Cell‐Penetrating, Dimeric α‐Helical Peptides: Nanomolar Inhibitors of HIV‐1 Transcription1. (23rd July 2014)

• Record Type: Journal Article
• Authors: Jang, Sangmok; Hyun, Soonsil; Kim, Seoyeon; Lee, Seonju; Lee, Im‐Soon; Baba, Masanori; Lee, Yan; Yu, Jaehoon
• Is Part Of: Angewandte Chemie. Volume 126:Number 38(2014)
• Page Start: 10250
• Page End: 10253
• Publication Date: 2014-07-23
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1002/ange.201404684
• Languages: English
• ISSNs: 0044-8249

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>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.</p> </abstract>