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P substance peptide probe capable of specific recognition of neurokinin-1 receptor protein, and preparation and application thereof

A technology of receptor protein and neurokinin, applied in the preparation method of peptide, preparation for in vivo test, tachykinin, etc.

Inactive Publication Date: 2015-07-01
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, there is no report on the use of substance P probes to detect NK-1 receptor protein through dual-functional imaging of magnetic imaging and fluorescence imaging.

Method used

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  • P substance peptide probe capable of specific recognition of neurokinin-1 receptor protein, and preparation and application thereof
  • P substance peptide probe capable of specific recognition of neurokinin-1 receptor protein, and preparation and application thereof
  • P substance peptide probe capable of specific recognition of neurokinin-1 receptor protein, and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] The preparation method of the substance P polypeptide dimer comprises the following steps:

[0088] a. Preparation of substance P sequence

[0089] (1) Synthesize using a microwave peptide synthesizer, put Rink amide resin (312mg, 0.25mmol) and Fmoc methionine (290.6mg, 0.75mmol) in a reaction bottle, add organic base and coupling agent, in DMF solution After reacting under microwave conditions for 30 minutes, the Fmoc protecting group was removed to obtain a resin coupled with methionine;

[0090] (2) Repeat step (1) in turn, wherein the raw amino acids are replaced by Fmoc leucine (265.06mg, 0.75mmol), Fmoc glycine (223.0mg, 0.75mmol), Fmoc benzoxyline (290.57mg, 0.75mmol) , Fmoc benzoic acid (290.57mg, 0.75mmol), Fmoc glutamine (458.03mg, 0.75mmol) with Trt protecting group on the side, Fmoc glutamine (458.03mg, 0.75mmol) with Trt protecting group on the side ), Fmoc proline (253.03mg, 0.75mmol), Fmoc lysine (351.41mg, 0.75mmol) with Boc protecting group on the sid...

Embodiment 2

[0104] This embodiment is an improvement made on the basis of Embodiment 1. For the same part as Embodiment 1 in this embodiment, please refer to the content disclosed in Embodiment 1 for understanding, and the content disclosed in Embodiment 1 should also be used as the content of this embodiment The content is not repeated here.

[0105] The preparation method of the substance P polypeptide dimer comprises the following steps:

[0106] Preparation of Substance P Polypeptide Polymers

[0107] (1) Using solid-phase Fmoc technology, the resin obtained in step a of Example 1 and the above-mentioned amino acids sequentially coupled and Fmoc lysine (339.38mg, 0.75mmol) with a protective group Allco on the side were placed in a reaction flask, Add organic base and coupling agent, and react in DMF solution to couple it to the peptide chain.

[0108] (2) Add Pd(Ph 3 P) 4 (105.6mg, 0.1mmol) and PhSiH 3 (1.48mL, 12mmol), react in DMF for 10 minutes to remove Allco on the side chai...

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Abstract

The invention provides a P substance peptide probe capable of specific recognition of a neurokinin-1 receptor protein. the P substance peptide probe is a polypeptide dimer or a polypeptide polymer, the monomer is formed by a P substance amino acid sequence MLGFFQQPKPR, a bifunctional chelating group, a fluorescence group and a terpyridyl group connected through lysine. The novel peptide probe is used for the preparation of a polypeptide dimer and polypeptide polymer with function of diagnosing multi tumors. The polypeptide dimer and polypeptide polymer marks metal Gd<3+> to a polypeptide molecule by the bifunctional chelating group; the marked P substance peptide probe and the NK-1 receptor protein specifically bind and concentrate to the tumor site in vivo; and magnetic imaging and optical imaging technology are utilized for detection of the neurokinin-1 receptor protein to improve the sensitivity of the detection.

Description

technical field [0001] The present invention relates to the field of drugs for tumor diagnosis, in particular to a substance P polypeptide probe specifically recognizing neurokinin-1 receptor protein and its preparation and application. The substance P polypeptide probe is a novel polypeptide dimer and Polypeptide polymers that detect tumors by specifically binding to the neurokinin-1 (NK-1) receptor protein in tumors. Background technique [0002] Lung cancer is one of the most common malignant tumors. Lung cancer ranks first among the causes of death from malignant tumors in urban population in my country. There is no obvious improvement in 10, and the total cure rate is about 10%. At present, there is a lack of specific indicators and methods for early diagnosis, and some tests that affect diagnostic staging are difficult to popularize and implement. Lung cancer patients have no specific symptoms in the early stage, so most of them are in the middle and late stages when t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/22C07K1/13C07K1/06C07K1/04A61K49/00
CPCY02P20/55
Inventor 田禾吴静娴陈磊吴君臣
Owner EAST CHINA UNIV OF SCI & TECH
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