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Polypeptide capable of specifically targeting HER2 protein and application of polypeptide

A kind of specific and targeted technology, applied in peptides, peptides specifically targeting HER2 protein and its application fields, can solve the problems of poor targeting effect and insufficient interaction

Active Publication Date: 2015-11-25
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although it discloses that the polypeptide has a targeting effect for the treatment of cancer, however, its interaction with HER2 binding is not high enough, and the targeting effect is relatively poor

Method used

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  • Polypeptide capable of specifically targeting HER2 protein and application of polypeptide
  • Polypeptide capable of specifically targeting HER2 protein and application of polypeptide
  • Polypeptide capable of specifically targeting HER2 protein and application of polypeptide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1 The synthesis of polypeptide of the present invention

[0055] 1) Experimental instruments and materials

[0056] Dimethylformamide (DMF), piperidine, resin, dichloromethane (DCM), ninhydrin reagent (ninhydrin, vitamin C, phenol), tetramethyluronium hexafluorophosphate (HBTU), six Hydropyridine (piperidine), triisopropylsilane (TIS), ethanedithiol (EDT), anhydrous ether, trifluoroacetic acid (TFA), N-methylmorpholine (NMM), methanol, various amino acids , Peptide solid-phase synthesis tube.

[0057] 2) Solution preparation

[0058] Deprotection solution - hexahydropyridine: DMF = 1:4

[0059] Reaction solution——NMM:DMF=1:24

[0060] Lysis solution - TFA (92.5%), TIS (2.5%), EDT (2.5%), H 2 O(2.5%)

[0061] Ninhydrin Test Solution—Ninhydrin: Vitamin C: Phenol = 1:1:1

[0062] 3) Experimental steps

[0063]Weigh the resin and put it into the peptide solid-phase synthesis tube (hereinafter referred to as the reactor), and add an appropriate amount of D...

experiment example 1

[0071] Experimental Example 1 Flow cytometry detection of the binding effects of SEQIDNO.1, SEQIDNO.2, SEQIDNO.3, and SEQIDNO.4 on human HER2-positive breast cancer cells respectively

[0072] 1. Experimental method

[0073] Collect human breast cancer HER2 high expression cell line SKBR3, suspend in RPMI1640 culture medium containing 10% heat-inactivated fetal bovine serum, cell density is 1x10 6 / mL, divided into four 1.5mL EP tubes, 200μL / tube. Add fluorescein isothiocyanate (FITC) labeled SEQIDNO.1, SEQIDNO.2, SEQIDNO.3, SEQIDNO.4 and anti-HER2 antibody (ebioscience) respectively, the final concentration is 50μM / L, the control group uses the same amount of polypeptide 0.01mMPBS (phosphate buffer pH 7.4) was used instead of the polypeptide. After incubating in an ice bath in the dark for 30 minutes, centrifuge at 1000g for 4 minutes to collect cells, add 1mL PBS to wash, repeat washing 3 times, add 500μL PBS, mix well, and use flow cytometry to detect fluorescence intensi...

experiment example 3

[0081] Experimental Example 3 Immunofluorescence method to detect the binding effects of SEQIDNO.1, SEQIDNO.2, SEQIDNO.3, and SEQIDNO.4 on human HER2-positive breast cancer cells respectively

[0082] 1. Experimental method

[0083] The human breast cancer HER2 high-expressing cell line SKBR3 was suspended in RPMI1640 culture medium containing 10% heat-inactivated fetal bovine serum, and seeded in three confocol small dishes at a density of 3000-5000 cells / dish. After cultivating for 24 hours, aspirate the medium in the small dish, and then add the culture medium containing 50 μM mol / L of fluorescein isothiocyanate (FITC) labeled SEQIDNO.1, SEQIDNO.2, SEQIDNO.3, SEQIDNO.4 polypeptide respectively The base was 200 μL, and the control group used the medium containing PBS (phosphate buffer pH 7.4) equal to the amount of the polypeptide, and the nuclei were stained with the hoechst reagent, which was diluted 1:200. Incubate in an ice bath protected from light for 30 minutes. Aft...

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Abstract

The invention relates to polypeptide capable of specifically targeting HER2 (human epidermal growth factor receptor 2) protein and an application of the polypeptide. The polypeptide is shown by the following general formula: X1X2X3X4X5LX6X7X8NPX9X10X11X12X13. The invention also relates to a nucleotide sequence for coding the polypeptide, and an expression vector for expressing the polypeptide, and host cells; and the invention also relates to the polypeptide, a bivalent or a multivalent formed by the polypeptide, and a pharmaceutical composition which is formed by the polypeptide serving as a targeting polypeptide, a preparation capable of killing cancer cells, and an imaging preparation, as well as applications of the polypeptide, the bivalent or the multivalent, and the pharmaceutical composition. The polypeptide provided by the invention can achieve a targeting effect on positive tumor cells of HER2, is strong in selectivity, can be prepared by adopting a chemical synthesis method, is high in purity, small in molecular weight and strong in specificity, and is free of immunogenicity, safe and reliable.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, in particular to a polypeptide, in particular to a polypeptide specifically targeting HER2 protein and its application. Background technique [0002] Cancer is a leading cause of death worldwide. Data show that in 2012 there were approximately 14.1 million new cancer cases and 8.2 million cancer deaths worldwide, compared with 12.7 million and 7.6 million in 2008. The most common cancers diagnosed worldwide were lung cancer (1.8 million, 13%), breast cancer (1.7 million, 11.9%), and colorectal cancer (1.4 million, 9.7%), and the leading cause of death was lung cancer (1.6 million, 19.4%), liver cancer (800,000, 9.1%) and gastric cancer (700,000, 8.8%). Based on available data, the International Agency for Research on Cancer predicts that due to global population growth and aging, by 2025, the number of new cancer cases worldwide will be as high as 19.3 million per year. In 2012, more ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08C12N15/11C12N15/63A61K51/08A61K49/00A61K47/42A61P35/00
Inventor 耿令令方巧君
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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