Loop–loop interaction of HIV-1 TAR RNA with N3′ → P5′ deoxyphosphoramidate aptamers inhibits in vitro Tat-mediated transcription

• DOI: 10.1073/pnas.122247199
• Publication Date: 2002-07-28T22:26:28Z
• Authors: Fabien Darfeuille; Andrey Arzumanov; Sergei Gryaznov; Michael J. Gait; Carmelo Di Primo; Jean-Jacques Toulmé
• Keywords: Aptamer; Phosphoramidate; Transcription; Nuclease; SELEX Aptamer Technique

A hairpin RNA aptamer has been identified by in vitro selection against the transactivation-responsive element (TAR) of HIV-1. nuclease-resistant N3′ → P5′ phosphoramidate isosequential analog this also folds as a and forms with TAR loop–loop “kissing” complex binding constant low nanomolar range demonstrated electrophoretic mobility-shift assays surface plasmon resonance experiments. The key structural determinants, which contribute to stability aptamer–TAR complex, loop complementarity GA residues closing loop, remain crucial for complex. Moreover, specifically interferes peptide derived from transactivator protein (Tat) selectively inhibits Tat-mediated transcription an assay, marks relevant candidate experiments cells.