title: Cell-penetrating, dimeric α-helical peptides: nanomolar inhibitors of HIV-1 transcription.
abstract: 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.
authors: Department of Chemistry, Seoul National University, Seoul 151-742 (Korea).
authors: Sangmok
authors: S
authors: Jang
authors: Soonsil
authors: S
authors: Hyun
authors: Seoyeon
authors: S
authors: Kim
authors: Seonju
authors: S
authors: Lee
authors: Im-Soon
authors: IS
authors: Lee
authors: Masanori
authors: M
authors: Baba
authors: Yan
authors: Y
authors: Lee
authors: Jaehoon
authors: J
authors: Yu
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D019281:Dimerization; D004305:Dose-Response Relationship, Drug; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics*; D006367:HeLa Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D010455:Peptides / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D017433:Protein Structure, Secondary; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000187:drug effects / Q000378:metabolism* / Q000821:virology*; D014158:Transcription, Genetic / Q000187:drug effects*; D014779:Virus Replication / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D010455:Peptides
keywords: HIV-1; antiviral agents; drug design; peptides; transcriptional inhibition