These authors contributed equally to this project.
Peptoid–Peptide Hybrid Ligands Targeting the Polo Box Domain of Polo-Like Kinase 1
Article first published online: 8 MAY 2012
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Volume 13, Issue 9, pages 1291–1296, June 18, 2012
How to Cite
Liu, F., Park, J.-E., Qian, W.-J., Lim, D., Scharow, A., Berg, T., Yaffe, M. B., Lee, K. S. and Burke, T. R. (2012), Peptoid–Peptide Hybrid Ligands Targeting the Polo Box Domain of Polo-Like Kinase 1. ChemBioChem, 13: 1291–1296. doi: 10.1002/cbic.201200206
- Issue published online: 13 JUN 2012
- Article first published online: 8 MAY 2012
- Manuscript Received: 26 MAR 2012
- National Cancer Institute
- National Institutes of Health. Grant Numbers: R01 GM60594, ES015339
- Deutsche Forschungsgemeinschaft. Grant Number: BE 4572/1-1
- molecular recognition;
We replaced the amino terminal Pro residue of the Plk1 polo-box-domain-binding pentapeptide (PLHSpT) with a library of N-alkyl-Gly “peptoids”, and identified long-chain tethered phenyl moieties giving greater than two-orders-of-magnitude affinity enhancement. Further simplification by replacing the peptoid residue with appropriate amides gave low-nanomolar affinity N-acylated tetrapeptides. Binding of the N-terminal long-chain phenyl extension was demonstrated by X-ray co-crystal data.