Polypeptide capable of specifically binding with human vascular endothelial growth factor receptor-3 (VEGFR-3) protein and screening method and identification and application of polypeptide

Abstract

Based on the protein crystal structure of human vascular endothelial growth factor receptor-3 (VEGFR-3), the present invention designs and develops a polypeptide that specifically binds to it, and discloses its screening method, identification and use. The general formula of the amino acid sequence of the polypeptide is CXXPFXP, X is any L-type or D-type amino acid in 20 kinds of natural amino acids. The present invention also relates to the amide, ester or salt of the polypeptide, or the active fragment, active derivative and fusion polypeptide formed by the polypeptide, or the polymer formed by using the polypeptide as a ligand. Using computer simulation screening and immunofluorescence in vitro verification to obtain tumor-targeting polypeptides with high expression of VEGFR-3, it is convenient and quick. The screened polypeptides have clear structures, high affinity with target proteins, almost no immunogenicity, and are easy to prepare and produce. It has broad application prospects in the fields of tumor-targeted drug delivery, imaging and diagnosis, and gene transfection.

Description

technical field [0001] The present invention belongs to the field of medicinal chemistry, and in particular relates to the screening and application of a polypeptide, in particular to a polypeptide capable of specifically binding to human vascular endothelial growth factor receptor-3 (VEGFR-3) and derivatives of the above polypeptide. Applications in the field of tumor-targeted drug delivery. Background technique [0002] In recent years, molecular targeted drugs developed for the specific molecular signaling pathways of tumor cells have emerged in an endless stream. However, with the deepening of research, its limitations began to be highlighted, and the existence of drug resistance caused by gene mutations limited its clinical application. Targeted drug delivery system (TDDS) refers to a new type of drug delivery system in which the carrier selectively concentrates and localizes drugs in diseased tissues, organs, cells or intracellular structures through local administrat...

AI Technical Summary

Problems solved by technology

Peptides targeting VEGFR-3 have appeared and effectively target the VEGFR-3 signaling pathway at the cellular level, but no further in vivo experiments have been reported. Therefore, there is an urgent need for further novel targeting polypeptides and The development and research of peptide drug delivery systems may also provide new means for tumor imaging and diagnosis

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