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Tumor-penetrating peptide for systemic targeting of Tenascin-C
Prakash Lingasamy1, Allan Tobi1, Kaarel Kurm1
1Laboratory of Cancer Biology, Institute of Biomedicine and Translational Medicine, University of Tartu, Tartu, Estonia.
Abstract:
Extracellular matrix in solid tumors has emerged as a specific, stable, and abundant target for affinity-guided delivery of anticancer drugs. Here we describe the homing peptide that interacts with the C-isoform of Tenascin-C (TNC-C) upregulated in malignant tissues. TNC-C binding PL3 peptide (amino acid sequence: AGRGRLVR) was identified by in vitro biopanning on recombinant TNC-C. Besides TNC-C, PL3 interacts via its C-end Rule (CendR) motif with cell-and tissue penetration receptor neuropilin-1 (NRP-1). Functionalization of iron oxide nanoworms (NWs) and metallic silver nanoparticles (AgNPs) with PL3 peptide increased tropism of systemic nanoparticles towards glioblastoma (GBM) and prostate carcinoma xenograft lesions in nude mice (eight and five-fold respectively). Treatment of glioma-bearing mice with proapoptotic PL3-guided NWs improved the survival of the mice, whereas treatment with untargeted particles had no effect. PL3-coated nanoparticles were found to accumulate in TNC-C and NRP-1-positive areas in clinical tumor samples, suggesting a translational relevance. The systemic tumor-targeting properties and binding of PL3-NPs to the clinical tumor sections, suggest that the PL3 peptide may have applications as a targeting moiety for the selective delivery of imaging and therapeutic agents to solid tumors.
Insights
Researchers developed a PL3 peptide that targets Tenascin-C (TNC-C) in tumors. This peptide guides nanoparticles to solid tumors, enhancing drug delivery and improving survival in preclinical models.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Oncology
Background:
- The extracellular matrix in solid tumors offers a stable target for drug delivery.
- Tenascin-C (TNC-C), particularly its C-isoform, is upregulated in malignant tissues.
Purpose of the Study:
- To identify and characterize a peptide that targets TNC-C for selective delivery of therapeutic agents to solid tumors.
- To evaluate the efficacy of PL3-peptide-functionalized nanoparticles in targeting and treating tumors in vivo.
Main Methods:
- In vitro biopanning was used to identify the TNC-C binding PL3 peptide (AGRGRLVR).
- PL3 peptide was conjugated to iron oxide nanoworms (NWs) and silver nanoparticles (AgNPs).
- Targeting efficacy was assessed in glioblastoma and prostate carcinoma xenograft models in nude mice.
Main Results:
- PL3 peptide functionalization enhanced nanoparticle tropism towards tumors by 8-fold (NWs) and 5-fold (AgNPs).
- PL3-guided nanoworms significantly improved survival in glioma-bearing mice compared to untargeted particles.
- PL3-coated nanoparticles localized to TNC-C and neuropilin-1 (NRP-1) positive areas in clinical tumor samples.
Conclusions:
- The PL3 peptide effectively targets TNC-C and NRP-1, demonstrating potential for selective delivery to solid tumors.
- PL3-functionalized nanoparticles show promise for targeted cancer therapy and imaging applications.
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