NMR-Based Characterization of Phenothiazines as a RNA Binding Scaffold

• Published in: Journal of the American Chemical Society Vol. 126; no. 13; pp. 4453 - 4460
• Main Authors: Mayer, Moriz, James, Thomas L
• Format: Journal Article
• Language: English
• Published: Washington, DC American Chemical Society 07.04.2004
• Subjects: Binding Sites; Biological and medical sciences; General pharmacology; HIV-1 - metabolism; Human immunodeficiency virus 1; Humans; Ligands; Magnetic Resonance Spectroscopy; Medical sciences; Nuclear Matrix - metabolism; Pharmacology. Drug treatments; Phenothiazines - chemistry; Phenothiazines - metabolism; Physicochemical properties. Structure-activity relationships; RNA - chemistry; RNA - metabolism; Sulfur nitrogen heterocycle; RNA; Neuroleptic; Psychotropic; Homonuclear correlation; Molecular interaction; Phenothiazine derivatives; Binding site; NMR spectrometry; Tricyclic compound; Two dimension spectrometry; Binding capacity; Structure activity relation; Aromatic compound

Phenothiazines were identified by virtual screening as promising ligands for HIV-1 TAR RNA and A-site ribosomal RNA, and binding in each case was verified experimentally. Consequently, since phenothiazines generally possess high bioavailability and low toxicity, we used several NMR techniques to exp...