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Small peptide TAT-AKPD for treating ischemic brain injury and application of small peptide TAT-AKPD

A TAT-AKPD, ischemic brain injury technology, applied in the field of biomedicine, can solve problems such as ineffective treatment of neuron damage, and achieve the effects of facilitating drug delivery, reducing cell apoptosis, and ensuring effectiveness

Active Publication Date: 2020-06-19
XUZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] From the above discussion, it can be seen that many neuroprotective drugs in clinical practice cannot effectively treat neuronal damage caused by stroke.

Method used

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  • Small peptide TAT-AKPD for treating ischemic brain injury and application of small peptide TAT-AKPD
  • Small peptide TAT-AKPD for treating ischemic brain injury and application of small peptide TAT-AKPD
  • Small peptide TAT-AKPD for treating ischemic brain injury and application of small peptide TAT-AKPD

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Embodiment 1

[0020] The small peptide TAT-AKPD used in the examples of the present invention for the treatment of ischemic brain injury is designed based on the binding and nitrosylation between Procaspase-7 and XIAP, and its sequence is: H-YGRKKRRQRRR-AKPD-OH , SEQ ID NO.1.

[0021]After cerebral ischemia, endogenous Procaspase-7 undergoes denitrosylation and hydrolysis activation, leading to cell apoptosis. The activity of caspases is regulated by the inhibitor of apoptosis protein family (Inhibitors of apoptosis, IAPs), among which the X-linked inhibitor of apoptosis protein (XIAP) directly binds to Procaspase-7 through its BIR domain. and inhibit its activity. After cerebral ischemia, XIAP undergoes nitrosylation, thereby inhibiting its own anti-apoptotic activity.

[0022] According to the amino acid sequence of the binding site between Procaspase-7 and XIAP, a small peptide TAT-AKPD was designed. The four amino acids of AKPD on Procaspase-7 constitute a motif, which is responsible ...

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Abstract

The invention discloses a small peptide TAT-AKPD for treating ischemic brain injury and an application of the small peptide TAT-AKPD. The complete sequence of the small peptide TAT-AKPD is H-YGRKKRRQRRR-AKPD-OH. After the small peptide TAT-AKPD disclosed by the invention is used, combination of XIAP and Procaspase-7 can be reduced, nitrosylation transformation of the Procaspase-7 and the XIAP as well as Procaspase-7 activation can be alleviated, and finally cerebral ischemia induced apoptosis is alleviated. In addition, TAT can directly introduce fused small peptide into cells, so that the wayproblem that medicines enter the cell is solved, and medicine administration is convenient. Finally, the small peptide TAT-AKPD does not have immunogenicity and cannot enable organisms to produce immune reactions, so that side effects are reduced, and validity of medicine administration for two times or more is guaranteed.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to a small peptide TAT-AKPD for treating ischemic brain injury and its application. Background technique [0002] Stroke is one of the top three causes of death worldwide. Among them, ischemic stroke is the main type of stroke, which has the characteristics of high disability rate and high mortality rate. With the aging of the population and the increase of various risk factors, the proportion of ischemic stroke is still increasing. Ischemic stroke (stroke) includes cerebral thrombosis, lacunar infarction, and cerebral embolism, accounting for about 70% of all strokes. A large number of neurons die during a stroke, causing irreversible damage to neurons, and the neurological sequelae left after a stroke will seriously affect the quality of life of patients. [0003] The existing drugs for the treatment of ischemic brain injury mainly include drugs for improving cerebral circula...

Claims

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Application Information

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IPC IPC(8): C07K5/103A61K38/07A61K47/64A61P9/10
CPCA61K38/07A61K47/645A61P9/10C07K5/1008C07K2319/10
Inventor 胡书群姚君伟燕宪亮吕兰欣韩东颜晓庆杨红宁
Owner XUZHOU MEDICAL UNIV
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