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Journal/Book: Angew. Chem. Intl. Ed. Engl.
Published: 2011
Pages: 3308-3312
Volume: 50
Issue:
Accession no.:
Publisher:
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NMR structures of Thiostrepton derivatives report target shape recognition

Hendrik R A Jonker, Sascha Baumann, Antje Wolf, Sebastian Schoof, Fabian Hiller, Kathrin W. Schulte, Karl N. Kirschner, Harald Schwalbe, Hans-Dieter Arndt
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.
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Prof. Dr. Harald Schwalbe
Institut für Organische Chemie und Chemische Biologie
Johann Wolfgang Goethe Universität
Max-von-Laue-Str. 7
D-60438 Frankfurt am Main
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