Structural basis of the activity of the microtubule-stabilizing agent epothilone a studied by NMR spectroscopy in solution

• Authors: REESE Marcel; SANCHEZ-PEDREGAL Victor M; KUBÍČEK Karel; MEILER Jens; BLOMMERS Marcel J; GRIESINGER Christian; CARLOMAGNO Teresa
• Year of publication: 2007
• Type: Article in Periodical
• Magazine / Source: Angewandte Chemie International Edition
• MU Faculty or unit: Faculty of Science
• web: http://www3.interscience.wiley.com/cgi-bin/abstract/114109930/ABSTRACT
• Field: Biophysics
• Keywords: epothilones; NMR spectroscopy; structure elucidation; structure-activity relationships; tubulins
• Description: Fits in a pocket: The binding mode of epothilone A (EpoA) to tubulin is determined by NMR spectroscopy in aqueous solution. The results explain the existing structure-activity relationship data for epothilones with both native and mutant tubulins, and support the existence of a common pharmacophore for EpoA and paclitaxel.