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

Chembiochem : a European Journal of Chemical Biology
Fa LiuTerrence R Burke

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.

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Citations

Oct 20, 2015·Trends in Pharmacological Sciences·Kyung S LeeEunhye Lee
Dec 5, 2015·Chembiochem : a European Journal of Chemical Biology·Andrej ScharowThorsten Berg
Oct 27, 2015·Journal of Analytical Science and Technology·Jung-Eun ParkKyung S Lee
Jan 4, 2015·Bioorganic & Medicinal Chemistry Letters·Meng LiuCheng Jiang
Dec 15, 2015·Chembiochem : a European Journal of Chemical Biology·Thorsten Berg, Angela Berg
Apr 25, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Xue Zhi ZhaoTerrence R Burke
Sep 4, 2018·Bioorganic & Medicinal Chemistry Letters·David HymelTerrence R Burke
Oct 28, 2014·Journal of Medicinal Chemistry·Mija AhnJeong Kyu Bang

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