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Application of histone deacetylase inhibitor in preparation of medicine for treating heart disease

A deacetylase and histone technology, which can be used in drug combinations, cardiovascular system diseases, pharmaceutical formulations, etc., can solve the lack of treatment methods, and has not yet seen histone deacetylase inhibitors in the treatment of heart disease and DMD deficiency. Cardiomyopathy, etc.

Pending Publication Date: 2022-04-12
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, there is no effective treatment for DMD-deficient cardiomyopathy caused by CDK13 mutations
There is no report on the treatment of heart disease with histone deacetylase inhibitors

Method used

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  • Application of histone deacetylase inhibitor in preparation of medicine for treating heart disease
  • Application of histone deacetylase inhibitor in preparation of medicine for treating heart disease
  • Application of histone deacetylase inhibitor in preparation of medicine for treating heart disease

Examples

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Embodiment Construction

[0052] The present invention will be further described below in conjunction with embodiment. However, the scope of the present invention is not limited to the following examples. Those skilled in the art can understand that various changes and modifications can be made in the present invention without departing from the spirit and scope of the present invention.

[0053] The instruments, reagents, materials, etc. involved in the following examples, unless otherwise specified, are conventional instruments, reagents, materials, etc. in the prior art, and can be obtained through formal commercial channels. The experimental methods, detection methods, etc. involved in the following examples, unless otherwise specified, are conventional experimental methods, detection methods, etc. in the prior art.

[0054] Experiment 1 Construction and study of CDK13 myocardial induced deletion mouse model

[0055] (1) Construction of CDK13 knockout mouse model: exon 3 (exon3) and exon 4 (exon4...

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Abstract

The invention discloses application of a histone deacetylase inhibitor in preparation of a medicine for treating heart diseases, and belongs to the technical field of medical application of compounds. A mouse model with CDK13 knocked out of myocardium is constructed, and it is confirmed that deficiency of CDK13 in myocardium can cause cardiac dysfunctions such as dilated cardiomyopathy and heart failure; a molecular mechanism that CDK13 causes cardiomyopathy by regulating down-regulation of DMD gene expression is found. A histone deacetylase inhibitor No.1217 (the molecular formula of the histone deacetylase inhibitor No.1217 is C24H27N3O4) is used for performing drug treatment on a myocardial knockout CDK13 mouse, and the result shows that after continuous administration is performed for one month, the cardiac function, the cardiac fibrosis pathological process and the dystrophy protein level of the myocardial knockout CDK13 mouse are partially reversed. The invention finds an effective molecule and a treatment strategy for treating cardiomyopathy by targeting CDK13, and has important significance for treating heart disease.

Description

technical field [0001] The invention relates to the application of histone deacetylase inhibitors in the preparation of medicines for treating heart diseases, and belongs to the technical field of medical applications of compounds. Background technique [0002] Heart disease is a devastating disease, clinically manifested as heart failure and cardioembolism, characterized by interstitial fibrosis, atrioventricular remodeling, decreased ventricular compliance, and decreased blood flow. A large proportion of adult heart disease patients are due to the loss of heart muscle function caused by protein inactivation caused by gene mutations. [0003] In a study on developmental disorders in 2016, it was found that the new mutation of CDK13 protein (cyclin-dependent kinase 13, cyclin-dependent kinase 13) was closely related to the pathogenesis of human congenital heart defect syndrome. In these discovered children, except CDK13 new mutations, no other known pathogenic gene mutation...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/216A61P9/00A61P9/04
Inventor 孙方霖常建锋
Owner TONGJI UNIV
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