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Directional Plk1 inhibition-driven cell cycle interruption using amphiphilic thin-coated peptide-lanthanide
Chi-Fai Chan1, Rongfeng Lan, Ming-Kiu Tsang
1Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong. klwong@hkbu.edu.hk.
Abstract:
Polo-like kinase 1 (Plk1) is a major serine/threonine protein kinase which regulates key mitotic events such as centrosome duplication, spindle assembly and chromosome separation. Overexpression and aberrant activities of Plk1 can be detected in different types of cancer. Given that the unique polo box domain (PBD) pocket provides an excellent drug target for Plk1 binding and inhibition, we have rationally designed multifunctional lanthanide-doped upconversion nanomaterials. NaGdF4:Yb3+, Er3+ (NaGdF4) and BaGdF5:Yb3+, Er3+ (BaGdF5) nanoparticles of two different sizes (60 nm and 10 nm, respectively) have been thin-coated with Plk1 specific peptides (-P1 = PLHSpT, -P2 = PLHSD, and -P3 = GGPLHSpT) to prepare novel nanomaterials. Comparative studies on cellular uptake, anti-cancer activity and imaging properties were then carried out. The experimental data obtained support our original hypothesis that the designed nanomaterials can successfully deliver Plk1 specific peptides into cancer cells causing Plk1 inhibition while simultaneously allowing direct NIR imaging and monitoring. Among the NaGdF4-Pn and BaGdF5-Pn nanoparticle series prepared in this study, NaGdF4-P1 emerged as the best candidate for Plk1 binding and imaging. NaGdF4-P1 can effectively exert cell cycle G2/M arrest and thus selective tumor inhibition both in vitro and in vivo and as such it offers a potentially interesting system for the development of new cancer therapies.
Insights
Researchers developed novel lanthanide-doped nanoparticles that deliver Plk1-specific peptides into cancer cells. This inhibits Polo-like kinase 1 (Plk1), enabling targeted cancer therapy and near-infrared imaging.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- Polo-like kinase 1 (Plk1) is crucial for cell division and often overexpressed in cancers.
- The Plk1 polo box domain (PBD) is a viable target for anti-cancer drug development.
- Current therapies lack targeted delivery and real-time monitoring capabilities.
Purpose of the Study:
- To design and synthesize multifunctional lanthanide-doped upconversion nanomaterials for targeted Plk1 inhibition.
- To functionalize nanoparticles with Plk1-specific peptides for enhanced cellular uptake and drug delivery.
- To evaluate the anti-cancer efficacy and imaging properties of the developed nanomaterials.
Main Methods:
- Synthesis of NaGdF4:Yb3+, Er3+ and BaGdF5: Yb3+, Er3+ nanoparticles.
- Functionalization of nanoparticles with Plk1-specific peptides (P1, P2, P3).
- In vitro and in vivo studies assessing cellular uptake, Plk1 inhibition, cell cycle arrest, and tumor inhibition.
Main Results:
- Designed nanoparticles successfully delivered Plk1-specific peptides into cancer cells.
- NaGdF4-P1 nanoparticles demonstrated potent Plk1 inhibition, leading to G2/M cell cycle arrest.
- Effective in vitro and in vivo tumor inhibition was observed with NaGdF4-P1, alongside NIR imaging capabilities.
Conclusions:
- The developed NaGdF4-P1 nanomaterials offer a promising dual-function platform for targeted cancer therapy and imaging.
- This approach provides a novel strategy for inhibiting Plk1 and treating various cancers.
- Further development of these nanomaterials could lead to advanced cancer treatment modalities.
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