Peptoid-Peptide hybrid ligands targeting the polo box domain of polo-like kinase 1.
Peptoid-Peptide hybrid ligands targeting the polo box domain of polo-like kinase 1.
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DOI：
10.1002/cbic.201200206
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发表时间：
2012-06-18
期刊：
影响因子：
--
通讯作者：
Burke TR Jr
中科院分区：
文献类型：
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作者：
Liu F;Park JE;Qian WJ;Lim D;Scharow A;Berg T;Yaffe MB;Lee KS;Burke TR Jr
We replaced the amino terminal Pro residue of the Plk1 polo box domain-binding 5-mer peptide (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 made clear by X-ray co-crystal data.
