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A kind of polypeptide targeting syntenin protein and its dimer and application

A technology of dimerization and action, which is applied in the field of peptides and dimers targeting Syntenin protein, which can solve the problems of high effective concentration and low affinity of small molecule inhibitors, and achieve high affinity effect

Active Publication Date: 2021-06-11
SHANGHAI FIRST MATERNITY & INFANT HOSPITAL
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to provide a high-affinity inhibitor targeting the Syntenin protein, which can inhibit the migration, proliferation and invasion of cancer cells by combining the tandem PDZ domains in the Syntenin protein, so as to solve the problem of small molecule inhibitor affinity Not high, the disadvantage of high effective concentration

Method used

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  • A kind of polypeptide targeting syntenin protein and its dimer and application
  • A kind of polypeptide targeting syntenin protein and its dimer and application
  • A kind of polypeptide targeting syntenin protein and its dimer and application

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Embodiment Construction

[0046] The present invention will be further described below in conjunction with specific examples.

[0047] 1. Peptide synthesis and affinity characterization

[0048] Select the following four polypeptide sequences from the literature: RVAFFEEL (polypeptide epitope of Merlin protein), TNEFYA (polypeptide epitope of syndecan protein), DKEYYV (polypeptide epitope of neurexin protein), LEDSVF (polypeptide epitope of interleukin-5 receptorα protein) .

[0049] In order to facilitate subsequent characterization, a FAM fluorescent group was added to the N-terminus, and GS amino acid was used as the spacer between the fluorescent group and the functional amino acid region.

[0050] 1. Synthesis of monomeric polypeptide

[0051] 1) Using Fmoc chemical solid-phase peptide synthesis, using Fmoc-wang resin, using 5-fold excess of Fmoc-protected amino acids and condensation reagents (HBTU / HOBt) to synthesize peptides.

[0052] 2) Cysteine ​​C is added near the N-terminus of the polyp...

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Abstract

The invention discloses a polypeptide targeting Syntenin protein and its dimer and application, belonging to the technical field of biomedicine. The amino acid sequence of the polypeptide is Cys-Asp-Lys-Glu-Φ-Φ-Val, wherein Φ is 3-(2-naphthyl)-L-alanine. The polypeptide provided by the invention is obtained by optimizing the amino acid of the screened natural polypeptide ligand, which significantly improves its affinity with the tandem PDZ domain of the Syntenin protein. The dimeric polypeptide obtained by dimerizing the above polypeptides has an affinity with the tandem PDZ domain as high as 210nM, and can effectively inhibit the migration, proliferation and invasion of various cancer cells with high expression of Syntenin at a concentration of 10uM without producing Other toxic and side effects provide design ideas for the development of drugs for the treatment of metastasis and invasion of malignant tumors with high expression of Syntenin.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a polypeptide targeting Syntenin protein and its dimer and application. Background technique [0002] Syntenin is a class of intracellular adapter proteins widely present in prokaryotes and eukaryotes. Studies have found that Syntenin protein is highly expressed in a variety of highly invasive malignant tumors, and its expression is up-regulated with the progression of tumor metastasis. [0003] Syntenin consists of N-terminal domain (N-terminal domain, NTD), two tandem PDZ domains (postsynaptic density protein, disc large and zonula occludens, PDZ) and C-terminal domain (C-terminal domain, CTD). The PDZ domain of syntenin protein can specifically bind to the PDZ binding motif (PBM) at the C-terminus of different membrane receptors, and the diversity of PDZ domain-binding receptors leads to the diversity of syntenin functions. [0004] During the development of tumor cells,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06C07K19/00A61K38/08A61K47/64A61P35/00
CPCA61K38/00A61P35/00C07K7/06C07K2319/10
Inventor 刘佳慧于永生夏江冯茜金莉萍王凯周倩
Owner SHANGHAI FIRST MATERNITY & INFANT HOSPITAL
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