Monitoring and inhibition of Plk1: Amphiphilic porphyrin conjugated Plk1 specific peptides for its imaging and anti-tumor function

Hongguang Li, Chi Fai Chan, Wai Lun Chan, Sam Lear, Steven L. Cobb*, Nai Ki MAK, Terrence Chi Kong Lau, Rongfeng Lan, Rick W K WONG, Ka-Leung WONG

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)

Abstract

Polo-like kinase 1 (Plk1) is well-known for taking part in cell cycle progression and regulation. Using small molecules for Plk inhibition has been well documented in the literature. However, there are several intrinsic and intractable problems associated with this approach. For example monitoring small molecule Plk inhibitors as anti-tumor agents in vitro/in vivo is often ineffective, they can have poor cell internalization and be susceptible to enzymatic degradation. Herein, we report the synthesis of cell-permeable, water-soluble amphiphilic porphyrin-Plk1 specific peptide bioconjugates, Por-P1 and Por-P2. In addition to resolving the aforementioned problems of the small molecule inhibitors Por-P2 manifests responsive emission enhancement upon binding with Plk1 in aqueous medium and in vitro, while potently triggering G2-M phase arrest and then apoptosis selectively in the cancer cells tested. In combination our findings make Por-P2 a promising candidate for the preparation of a new generation of smart chemotherapeutic targeting agents (imaging and inhibition) for Plk1 in particular cancer cell lines. This journal is

Original languageEnglish
Pages (from-to)5876-5882
Number of pages7
JournalOrganic and Biomolecular Chemistry
Volume12
Issue number31
DOIs
Publication statusPublished - 21 Aug 2014

Scopus Subject Areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

Fingerprint

Dive into the research topics of 'Monitoring and inhibition of Plk1: Amphiphilic porphyrin conjugated Plk1 specific peptides for its imaging and anti-tumor function'. Together they form a unique fingerprint.

Cite this