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PD-1/PD-L1 inhibitor and application thereof

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

Active Publication Date: 2021-02-19
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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  • PD-1/PD-L1 inhibitor and application thereof
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  • PD-1/PD-L1 inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] A preparation method of S-cyanomethyl-L-cysteine ​​(SCC), comprising the following steps:

[0038] 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;

[0039] 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

[0041] A preparation method of S-cyanomethyl-L-cysteine ​​(SCC), comprising the following steps:

[0042] 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;

[0043] 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

[0045] A preparation method of S-cyanomethyl-L-cysteine ​​(SCC), comprising the following steps:

[0046] 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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PUM

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Abstract

The invention relates to the field of molecular immunology, and particularly discloses a PD-1 / PD-L1 inhibitor and application thereof. The PD-1 / PD-L1 inhibitor comprises S-cyanomethyl-L-cysteine, activation of lymphocytes is promoted by releasing H2S, PD-1 gene expression is down-regulated, and PD-L1 gene expression of liver cancer cells is down-regulated, so that a PD-1 / PD-L1 pathway is inhibited, cancer cell immune escape reaction is blocked, the immune response capacity of the lymphocytes to HepG2 cells is enhanced, the inhibition effect of the lymphocytes on the liver cancer cells is enhanced, the immune function of mice is also enhanced, and the cancer inhibition effect of quinoline derivatives of a tumor targeted drug N isostere tectoridin can also be effectively enhanced.

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, radiotherapy, 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 time,...

Claims

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Application Information

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IPC IPC(8): A61K31/277A61K31/47A61P35/00A61P1/16C07C319/14C07C323/58
CPCA61K31/277A61K31/47A61P35/00A61P1/16C07C319/14A61K2300/00C07C323/58
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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