This work was supported by the Max Planck Society, the Bioband of TU Dortmund (R.B. and W.B.), the Deutsche Forschungsgemeinschaft (grant BL587 to W.B.), and the University of Leipzig (R.B.). W.B. thanks Roger S. Goody for his support. We thank Dmitri V. Mavrodi and Linda S. Thomashow for the expression plasmid and Isha Himani Jain for performing crystallization experiments. The help of the X-ray communities at the MPI of Molecular Physiology, the MPI for Medical Research, and the beamline staff at beamline X10SA of the Swiss Light Source with data collection is gratefully acknowledged.
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Communication
The Active Site of an Enzyme Can Host Both Enantiomers of a Racemic Ligand Simultaneously†
Article first published online: 28 OCT 2009
DOI: 10.1002/anie.200902997
Copyright © 2009 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Issue
Angewandte Chemie International Edition
Volume 48, Issue 48, pages 9084–9087, November 16, 2009
Additional Information
How to Cite
Mentel, M., Blankenfeldt, W. and Breinbauer, R. (2009), The Active Site of an Enzyme Can Host Both Enantiomers of a Racemic Ligand Simultaneously. Angew. Chem. Int. Ed., 48: 9084–9087. doi: 10.1002/anie.200902997
- †
Publication History
- Issue published online: 11 NOV 2009
- Article first published online: 28 OCT 2009
- Manuscript Received: 3 JUN 2009
Funded by
- Max Planck Society
- TU Dortmund
- Deutsche Forschungsgemeinschaft. Grant Number: BL587
Keywords:
- biosynthesis;
- chirality;
- drug design;
- medicinal chemistry;
- protein structures
Two in one: Proteins usually bind only one enantiomer of a racemic ligand. Now a new binding mode for chiral drugs has been identified by protein crystallography. The homodimeric enzyme PhzA/B (in the picture the monomers are yellow and magenta) can host both enantiomers of a racemic ligand (light and dark gray) in its active site at the same time (dark red Br, blue N, light red O).