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A small molecule inhibitor yap1-y7 against yap1 and its application

A YAP1-Y7, small molecule inhibitor technology, applied in the direction of heterocyclic compound active ingredients, organic chemistry, anti-tumor drugs, etc., can solve the problems of high phototoxicity, easy decomposition when exposed to light, low affinity, etc., and achieve high selectivity and specificity. Sexual, targeted and affinity effects

Active Publication Date: 2022-07-01
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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  • A small molecule inhibitor yap1-y7 against yap1 and its application
  • A small molecule inhibitor yap1-y7 against yap1 and its application
  • A small molecule inhibitor yap1-y7 against yap1 and its application

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Embodiment Construction

[0022] The specific embodiments of the present invention will be described in further detail below with reference to 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 performed according to the description 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 of YAP1 protein (5oaq) was obtained in the PDB library, and after the s...

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Abstract

The invention belongs to the field of molecular targeted therapy, and in particular relates to a small molecule inhibitor YAP1-Y7 of Yes-associated protein 1 (Yes-associated protein 1, YAP1) and its application in the treatment of tumors. A small molecule inhibitor YAP1-Y7 against YAP1, the chemical structural formula of the small molecule inhibitor YAP1-Y7 is: The small molecule inhibitor can inhibit YAP1, and by inhibiting YAP1, the YAP1-TEAD complex is reduced, thereby inhibiting the effect of tumor cell proliferation. The application of the small molecule inhibitor in the preparation of a medicament for the treatment of gastric cancer. Compared with the known inhibitors, the small molecule inhibitor against YAP1 provided by the present invention has a strong affinity. It can be used as a new anti-tumor drug to completely remove tumor and stem cells, and has broad application prospects.

Description

technical field [0001] The invention belongs to the field of molecular targeted therapy, in particular to YAP1-Y7, a small molecule inhibitor of Yes-associated protein 1 (Yes-associated protein 1, YAP1) and its application in the treatment of 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 tumors is an extremely complex process involving the abnormal expression of various proteins. Today, many small-molecule inhibitor drugs targeting abnormal protein expression have been launched, such as EGFR-targeting small-molecule drugs gefitinib and erlotinib. These small molecule inhibitor drugs have achieved great success in the global molecularly targeted antitumor drug market. [0003] Hippo signaling pathway is involved in organ growth, control of developm...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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