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A kind of PD-1/PD-L1 inhibitor and application thereof

A technology of PD-L1 and PD-1, applied in the field of molecular immunology, to achieve the effect of inhibiting proliferation, enhancing immune response ability, and improving tumor suppressor effect

Active Publication Date: 2022-02-18
GUANGZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, there are relatively few studies and applications of PD-1 / PD-L1 inhibitors in clinical trials for liver cancer, so there is still room for improvement

Method used

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  • A kind of PD-1/PD-L1 inhibitor and application thereof
  • A kind of PD-1/PD-L1 inhibitor and application thereof
  • A kind of PD-1/PD-L1 inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A preparation method of S-cyanomethyl-L-cysteine ​​(SCC), comprising the following steps:

[0039] S1. Take 200mg of L-cysteine ​​with a mass concentration of 1.65mmol as the raw material and dissolve it in 2mL of NH with a mass concentration of 2M 4 OH solution, stir the mixture, the stirring temperature is -10°C, and the stirring time is 30min;

[0040] S2. Add dropwise 218 mg of 2-bromoacetonitrile with a mass concentration of 1.82 mmol in the mixture, stir overnight, concentrate and filter under a vacuum of 0.08 MPa, wash the filtrate with ethanol, and then use water with a volume ratio of 1:2 - Recrystallization from ethanol solution to obtain S-cyanomethyl-L-cysteine ​​as a pale yellow solid.

Embodiment 2

[0042] A preparation method of S-cyanomethyl-L-cysteine ​​(SCC), comprising the following steps:

[0043] S1. Take 200mg of L-cysteine ​​with a mass concentration of 1.65mmol as the raw material and dissolve it in 2mL of NH with a mass concentration of 2M 4 OH solution, stir the mixture, the stirring temperature is 10°C, and the stirring time is 30min;

[0044] S2. Add dropwise 218 mg of 2-bromoacetonitrile with a mass concentration of 1.82 mmol into the mixture, stir overnight, concentrate and filter under a vacuum of 0.08 MPa, wash the filtrate with ethanol, and then use water with a volume ratio of 3:4 - Recrystallization from ethanol solution to obtain S-cyanomethyl-L-cysteine ​​as a pale yellow solid.

Embodiment 3

[0046] A preparation method of S-cyanomethyl-L-cysteine ​​(SCC), comprising the following steps:

[0047] S1. Take 200mg of L-cysteine ​​with a mass concentration of 1.65mmol as the raw material and dissolve it in 2mL of NH with a mass concentration of 2M 4 In the OH solution, stir the mixture, the stirring temperature is 0°C, and the stirring time is 30min; S2. Add 218mg of 2-bromoacetonitrile with a mass concentration of 1.82mmol dropwise to the mixture, stir overnight, and concentrate under the condition of a vacuum of 0.08MPa and filtered, the filtrate was washed with ethanol, and then recrystallized from a water-ethanol solution with a volume ratio of 2:2 to obtain S-cyanomethyl-L-cysteine ​​as a pale yellow solid.

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Abstract

The invention relates to the field of molecular immunology, and specifically discloses a PD-1 / PD-L1 inhibitor and its application. The PD-1 / PD-L1 inhibitors of the present invention include S-cyanomethyl-L-cysteine, which releases H 2 S promotes the activation of lymphocytes, down-regulates the expression of PD-1 gene, and down-regulates the expression of PD-L1 gene in liver cancer cells, thereby inhibiting the PD-1 / PD-L1 pathway, blocking the immune escape response of cancer cells, and enhancing the response of lymphocytes to HepG2 The immune response ability of cells has enhanced the inhibitory effect of lymphocytes on liver cancer cells, and also enhanced the immune function of mice, and can also effectively enhance the tumor suppressor effect of quinoline derivatives of tumor-targeting drugs N-electron isostere irisin .

Description

technical field [0001] The present invention relates to the field of molecular immunology, in particular to a PD-1 / PD-L1 inhibitor and its application. Background technique [0002] Primary liver cancer (PHC) is a malignant tumor caused by liver cells or intrahepatic bile duct epithelial cells. In 2012, the death rate of liver cancer in my country ranked third among malignant tumors. Therefore, how to effectively treat PHC has very important clinical significance. At present, the treatment of PHC can be divided into surgical treatment and non-surgical treatment. Surgical treatment includes liver transplantation and liver resection, and non-surgical treatment includes hepatic arterial chemoembolization, radiofrequency ablation, radiation therapy, systemic chemotherapy, and biological therapy. and Chinese medicine treatment. Among them, molecular targeted therapy has attracted people's attention due to its strong targeting and good curative effect. However, after a period of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/277A61K31/47A61P35/00A61P1/16C07C319/14C07C323/58
CPCA61K31/277A61K31/47A61P35/00A61P1/16C07C319/14
Inventor 陈鲲蔡银怡樊静李文甫蔺佳雨许洁虹杜俊熹吕鹏程
Owner GUANGZHOU UNIVERSITY
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