NMR structures of Thiostrepton derivatives report target shape recognition

TitleNMR structures of Thiostrepton derivatives report target shape recognition
Publication TypeJournal Article
Year of Publication2011
AuthorsJonker HRA, Baumann S, Wolf A, Schoof S, Hiller F, Schulte KW, Kirschner KN, Schwalbe H, Arndt H-D
JournalAngew. Chem. Intl. Ed. Engl.
Volume50
Pagination3308-3312
Abstract

Structural probing: The activity of thiostrepton and derivatives with targeted shape changes was determined at their ribosomal binding site by using semisynthesis, NMR structure determination, docking (see picture), and biological evaluation in an integrated fashion. This combination revealed important elements of molecular recognition within the embedded pharmocophore of the target, a composite RNA–protein complex.
URLhttp://onlinelibrary.wiley.com/doi/10.1002/anie.201003582/pdf
DOI10.1002/anie.201003582