Screening method and screening system for beta-secretase specific inhibitor

A screening method and specific technology, applied in the field of inhibitor screening methods and screening systems, can solve problems such as side effects, influence on normal processing, influence on activity, etc.
CN104880441AActive Publication Date: 2015-09-02安徽昊拓生物科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
安徽昊拓生物科技有限公司
Publication Date
2015-09-02

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Abstract

The invention discloses a screening system for a beta-secretase specific inhibitor. The system is a micro-micelle-APP system formed by encapsulating APP protein with a fluorescent label by a micro-micelle solution; the APP protein is amyloid precursor protein; the micro-micelle solution is prepared by adopting amphiphilic polymer molecule modified quantum dots; and the APP protein with the fluorescent label is prepared by carrying out fixed-point fluorescence labeling on the APP protein by utilizing an orthogonal reaction system. In addition, the invention also discloses a screening method for the beta-secretase specific inhibitor. According to the screening system and the screening method disclosed by the invention, BACE natural substrate molecules are used as targets, the condition that the screened medicine precursor molecules have accurate substrate specificity can be achieved, and sensitive real-time monitoring can be achieved.
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Description

technical field

[0001] The invention relates to an inhibitor screening method and its screening system, in particular to a beta-secretase (BACE) specific inhibitor screening method and its screening system. Background technique

[0002] A large amount of evidence has shown that the abnormal aggregation and deposition of amyloid (Aβ) in the central system is neurotoxic and can lead to the occurrence of Alzheimer's disease. Aβ is formed by the stepwise hydrolysis of amyloid precursor protein (APP protein) by β-secretase (BACE) and γ-secretase. Among them, BACE is the rate-limiting step of Aβ generation. Inhibitors against BACE are considered to be the most promising drugs for the treatment and prevention of Alzheimer's disease. Many pharmaceutical companies around the world are conducting fierce competition around the screening of BACE inhibitors. Through structural analysis and molecular design, people have obtained tens of thousands of compounds that are expected to be BA...

Claims

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