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Application of small-molecule inhibitor to preparation of antitumor medicine

A technology of small molecule inhibitors and anti-tumor drugs, which can be used in the field of biomedicine to solve problems such as toxic side effects and inability to distinguish tumor cells.

Active Publication Date: 2021-02-02
XINXIANG MEDICAL UNIV
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  • Abstract
  • Description
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Problems solved by technology

Although traditional anticancer drugs have certain clinical efficacy, they can cause serious toxic and side effects because they cannot distinguish tumor cells from normal body cells

Method used

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  • Application of small-molecule inhibitor to preparation of antitumor medicine
  • Application of small-molecule inhibitor to preparation of antitumor medicine
  • Application of small-molecule inhibitor to preparation of antitumor medicine

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Embodiment Construction

[0016] In order to make the purpose and technical solution of the present invention clearer, the present invention will be further described below in conjunction with the examples, but the implementation of the present invention is not limited thereto. The experimental methods and unspecified recipes in the examples are all in accordance with conventional conditions, such as the conditions described in the Experimental Tutorial of Medical Biochemistry and Molecular Biology, 2011 edition, Higher Education Press.

[0017] In the present invention, 16 potential small-molecule inhibitors of ID2 are initially obtained through virtual screening of pharmacophore modeling. Subsequent in vitro cell tests were carried out to test the biological activity of 16 candidate small molecule compounds, and the results showed good water solubility and inhibitory IC for glioma growth. 50 A better small molecule compound is named AK778 / 43420895, and the affinity between it and ID2 protein is deter...

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Abstract

The invention belongs to the field of biological medicines, and particularly relates to a differentiation inhibition factor 2, namely an ID2 inhibitor, and an application of the inhibitor to preparation of brain glioma medicines. According to the research, an effective ID2 inhibitor is obtained through a computer pharmacophore virtual screening technology and CCK-8 cytotoxicity experiment. Throughdetection by a surface plasmon resonance technology, the inhibitor is found to have high affinity with ID2. In-vitro and in-vivo experiments show that the inhibitor can reduce the expression of the ID2 in glioma and significantly inhibit the proliferation of glioma cells, and has potential clinical application prospects.

Description

technical field [0001] The invention belongs to the field of biomedicine. Specifically, the invention relates to a differentiation inhibitor 2, ie ID2 inhibitor, and its application in the preparation of glioma drugs. Background technique [0002] Malignant glioma, represented by glioblastoma (GBM), lacks effective treatment methods. The current treatment options are still based on traditional surgery and radiotherapy and chemotherapy, with severe side effects. The tumor recurrence rate exceeds 90%, and the median survival period of patients is only about one year. Because glioma has abundant new blood vessels to support its invasive growth, the effect of surgical treatment is not ideal. Therefore, finding potential targets that play a key role in the progression of glioma has important clinical and practical significance. [0003] Chemotherapy drugs currently approved by the FDA for the treatment of malignant glioma include Temozolomide (Temozolomide, TMZ) and Bevacizumab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61P35/00
CPCA61K31/4439A61P35/00
Inventor 钟根深王怡春吴敏娜林斌黄毓杰齐劲松
Owner XINXIANG MEDICAL UNIV
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