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Application of PERK inhibitor to preparation of synergist of liver cancer medicine

A technology of inhibitors and multi-kinase inhibitors, applied in the field of liver cancer, can solve the problems of limited therapeutic effect of liver cancer, single immune method, unsatisfactory anti-liver cancer treatment effect, etc.

Active Publication Date: 2021-05-18
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the efficacy of anti-PD-1 / PD-L1 therapy in HCC patients is still limited
[0004] The above clinical anti-liver cancer treatments are not effective, and can only prolong the survival time of patients with advanced liver cancer by about 3 months
Directly acting on tumors with targeted drugs is not effective in the treatment of liver cancer, ignoring the role of the body's immune system in the development of tumors
[0005] At present, the anti-PD-1 / PD-L1 immune method for liver cancer is too single, so the curative effect is limited. It is necessary to find other immunotherapy targets to improve the effect of anti-tumor therapy
The effect of single therapy on liver cancer is very limited, and it is necessary to explore the combination of immune and targeted therapy to improve the curative effect

Method used

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  • Application of PERK inhibitor to preparation of synergist of liver cancer medicine
  • Application of PERK inhibitor to preparation of synergist of liver cancer medicine
  • Application of PERK inhibitor to preparation of synergist of liver cancer medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Establishment of mouse liver orthotopic tumor transplantation model

[0035] 1. Experimental method

[0036] 1. The cell line used to establish liver orthotopic tumor transplantation in this experiment was Hepa1-6-Luciferase, cultured in DMEM medium + 10% fetal bovine serum (both purchased from Thermo Fisher Scientific Company), 37°C, 5% CO 2 cultured to the 3rd passage, harvested cells, and used for liver tumor formation in situ;

[0037] 2. Put 7.5×10 5 Hepa1-6-Luciferase cells were mixed with 50% Matrigel (purchased from Trevigen, product number: 3432-001-01) to prepare a cell suspension, and then transplanted the cell suspension into the left lobe of the liver of C57B / L6 mice Subcapsular;

[0038] 3. On the 5th day after bearing the tumor, the mice were divided into groups and administered with medication. The experimental grouping and administration methods are shown in Table 1:

[0039] Table 1 Experimental grouping of mice with C57B / L6 liver orthoto...

Embodiment 2

[0051] Example 2 Establishment of subcutaneous liver cancer tumor model in NOD-SCID mice

[0052] 1. Experimental method

[0053] 1. The cell line used to establish liver orthotopic tumor transplantation in this experiment was Hepa1-6, cultured in DMEM medium + 10% fetal bovine serum (both purchased from Thermo Fisher Scientific Company), 37°C, 5% CO 2 In the system, cultured to the third generation, harvested cells, used for subcutaneous tumor formation;

[0054] 2. Put 7.5×10 5 Hepa1-6 was prepared into a cell suspension and injected subcutaneously into the right leg of NOD-SCID mice. On the 3rd day after bearing the tumor, the mice were divided into groups and administered for treatment. The experimental groups and administration methods are shown in Table 2 .

[0055] Table 2 Grouping of NOD-SCID mice anti-tumor therapy experiments:

[0056]

[0057] 3. From the 7th day, the tumor size of the mice was measured every 4 days. The length and width of the tumor were me...

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Abstract

The invention discloses an application of a PERK inhibitor to preparation of a synergist of a liver cancer medicine. By researches, the following case is found that PERK is a target for liver cancer treatment, blockage of PERK activation through a small molecule compound is a new strategy of anti-liver cancer immunotherapy, which uses tumor-related spleen as a target spot, and the PERK has clinical application value. The invention shows that the PERK inhibitor GSK2606414 takes an anti-tumor effect by acting on an immune system in the spleen of a mouse suffering from liver cancer. Moreover, the PERK inhibitor GSK2606414 can significantly and synergistically enhance the liver cancer treatment effect of an anti-PD-1 / PD-L1 antibody and Lenvatinib, and can be used as a novel liver cancer treatment drug for treating the liver cancer or enhancing the curative effect.

Description

technical field [0001] The invention relates to the technical field of liver cancer, in particular to the application of PERK inhibitors in the preparation of synergists for liver cancer drugs. Background technique [0002] Primary hepatocellular carcinoma (hepatocellular carcinoma for short) is a common malignant tumor in the world, and its morbidity and mortality rank the sixth and third respectively, while China is a high-incidence area of ​​liver cancer. In recent years, the incidence of liver cancer has a rising trend, seriously endangering human health and life safety. At present, the clinical treatment options for liver cancer are very limited. For unresectable liver cancer, targeted drugs are usually used to directly act on the tumor to prolong the life of advanced patients, but the treatment effect is not satisfactory. However, in the tumor body, the immune system also plays a vital role in the progression of tumors, and new anti-tumor treatments targeting the immu...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K39/395A61K31/47A61K31/519A61K45/06A61P35/00
CPCA61K45/00A61K39/39558A61K31/47A61K31/519A61K45/06A61P35/00A61K2300/00
Inventor 郑利民刘明宇吴翀
Owner SUN YAT SEN UNIV
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