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Small-molecule inhibitor YAP1-Y7 for YAP1, and application thereof

A YAP1-Y7, small molecule inhibitor technology, applied in the field of molecular targeted therapy, can solve the problems of high phototoxicity, easy decomposition under light exposure, low affinity, etc., and achieve high selective specificity, strong pertinence, and strong affinity. Effect

Active Publication Date: 2021-10-01
THE FIRST HOSPITAL OF CHINA MEDICIAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of VP as an inhibitor of YAP1 has some disadvantages: it is an inflammatory photosensitizer and therefore highly phototoxic; it is easily decomposed and unstable when exposed to light; VP has a low affinity for YAP1, at the micromolar level
There are currently no small molecule inhibitors of YAP1 on the market

Method used

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  • Small-molecule inhibitor YAP1-Y7 for YAP1, and application thereof
  • Small-molecule inhibitor YAP1-Y7 for YAP1, and application thereof
  • Small-molecule inhibitor YAP1-Y7 for YAP1, and application thereof

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Embodiment Construction

[0022] The specific implementation manners of the present invention will be further described in detail below in conjunction with the accompanying drawings and examples. The following examples illustrate the invention in detail, but are not intended to limit the scope of the invention. This embodiment adopts conventional experimental techniques, which are familiar to those skilled in the art, and can be carried out according to the instructions provided by the material manufacturer according to this embodiment.

[0023] Example.

[0024] 1. Experimental materials.

[0025] 1.1 Cell lines.

[0026] Human gastric cancer cell line MGC-803, tool cell line HEK293T.

[0027] 1.2 Experimental reagents.

[0028] DMEM medium, RPMI-1640 medium, trypsin, fetal bovine serum, 0.5% crystal violet, CCK8 reagent.

[0029] 2. Experimental method.

[0030] 2.1 MOE software for drug screening.

[0031] Firstly, the specific structure (5oaq) of YAP1 protein was obtained in the PDB library,...

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Abstract

The invention belongs to the field of molecular targeted therapy, and particularly relates to a small molecule inhibitor YAP1-Y7 for Yes-associated protein 1 (YAP1), and application thereof in tumor treatment. The chemical structural formula of the small-molecule inhibitor YAP1-Y7 for YAP1 is shown in the specification. The small-molecule inhibitor can inhibit YAP1, and a YAP1-TEAD compound is reduced by inhibiting the YAP1, so that the effect of inhibiting tumor cell proliferation is achieved. The small-molecule inhibitor is applied to preparation of drugs for treating gastric cancer. Compared with a known inhibitor, the small-molecule inhibitor for YAP1 provided by the invention has strong affinity. The small-molecule inhibitor for YAP1 can be used as a novel anti-tumor drug to thoroughly remove tumors and stem cells, and has a wide application prospect.

Description

technical field [0001] The invention belongs to the field of molecular targeted therapy, and in particular relates to YAP1-Y7, a small molecule inhibitor of Yes-associated protein 1 (YAP1), and its application in treating tumors. Background technique [0002] Malignant tumors seriously threaten human life and health. At present, malignant tumors have surpassed cardiovascular and cerebrovascular diseases and become the disease with the highest mortality rate. The occurrence and development of tumor is an extremely complicated process, involving the abnormal expression of various proteins. Today, many small-molecule inhibitors targeting abnormal protein expression have been marketed, such as EGFR-targeting small-molecule drugs gefitinib and enlotinib. These small molecule inhibitor drugs have achieved great success in the global molecularly targeted antineoplastic drug market. [0003] The Hippo signaling pathway is involved in organ growth, developmental control, tissue gr...

Claims

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Application Information

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IPC IPC(8): C07D207/44A61K31/40A61P35/00
CPCC07D207/44A61P35/00
Inventor 刘晓芳
Owner THE FIRST HOSPITAL OF CHINA MEDICIAL UNIV
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