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Published on: September 17, 2013
Neuropilin-1-target self-assembled peptide nanoparticles contribute to tumor treatment by inducing pyroptosis
Zheng Zhao1, Jingyun Wang1, Mengmeng Liu2,3
1State Key Laboratory of Oncology in South China, Guangdong Key Laboratory of Nasopharyngeal Carcinoma Diagnosis and Therapy, Guangdong Provincial Clinical Research Center for Cancer, Sun Yat-Sen University Cancer Center, 651 Dongfeng East Road, Guangzhou, 510060, People's Republic of China.
Background:
Expression of the Neuropilin-1 (NRP1) is reported in malignant cells of multiple human tumor types represented as a tumor marker. Targeting NRP1 with a peptide, CK3, is used for tumor molecular imaging, raising the question of the therapeutic potential of CK2, a peptide with a CK3 backbone which enhanced targeting and tumor enrichment properties.
Methods:
The tumor targeting and enrichment capacity of CK2 was detected by IncuCyte, flow cytometry and animal living imaging. To enhance its therapeutic efficacy, we developed a self-assembling peptide nanoparticles Fmoc-Gffy-AP-CK2, incorporating a peptide protective domain (Fmoc), a self-assemble domain (Gffy) and an anti-tumor peptide (AP). In vitro cellular assays and in vivo tumor-xenograft experiments were conducted to evaluate the anti-tumor effect of Fmoc-Gffy-AP-CK2.
Results:
While CK3 peptide specifically targets NRP1 in vitro and in vivo, CK2 markedly achieves stronger binding with NRP1 and higher tumor accumulation. Fmoc-Gffy-AP-CK2 exhibits a potent NRP1-dependent cytotoxic effect in vitro and in vivo. Mechanically, Fmoc-Gffy-AP-CK2 triggered caspase3/gasdermin E (GSDME)-mediated pyroptosis. Fmoc-Gffy-AP-CK2 also promotes the response rate of PD-1 checkpoint blockade.
Conclusions:
CK2, When combined with Fmoc-Gffy-AP domain, Demonstrated high anti-tumor efficacy, Providing a novel strategy for tumor treatment.
Insights
A novel peptide nanoparticle, Fmoc-Gffy-AP-CK2, shows enhanced tumor targeting and potent anti-tumor effects by inducing pyroptosis. This peptide nanoparticle strategy offers a promising new approach for cancer treatment.
Area of Science:
- Biomedical Engineering
- Oncology
- Nanotechnology
Background:
- Neuropilin-1 (NRP1) is a marker in various human tumors.
- Peptide CK3 targets NRP1 for tumor imaging.
- CK2 peptide shows enhanced NRP1 targeting and tumor accumulation compared to CK3.
Purpose of the Study:
- To evaluate the therapeutic potential of the CK2 peptide.
- To develop and assess a self-assembling peptide nanoparticle (Fmoc-Gffy-AP-CK2) for enhanced tumor targeting and therapeutic efficacy.
- To investigate the anti-tumor mechanisms and effects of Fmoc-Gffy-AP-CK2.
Main Methods:
- IncuCyte, flow cytometry, and in vivo imaging were used to assess CK2's tumor targeting and accumulation.
- Fmoc-Gffy-AP-CK2 nanoparticles were synthesized, incorporating protective, self-assembly, and anti-tumor peptide domains.
- In vitro cellular assays and in vivo tumor-xenograft models were employed to evaluate anti-tumor activity.
Main Results:
- CK2 demonstrated superior NRP1 binding and tumor accumulation over CK3.
- Fmoc-Gffy-AP-CK2 exhibited significant NRP1-dependent cytotoxicity in vitro and in vivo.
- The nanoparticle induced caspase3/gasdermin E (GSDME)-mediated pyroptosis and enhanced PD-1 blockade response.
Conclusions:
- Fmoc-Gffy-AP-CK2 nanoparticles display high anti-tumor efficacy.
- This peptide nanoparticle system represents a novel strategy for cancer therapy.
- The findings highlight the potential of NRP1-targeted peptide nanoparticles in oncology.
