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PEP06 polypeptide 30 exerts antitumour effect in colorectal carcinoma via inhibiting epithelial mesenchymal transition

Author：Siming Yu, Linnan Li, Wei Tian, Dan Nie, Wei Mu, Fang Qiu, Yu Liu, Xinghan Liu, Xiaofeng Wang, Zhimin Du, WenFeng Chu, Baofeng Yang   《British Journal of Pharmacology》

ABSTRACTS

BACKGROUND AND PURPOSE

This study aimed to verify the antitumour effects of PEP06, a polypeptide modified from endostatin, and to elaborate the mechanisms in treating colorectal carcinoma (CRC).

EXPERIMENTAL APPROACH

After PEP06 treatment, cell proliferation and migration assays were performed in CRC cells. Epithelial mesenchymal transition (EMT) progression was determined with Western blot, immunofluorescent staining and immunohistochemistry in vitro and in a residual xenograft model. MiRNAs regulated by PEP06 were identified by miRNA microarray and verified by in situ hybridization and qRT‐PCR. The interactions between PEP06 and integrin αvβ3 were determined with Biacore SA biochips. Cellular function of miR‐146b‐5p was validated by gain‐ and loss‐of‐function approaches. A mouse model of lung metastasis was used for survival analysis following PEP06 treatment.

CONCLUSION AND IMPLICATIONS

PEP06 is an effective polypeptide against growth and metastasis of colon cancer through its RGD motif binding to integrin αvβ3, thereby downregulating miR‐146b‐5p to inhibit EMT in vitro and in vivo. It might be a promising agent for future application to CRC treatment.
SCREENSHOT

RELATED PRODUCTS
An artificial 24 amino acid with deletion of RGD motif was synthesized by ChinaPeptides (Shanghai, China) and dissolved in glucose. 
CHAINING
https://bpspubs.onlinelibrary.wiley.com/doi/abs/10.1111/bph.14352
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