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Anti-pulmonary fibrosis application of DDR2 small-molecule inhibitor

A technology of small molecule inhibitors and pulmonary fibrosis, which is applied in the field of application of DDR2 small molecule inhibitors in the preparation of anti-pulmonary fibrosis drugs, can solve the problem of no breakthrough in early prevention and treatment, unclear exact mechanism of pulmonary fibrosis, There are no reports on the application of small molecule inhibitors of DDR2 to achieve the effect of alleviating pulmonary fibrosis and improving the condition of pulmonary fibrosis

Inactive Publication Date: 2015-04-08
FOURTH MILITARY MEDICAL UNIVERSITY
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Problems solved by technology

At present, the exact mechanism of pulmonary fibrosis is still unclear, and there has been no breakthrough in early prevention and treatment
There is no report on the application of DDR2 small molecule inhibitors in pulmonary fibrosis

Method used

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  • Anti-pulmonary fibrosis application of DDR2 small-molecule inhibitor
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  • Anti-pulmonary fibrosis application of DDR2 small-molecule inhibitor

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Embodiment Construction

[0034] The present invention will be further described in detail below in conjunction with specific embodiments, which are explanations of the present invention rather than limitations.

[0035] The pathological and physiological changes of the pulmonary fibrosis model made with bleomycin are similar to those of human pulmonary fibrosis, so it has become a common drug for pulmonary fibrosis modeling. Bleomycin administered by intranasal instillation can induce pulmonary fibrosis in C57 mice, and the control is C57 mice administered by intranasal instillation of PBS.

[0036] 1. Identification of DDR2 small molecule inhibitor D856

[0037] 1.1 The DDR2 small molecule inhibitor D856 was developed by the research group of Professor Ding Ke, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences. The chemical structure of D856 is as follows:

[0038]

[0039] 1.2 In order to verify the targeting of the inhibitor D856, the present invention uses the kinase s...

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Abstract

The invention discloses an anti-pulmonary fibrosis application of a DDR2 small-molecule inhibitor, belonging to the technical field of biological medicines. In a DDR2 gene deletion mouse model, the pulmonary fibrosis condition can be remarkably improved through D856 in case of simultaneously giving bleomycin and the DDR2 small-molecule inhibitor D856; even in a homozygous mouse for restoring expressing DDR2, the inhibitor also can achieve the effect of relieving pulmonary fibrosis. On cell lever, the inhibitor D856 is added to lower the content of alpha-SMA. In an experiment of giving an inhibitor within different days, the pulmonary fibrosis also can be remarkably relieved even the inhibitor D856 is given from the 14th day, and the same result is obtained by verifying the small interference RNA of DDR2. The experimental results sufficiently support of the application of the DDR2 small-molecule inhibitor D856 to preparing an anti-pulmonary fibrosis drug and / or a health product.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, relates to the field of prevention and treatment of pulmonary fibrosis, and specifically relates to the application of DDR2 small molecule inhibitors in the preparation of anti-pulmonary fibrosis drugs. Background technique [0002] Various types of pulmonary fibrosis (pulmonary fibrosis, PF) are characterized by fibroblast (fibroblast, Fb) proliferation and a large number of extracellular matrix (ECM) accumulation. Various factors can cause pulmonary fibrosis, such as occupational dust (SiO 2 etc.), radiation injury and certain drugs (bleomycin), etc., in addition to a type of pulmonary fibrosis of unknown etiology - idiopathic pulmonary fibrosis (IPF). Although the causes are different, the development and outcome of fibrosis are basically similar, that is, it starts with the infiltration of inflammatory cells in the lower respiratory tract, and gradually causes damage to alveolar epitheli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61P11/00
CPCA61K31/519
Inventor 苏金丁克赵虎药立波卜歆任小梅陆小云于江天王德平
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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