Target degradation Bcr-Abl protein reagent and application of target degradation Bcr-Abl protein reagent in preparing Philadelphia chromosome positive tumor treatment medicine

A Philadelphia chromosome and bcr-abl technology, which is applied to a reagent for targeting degrading Bcr-Abl protein and its application in the preparation of a Philadelphia chromosome positive tumor treatment drug, and achieves the effects of inhibiting growth, good curative effect and difficult reversal.
CN102895221AInactive Publication Date: 2013-01-30SUN YAT SEN UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SUN YAT SEN UNIV
Publication Date
2013-01-30
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses an oridonin which can be used for treating Philadelphia chromosome positive tumor through degradation of Bcr-Abl fusion protein and relates to an application of the oridonin in preparing a Philadelphia chromosome positive tumor treatment medicine. A large number of studies show that the oridonin is capable of activating Bcr-Abl specific ubiquitination degradation ways and rapidly and efficiently degrading Bcr-Abl oncoprotein, and thereby Philadelphia chromosome positive tumor cells are subjected to remarkable growth inhibition and irreversible cell apoptosis. In a mouse body, the oridonin also can degrade the Bcr-Abl protein and remarkably inhibit growth of the Philadelphia chromosome positive tumor. The oridonin is mainly derived from rabdosia rubescens which is a traditional Chinese medicine and the oridonin has slight toxic effect on human body and is easy to prepare and high in applicability. Besides, the action mechanism of the oridonin is completely different from STI-571 (gleevec) which is a first-line medicine used for leukemia clinical treatment presently, and thereby the oridonin can be used as a potential medicine for treating STI-571 tolerant Philadelphia chromosome positive tumor.
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Description

technical field

[0001] The invention discloses a method and reagent for targeted degradation of Bcr-Abl protein and its application in the preparation of Ph-positive tumor treatment drugs, belonging to the technical fields of medicine, biochemistry and cell biology, and specifically relates to the application of oridonin in pharmaceuticals and In clinical treatment, target ubiquitination to degrade pathogenic protein Bcr-Abl and inhibit and kill Ph-positive tumor cells, as well as in clinical and basic research as an inducer to analyze the biological functions of Bcr-Abl and its related signaling pathways. Background technique

[0002] Tumor is the number one killer threatening human health. In 2008, there were 12.7 million new cancer patients and 7.6 million deaths worldwide, and these numbers are still growing. With the development of modern medicine, people have gradually realized that the formation of tumors is caused by gene mutations, and thus developed a variety of ...

Claims

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