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Cell‐Penetrating, Dimeric α‐Helical Peptides: Nanomolar Inhibitors of HIV‐1 Transcription
Author(s) -
Jang Sangmok,
Hyun Soonsil,
Kim Seoyeon,
Lee Seonju,
Lee ImSoon,
Baba Masanori,
Lee Yan,
Yu Jaehoon
Publication year - 2014
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201404684
Subject(s) - dimer , peptide , chemistry , biophysics , transcription (linguistics) , penetration (warfare) , cell , human immunodeficiency virus (hiv) , biochemistry , stereochemistry , biology , virology , linguistics , philosophy , organic chemistry , operations research , engineering
We constructed dimeric α‐helical peptide bundles based on leucine (L) and lysine (K) residues for both efficient cell penetration and inhibition of the Tat–TAR interaction. The LK dimers can penetrate nearly quantitatively into eukaryotic cells and effectively inhibit the elongation of the TAR transcript at low nanomolar concentrations. The effective inhibition of HIV‐1 replication strongly suggests that the LK dimer has strong potential as an anti‐HIV‐1 drug.