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

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.

SUBMITTER: Liu F

PROVIDER: S-EPMC4536914 | biostudies-literature | 2012 Jun

REPOSITORIES: biostudies-literature

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

Liu Fa F Park Jung-Eun JE Qian Wen-Jian WJ Lim Dan D Scharow Andrej A Berg Thorsten T Yaffe Michael B MB Lee Kyung S KS Burke Terrence R TR

Chembiochem : a European journal of chemical biology 20120508 9

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. ...[more]

PMID: 22570300

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