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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

A technology of growth factor receptors and vascular endothelium, which is applied in the field of tumor targeted drug delivery and medicinal chemistry, can solve the problems that there are no further in vivo experimental reports, and achieve good tumor targeting effect, high purity and broad application prospects Effect

Inactive Publication Date: 2016-06-22
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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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  • 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
  • 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
  • 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

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Embodiment Construction

[0027] Below in conjunction with specific embodiment, further illustrate the present invention. These examples are only for illustrating the present invention and are not intended to limit the scope of the present invention.

[0028] 1. The search for active sites of VEGFR-3 and the construction of a preferential peptide library

[0029] In RCSB Protein Data Bank (PDB), there are 2 X-ray diffraction crystal structures of VEGFR-3, and we selected the crystal structure of the D4-D5 region of VEGFR-3 for research (PDBID: 4BSJ). Before using the crystal structure, first use The ProteinPreparationWizardWorkflow process in 2009 processes the crystal structure, and optimizes the hydrogen atoms by using the OPLS2005 force field after hydrogenation. Subsequently, to find suitable binding targets, virtual molecular probes and The sitemap module in 2009 comprehensively searched for potential binding hotspots of VEGFR-3. Each binding hotspot has its own different structural character...

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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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K47/42A61K41/00A61K49/14A61K51/08A61K9/127A61K45/00A61P35/00A61P35/02
CPCC07K7/06A61K9/127A61K41/00A61K45/05A61K47/42A61K49/146A61K51/08
Inventor 王越李红玫陆涛刘理想李秉霞王齐彦李祯董志鹏
Owner CHINA PHARM UNIV
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