Communication

The Absolute Configuration of Rhizopodin and Its Inhibition of Actin Polymerization by Dimerization†

  1. Gregor Hagelueken1,
  2. Simone C. Albrecht1,
  3. Heinrich Steinmetz Dipl.-Chem.3,
  4. Rolf Jansen Dr.3,
  5. Dirk W. Heinz Prof.2,
  6. Markus Kalesse Prof.3,
  7. Wolf-Dieter Schubert Dr.1

Article first published online: 26 NOV 2008

DOI: 10.1002/anie.200802915

Issue

Angewandte Chemie International Edition

Angewandte Chemie International Edition

Volume 48, Issue 3, pages 595–598, January 5, 2009

Additional Information

How to Cite

Hagelueken, G., Albrecht, Simone C., Steinmetz, H., Jansen, R., Heinz, Dirk W., Kalesse, M. and Schubert, W.-D. (2009), The Absolute Configuration of Rhizopodin and Its Inhibition of Actin Polymerization by Dimerization. Angew. Chem. Int. Ed., 48: 595–598. doi: 10.1002/anie.200802915

Author Information

  1. 1

    Research Group Molecular Host–Pathogen Interactions, Helmholtz-Centre for Infection Research, Inhoffenstrasse 7, 38124 Braunschweig (Germany), Fax: (+49) 531-6181-7099

  2. 2

    Division of Structural Biology, Helmholtz-Centre for Infection Research, Braunschweig (Germany)

  3. 3

    Departments of Microbial Drugs and Medicinal Chemistry, Helmholtz-Centre for Infection Research, Braunschweig (Germany)

  1. †

    This work was supported by the Deutsche Forschungsgemeinschaft as part of the Priority Program 1150 (SCHU 1560/1-1 to 1-3). Beam time and support by X12 beamline staff (EMBL Hamburg outstation, DESY) is gratefully acknowledged. Coordinates of the actin/rhizopodin complex have been deposited in the Protein Data Bank under access number 2VYP.

Publication History

  1. Issue published online: 29 DEC 2008
  2. Article first published online: 26 NOV 2008
  3. Manuscript Revised: 3 OCT 2008
  4. Manuscript Received: 18 JUN 2008

Funded by

  • Deutsche Forschungsgemeinschaft

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Keywords:

  • actin;
  • inhibitors;
  • macrolides;
  • myxobacteria;
  • rhizopodin
Thumbnail image of graphical abstract

Three's company: Rhizopodin is a cytostatic macrolide and a potent actin depolymerizer produced by the myxobacterium Myxococcus stipitatus. A crystal structure analysis of the rhizopodin/actin complex reveals that rhizopodin is a C2-symmetric bislactone (see formula). The ternary complex supports the mode of rhizopodin-induced actin dimerization and reveals the absolute configuration and biologically active conformation of this macrolide.

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