in its RNA receptor. These terphenyls can mimic one α‐helix of the HIV‐1 protein Rev and inhibit Rev function and HIV‐1 replication in cells. This scaffold may open new avenues for targeting nucleic acids with small molecules.