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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.

Active Publication Date: 2015-09-02
安徽昊拓生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This will inevitably cause these inhibitors to block the production of Aβ while affecting the normal processing of other substrates by BACE
Or affect the activity of other proteases of the same family as BACE
These can cause serious side effects

Method used

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  • Screening method and screening system for beta-secretase specific inhibitor
  • Screening method and screening system for beta-secretase specific inhibitor
  • Screening method and screening system for beta-secretase specific inhibitor

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Experimental program
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Embodiment

[0075] The general implementation of the embodiment of the present invention is as figure 1 Shown: the use of amphoteric quantum dots mixed with liposomes to form a micromicelle system. And the fluorescent site-labeled APP protein is packaged. Fluorescent resonance energy transfer can be formed between the fluorescent labeling group of the APP protein and the quantum dots, and this resonance will disappear with the enzymatic cleavage of the APP protein by BACE. Therefore, the influence of the compound on the activity of BACE can be detected by the change of the fluorescence intensity in the system. The specific steps include the following:

[0076] (1) Synthesis of micellar solutions with quantum dots modified with amphiphilic polymer molecules; refer to the literature (YK Lee, J M Jeong, et al, Nanoparticles Modified by Encapsulation of Ligands with a Long Alkyl Chain to Affect Multispecific and Multimodal Imaging J Nucl Med 2012;53:1462–1470)

[0077] 1. Oil phase synth...

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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.

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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Application Information

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IPC IPC(8): G01N21/64
Inventor 汪弋郑莉
Owner 安徽昊拓生物科技有限公司
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