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Chembiochem. 2012 Jun 18;13(9):1291-6. doi: 10.1002/cbic.201200206. Epub 2012 May 8.

Peptoid-Peptide hybrid ligands targeting the polo box domain of polo-like kinase 1.

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  • 1Chemical Biology Laboratory, Frederick National Lab, NCI, NIH, Frederick, MD 21702, USA.

Abstract

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.

PMID:
22570300
PMCID:
PMC4536914
DOI:
10.1002/cbic.201200206
[PubMed - indexed for MEDLINE]
Free PMC Article
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