Multifunctional cerebral neuron targeting polypeptide and its application in preparing medicine for treating Alzheimer's disease

A technology targeting polypeptides and brain neurons, which can be applied to nervous system diseases, fusion polypeptides, drug combinations, etc., can solve the problems of complex preparation, insufficient targeting efficiency, and high dosage, and achieve strong brain targeting and neural Meta-targeting, facilitating subsequent development and industrialization, and avoiding the effects of aggregation

Pending Publication Date: 2019-08-06
FUDAN UNIV
View PDF1 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to solve this problem, our research group constructed a cascade targeting nano-delivery system in the early stage. By simultaneously modifying the bifunctional groups (both polypeptides) targeting the BBB and neurons on the surface of the nano-system, it can improve the peptide / transfer ratio to a certain extent. The amount of gene medicine that penetrates the BBB and enters the central neurons improves the therapeutic effect on AD; however, the delivery system needs to modify two targeting peptides, which has disadvantages such as large dosage, complicated preparation, and insufficient targeting efficiency

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Multifunctional cerebral neuron targeting polypeptide and its application in preparing medicine for treating Alzheimer's disease
  • Multifunctional cerebral neuron targeting polypeptide and its application in preparing medicine for treating Alzheimer's disease
  • Multifunctional cerebral neuron targeting polypeptide and its application in preparing medicine for treating Alzheimer's disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The polypeptide TGN targeting the BBB and the polypeptide Tet1 targeting neurons are respectively connected via glycine (2-6) or histidine (1-4) to prepare multifunctional brain neuron-targeting polypeptides, respectively named as TGT1 and THT1; in the present invention, the peptide synthesis was completed by Hangzhou Zhongpei Biological Co., Ltd.

Embodiment 2

[0040] The BBB-targeted polypeptide Angiopep-2 and the neuron-targeted polypeptide Penetratin were connected via glycine (2-8) or alanine (1-5) respectively to prepare a multifunctional brain neuron-targeted polypeptide. Named as TGR and TAR; in the present invention, the peptide synthesis is completed by Hangzhou Zhongpei Biology Co., Ltd.

Embodiment 3

[0042] Link the head and tail of the neuron-targeting polypeptide TAxI to aspartic acid (D) and lysine (K) to form a cyclic peptide, and connect the BBB-targeting polypeptide mApoE to the aspartic acid end of the cyclic peptide, respectively. Linked by histidine (1 to 4) or alanine (2 to 6), the multifunctional brain neuron targeting polypeptide is prepared and named as CHS and CAS respectively; in the present invention, the polypeptide is synthesized by Hangzhou Zhongpei Bio Ltd. completed.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
The average particle sizeaaaaaaaaaa
The average particle sizeaaaaaaaaaa
Login to view more

Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to a multifunctional cerebral neuron targeting polypeptide and its application in preparing a medicine for treating Alzheimer's disease. The polypeptide of the present invention comprises a peptide chain X targeting a blood brain barrier and a peptide chain Y targeting neuron, which are connected by a flexiblepeptide chain L at middle, and a structure thereof is X-L-Y or Y-L-X. The polypeptide has greater brain targeting and neuronal targeting than the original single targeting peptide (X or Y), and a nano-delivery system linked to targeting polypeptide is used to deliver more drugs to a central neuron part, which greatly improves the therapeutic effect on Alzheimer's disease; the targeted modification is simpler and controllable, the dosage is reduced, and the economic cost is reduced, which has broad application prospects.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a polypeptide targeting brain neurons and its application in the preparation of drugs for treating Alzheimer's disease. Background technique [0002] The prior art discloses that Alzheimer's disease (AD) is the most common type of dementia, and its main clinical manifestations are progressive cognitive dysfunction, memory loss, and personality and behavior changes. According to statistics, with the aging of the population, the incidence of AD is increasing year by year. At present, there are about 47 million AD patients in the world. It is estimated that by 2050, the number of AD patients will reach 130 million. Due to the complex etiology and long course of AD (latency period as long as 10 to 25 years), when the clinical diagnosis is made, the apoptotic neurons in the brain tissue of the patient often fail to regenerate, so far there is still no e...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): C07K19/00A61K45/00A61P25/28
CPCC07K7/08C07K7/06C07K14/00C07K11/02A61K47/42A61K45/00C07K2319/00
Inventor 张奇志郭倩许舒婷杨鹏王鹏真钱康
Owner FUDAN UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products