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

Murugan RN, Park JE, Lim D, Ahn M, Cheong C, Kwon T, Nam KY, Choi SH, Kim BY, Yoon DY, Yaffe MB, Yu DY, Lee KS, Bang JK
Bioorg Med Chem 21 2623-34 (2013)
Cited: 27 times
EuropePMC logo PMID: 23498919

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.

Articles - 4hy2 mentioned but not cited (2)

  1. Exploring the binding nature of pyrrolidine pocket-dependent interactions in the polo-box domain of polo-like kinase 1. Murugan RN, Ahn M, Lee WC, Kim HY, Song JH, Cheong C, Hwang E, Seo JH, Shin SY, Choi SH, Park JE, Bang JK. PLoS One 8 e80043 (2013)
  2. Dynamic and multi-pharmacophore modeling for designing polo-box domain inhibitors. Sakkiah S, Senese S, Yang Q, Lee KW, Torres JZ. PLoS One 9 e101405 (2014)


Reviews citing this publication (7)

  1. Modulating protein-protein interactions: the potential of peptides. Nevola L, Giralt E. Chem Commun (Camb) 51 3302-3315 (2015)
  2. Recent Advances and New Strategies in Targeting Plk1 for Anticancer Therapy. Lee KS, Burke TR, Park JE, Bang JK, Lee E. Trends Pharmacol Sci 36 858-877 (2015)
  3. Recent Trends in Cyclic Peptides as Therapeutic Agents and Biochemical Tools. Choi JS, Joo SH. Biomol Ther (Seoul) 28 18-24 (2020)
  4. Current progress and future perspectives in the development of anti-polo-like kinase 1 therapeutic agents. Park JE, Hymel D, Burke TR, Lee KS. F1000Res 6 1024 (2017)
  5. Inhibitors of the Polo-Box Domain of Polo-Like Kinase 1. Berg A, Berg T. Chembiochem 17 650-656 (2016)
  6. Targeting kinase signaling pathways with constrained peptide scaffolds. Hanold LE, Fulton MD, Kennedy EJ. Pharmacol Ther 173 159-170 (2017)
  7. Putting a bit into the polo-box domain of polo-like kinase 1. Park JE, Kim TS, Meng L, Bang JK, Kim BY, Lee KS. J Anal Sci Technol 6 27 (2015)

Articles citing this publication (18)



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