Work

Peptoid–Peptide Hybrid Ligands Targeting the Polo Box Domain of Polo‐Like Kinase 1

Year: 2012

Type: article

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.

Source: ChemBioChem

DOI: 10.1002/cbic.201200206

Authors: Fa Liu, Jung‐Eun Park, Wen‐Jian Qian, Dan Lim, Andrej Scharow, Thorsten Berg, Michael B. Yaffe, Kyung S. Lee, Terrence R. Burke

Institutions: National Institutes of Health, National Cancer Institute, Massachusetts Institute of Technology, Leipzig University, Frederick National Laboratory for Cancer Research

Language: English

Topic: Chemical Synthesis and Analysis

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

Open Access status: green

Funders: National Institutes of Health, National Institute of General Medical Sciences, National Institute of Environmental Health Sciences

Awards: G4206668042, Protein Kinase Signaling and Cell Cycle Control, G607431349, G6350445350

OpenAlex ID: W1983267196

FWCI: 2.322

Cites: 31

Cited by: 40

Related to: 10