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Title 

Development of cyclic peptomer inhibitors targeting the polo-box domain of polo-like kinase 1

Authors 

R N MuruganJ E ParkD LimM AhnC CheongT KwonK Y NamS H ChoiBo Yeon KimD Y YoonM B YaffeDae Yeul YuK S LeeJ K Bang

Publisher 

Elsevier

Issue Date 

2013

Citation 

Bioorganic & Medicinal Chemistry, vol. 21, no. 9, pp. 2623-2634

Keywords 

Cyclic peptomersKinase inhibitorsPolo-box domain (PBD)Solid phase peptide synthesis

Abstract 

The polo-box domain (PBD) of polo-like kinase 1 (Plk1) is essentially required for the function of Plk1 in cell proliferation. The availability of the phosphopeptide-binding pocket on PBD provides a unique opportunity to develop novel protein-protein interaction inhibitors. Recent identification of a minimal 5-residue-long phosphopeptide, PLHSpT, as a Plk1 PBD-specific ligand has led to the development of several peptide-based inhibitors, but none of them is cyclic peptide. Through the combination of single-peptoid mimics and thio-ether bridged cyclization, we successfully demonstrated for the first time two cyclic peptomers, PL-116 and PL-120, dramatically improved the binding affinity without losing mono-specificity against Plk1 PBD in comparison with the linear parental peptide, PLHSpT. These cyclic peptomers could serve as promising templates for future drug designs to inhibit Plk1 PBD.

ISSN 

0968-0896

Link 

http://dx.doi.org/10.1016/j.bmc.2013.02.020

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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