1256286-88-0Relevant articles and documents
Peptoid-Peptide Hybrid Ligands Targeting the Polo Box Domain of Polo-Like Kinase 1
Liu, Fa,Park, Jung-Eun,Qian, Wen-Jian,Lim, Dan,Scharow, Andrej,Berg, Thorsten,Yaffe, Michael B.,Lee, Kyung S.,Burke Jr., Terrence R.
, p. 1291 - 1296 (2012)
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.