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Polypeptide molecule with brain targeting function as well as preparation method and application thereof

A brain-targeting and molecular technology, applied in the field of polypeptide molecules with brain-targeting function and their preparation, can solve the problem that macromolecules cannot cross the blood-brain barrier, avoid adverse immune reactions in the human body, and improve the cure rate and speed. Effect

Inactive Publication Date: 2017-05-17
天津博锐生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] An object of the present invention is to provide a polypeptide molecule with brain-targeting function to overcome the technical problem that macromolecules cannot cross the blood-brain barrier in the prior art

Method used

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  • Polypeptide molecule with brain targeting function as well as preparation method and application thereof
  • Polypeptide molecule with brain targeting function as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Liquid Phase Synthesis of CGQK (SEQ ID NO 5)

[0060] Selection of reagents used for synthesis:

[0061] (1) Amino acids: H-Cys(Trt)-OH, Fmoc-Gly-OH, Fmoc-Gln-OH, H-Lys(Boc)-Ome;

[0062] (2) Condensing agent: DIC or HOBT;

[0063] (3) Solvent: DCM;

[0064] (4) Condensation base: DMAP;

[0065] (5) Deprotection reagent: piperidine;

[0066] (6) Cutting fluid: TFA / TIS / H 2 O, the ratio is: 95:2.5:2.5;

[0067] The reaction is carried out in a round bottom flask, stirred with a magnet, the first step reaction:

[0068] Add H-Lys(Boc)-Ome, Fmoc-Gln-OH, condensing agent, and condensing base into the flask at the same time according to the ratio of 1:1:1:1, stir, control the temperature and react at 25°C for 4 hours, add Protecting agent to a concentration of 20%, react for 30 minutes, remove the reaction solution by rotary evaporation, add the solvent DCM for the next reaction: add Fmoc-Gly-OH, condensing agent, and condensing base to the flask according to the ratio...

Embodiment 2

[0070] Solid phase synthesis of CAQKCAQKCAQKCAQKCAQK (SEQ ID NO 4)

[0071] CAQKCAQKCAQKCAQKCAQK (SEQ ID NO 4) was synthesized using the solid-phase peptide synthesis method of the Fmoc strategy, using a Biotage instrument produced by SyroII Company. The operation method was carried out according to the manufacturer's instruction manual.

[0072] Selection of reagents used for synthesis:

[0073] (1) Solid phase resin: 2-cl-trt resin, resin substitution degree 0.75;

[0074] (2) Protected amino acids: Fmoc-Cys(Boc)-OH, Fmoc-Ala-OH, Fmoc-Gln-OH, Fmoc-Lys(Boc)-OH;

[0075] (3) Deprotection reagent: piperidine, the concentration of piperidine in the solution used is 15%-50%; in a preferred embodiment, the concentration of piperidine in the solution used is 20%;

[0076] (4) Coupling reagent: HATU / HOBT / DIEA, the ratio is 1:1:2

[0077] (5) Cutting reagent: TFA / TIS / H 2 O, the ratio is: 95:2.5:2.5;

[0078] The crude peptide was purified by HPLC. Purification conditions: grad...

Embodiment 3

[0080] Solid phase synthesis of CAQKCAQK (SEQ ID NO 2)

[0081] CAQKCAQK (SEQ ID NO 2) was synthesized using the solid-phase peptide synthesis method of the Fmoc strategy, using a Biotage instrument produced by SyroII Company. The operation method was carried out according to the manufacturer's instruction manual.

[0082] Selection of reagents used for synthesis:

[0083] (1) Carrier resin: Fmoc-Lys-wang-rink, degree of substitution: 0.8

[0084] (2) Protected amino acids: Fmoc-Cys(Boc)-OH, Fmoc-Ala-OH, Fmoc-Gln-OH, Fmoc-Lys(Boc)-OH, 5-fold excess of protected amino acids used in the reaction.

[0085] (3) Deprotection reagent: piperidine / N,N-dimethylformamide, the ratio is 20:80.

[0086] (4) Coupling reagent: DIC / HOBT, the ratio is 1:1.5.

[0087] (5) Cutting reagent: TFA / TIS / water, the ratio is: 95:2.5:2.5.

[0088] The prepared polypeptide was purified using a HPLCC18 semi-preparative column, and the detection conditions were: detection wavelength: 214nm, mobile phas...

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Abstract

The invention provides a polypeptide molecule with a brain targeting function as well as a preparation method and application thereof and relates to the technical field of biomedicines. The polypeptide molecule with the brain targeting function, provided by the invention, can pass through a blood brain barrier, and the polypeptide molecule does not have immunogenicity, so that bad immune response on human bodies can be avoided. The polypeptide molecule provided by the invention also can be used as a drug-releasing carrier and can be coupled with related drugs for treating brain diseases to form a conjugate, so that the drugs for treating related brain diseases can pass through the blood brain barrier to directly act on wounds, and furthermore, the healing rate and healing speed of the related brain diseases can be effectively improved.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a polypeptide molecule with brain-targeting function and its preparation method and application. Background technique [0002] At present, the incidence of brain-related diseases is showing an increasing trend year by year, among which the rising trend of brain tumors and brain metastases, ischemic brain injury and various viral inflammation-related diseases is particularly obvious. [0003] In the treatment of brain-related diseases, the blood-brain barrier is considered to be the main reason for preventing chemotherapy drugs from entering the brain tissue and affecting the curative effect. The blood-brain barrier refers to the barrier between the plasma and brain cells formed by the brain capillary wall and glial cells, and the barrier between the plasma and cerebrospinal fluid formed by the choroid plexus. It is one of the internal barriers for the body to participate in i...

Claims

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Application Information

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IPC IPC(8): C07K5/103C07K7/06C07K7/08C07K1/02C07K1/04A61K47/42A61K47/64A61K45/00A61P25/00
CPCA61K45/00A61K47/42C07K5/1013C07K7/06C07K7/08
Inventor 黄秀举
Owner 天津博锐生物科技有限公司
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