VEGFR (vascular endothelial growth factor receptor) targeting cracking peptide conjugate and application thereof

Abstract

The invention relates to a VEGFR (vascular endothelial growth factor receptor)-targeted cleavage peptide conjugate and application thereof, a polypeptide ligand of a targeted VEGFR is coupled with cleavage peptide KLU to form a dual-function polypeptide conjugate with an anti-tumor effect, and the specific structure is shown in Figure 1. The invention further discloses the binding capacity of the VEGFR-targeted cleavage peptide conjugate to VEGFR on the surface of a vascular endothelial cell and the binding capacity of the cleavage peptide conjugate to the VEGFR on the surface of the vascular endothelial cell. Experiments of cell proliferation, cell apoptosis and the like prove that the split peptide conjugate can effectively inhibit proliferation of malignant liver cancer. According to the present invention, the rabbit liver cancer treatment experiment through the combination of the VEGFR-targeting lysis peptide conjugate and the hepatic artery embolism shows that the polypeptide conjugate can effectively inhibit the proliferation of the in-vivo tumor, and further has significant in-vivo anti-angiogenesis effect; further biological safety evaluation shows that the split peptide conjugate drug has better biocompatibility and does not cause injury to tissues and organs of a body.

Description

technical field [0001] The invention belongs to the field of bioengineering, and relates to a polypeptide drug conjugate, in particular to a split peptide conjugate targeting VEGFR and its anti-liver cancer application. Background technique [0002] Cancer is a major public health problem worldwide. According to the 2020 global cancer data released by the WHO, there will be 4.57 million new cancer cases and more than 3 million deaths in China in 2020. The number of new cancer cases in China ranks first in the world. Liver cancer, represented by hepatocellular carcinoma (HCC), is the fifth most common cancer and the second leading cause of cancer death worldwide. Unlike the surrounding liver parenchyma, liver tumors are preferentially vascularized by the hepatic artery rather than the portal vein. This difference in vascularization makes selective intravascular delivery of drugs, embolic agents, or radiopharmaceuticals promising for effective treatment of HCC. Studies have...

AI Technical Summary

Problems solved by technology

However, the current clinical TACE technology is mainly based on the chemotherapeutic drug doxorubicin, and there has been no report on the use of lytic peptides combined with anti-VEGFR for TACE treatment research

Images