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Screening and characterisation of a novel efficient tumour cell-targeting peptide derived from insulin-like growth
Min-Lin He1, Jin Lei1, Xue-Wei Cao1,2
1Department of Applied Biology, East China University of Science and Technology, Shanghai, People's Republic of China.
Abstract:
Targeted delivery of antitumor drugs is particularly important in tumour treatment. Tumour-targeted peptide is a very effective drug carrier for tumour therapy. Here, we screened and characterised a highly efficient targeted peptide named IHP5, which was derived from insulin-like growth factor binding proteins (IGFBPs). IHP5 exhibited preferential binding to the tested tumour cell lines. The delivery efficiency of IHP5 was higher in various tested tumour cells than in normal cells, especially in the human cervical cancer cell line HeLa, which was 11.7-fold higher than in normal human embryonic kidney cells HEK293. Moreover, the penetration efficiency of IHP5 was 13 times higher than that of the classical cell penetrating peptide TAT in HeLa cells. Detail analysis revealed that IHP5 endocytosis was possibly correlated with acetylated heparan sulphate proteoglycans including phosphatidylinositol proteoglycan 3 (GPC3), phosphatidylinositol proteoglycan 5 (GPC5) and syndecan 2 (SDC2). Subsequently, the introduction of IHP5 enhanced the inhibitory effect of trichosanthin (TCS) on tumour cells, resulting in at least 19-fold increase in tumour cells without enhanced cytotoxicity in normal cells HEK293. These results suggested that IHP5, as a novel tumour cell-targeting penetrating peptide with the ability to target tumour cells, has great potential in drug delivery applications.
Insights
Researchers identified IHP5, a novel peptide targeting tumor cells for enhanced drug delivery. This peptide significantly improves antitumor drug efficacy without increasing toxicity in normal cells, showing great therapeutic potential.
Area of Science:
- Biotechnology
- Molecular Biology
- Oncology
Background:
- Targeted drug delivery is crucial for effective tumor treatment.
- Tumor-targeted peptides serve as efficient carriers for antitumor drugs.
Purpose of the Study:
- To screen and characterize a novel, highly efficient tumor-targeting peptide named IHP5.
- To evaluate the drug delivery and penetration efficiency of IHP5 in tumor cells compared to normal cells.
- To assess the potential of IHP5 in enhancing the efficacy of antitumor drugs.
Main Methods:
- Screening and characterization of the IHP5 peptide derived from insulin-like growth factor binding proteins (IGFBPs).
- Assessing IHP5 binding affinity and delivery efficiency in various tumor cell lines (e.g., HeLa) versus normal cells (e.g., HEK293).
- Evaluating IHP5 penetration efficiency compared to the TAT peptide.
- Investigating the endocytosis mechanism of IHP5, focusing on interactions with specific proteoglycans.
- Assessing the combined effect of IHP5 and trichosanthin (TCS) on tumor cell inhibition and cytotoxicity in normal cells.
Main Results:
- IHP5 demonstrated preferential binding and higher delivery efficiency in tested tumor cells compared to normal cells, with an 11.7-fold increase in HeLa cells versus HEK293 cells.
- IHP5 exhibited 13 times higher penetration efficiency than the TAT peptide in HeLa cells.
- IHP5 endocytosis was linked to acetylated heparan sulfate proteoglycans (GPC3, GPC5, SDC2).
- Co-administration of IHP5 with trichosanthin (TCS) resulted in at least a 19-fold increase in tumor cell inhibition without enhanced cytotoxicity in HEK293 cells.
Conclusions:
- IHP5 is a novel tumor cell-targeting and penetrating peptide with significant potential for drug delivery applications.
- IHP5 enhances the efficacy of antitumor drugs like TCS specifically in tumor cells, minimizing off-target effects.
- The findings support the development of IHP5-based strategies for improved cancer therapy.
