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LRPPRC (leucine rich pentatricopeptide repeat containing) negative regulating agent and application thereof

A technology of regulator and negative regulation, applied in aldehyde active ingredients, drug combinations, anti-tumor drugs, etc., can solve the problems of reducing the quality of life of patients, limited efficacy, etc., achieving simple administration, low price, and inhibition of tumor cells. effect of growth

Inactive Publication Date: 2019-06-21
INST OF CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this treatment method has limited curative effect, and most patients will eventually relapse. In addition, this method has very large side effects, which greatly reduces the quality of life of patients

Method used

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  • LRPPRC (leucine rich pentatricopeptide repeat containing) negative regulating agent and application thereof
  • LRPPRC (leucine rich pentatricopeptide repeat containing) negative regulating agent and application thereof
  • LRPPRC (leucine rich pentatricopeptide repeat containing) negative regulating agent and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Expression of LRPPRC in various tumors

[0028] The expression level of LRPPRC RNA in various tumor tissues and normal tissues was analyzed on the public database TCGA, from figure 1 It can be seen that it is significantly highly expressed in various tumors such as colon cancer, rectal cancer, esophageal cancer, lung cancer, lung adenocarcinoma, lung squamous cell carcinoma, pancreatic cancer, gastric cancer, breast cancer, and breast ductal carcinoma.

[0029] In order to provide an inhibitor that can specifically bind to tumor cells with high expression of LRPPRC, on the basis of a large number of experiments, the embodiments of the present invention have verified the specific binding of gossypol acetate (GAA) to LRPPRC from the following aspects:

Embodiment 2

[0031] High-throughput screening of LRPPRC small molecule inhibitor GAA

[0032] In this example, a high-throughput drug screening system based on nucleic acid aptamers is used to screen small molecules that can inhibit the binding function of LRPPRC and nucleic acid aptamers from a small molecule compound library containing 850 natural products. From figure 2 It can be seen that a total of 19 compounds can hinder the binding of LRPPRC to the nucleic acid aptamer. From image 3 It was seen that GAA exhibited a strong LRPPRC inhibitory function. The specific screening method is as follows:

[0033] 1) In vitro prokaryotic expression and purification of the RNA-binding region C-domain protein of LRPPRC;

[0034] 2) In vitro synthesis of fluorescein-labeled LRPPRC-specific aptamer R14-flu;

[0035] 3) Configure the complex system of LRPPRC and R14-flu, use PBS as the buffer, the concentration is LRPPRC (120ug / ml), R14-flu (40nM), in a black opaque 384-well plate, add 15ul t...

Embodiment 3

[0041] In this example, fluorescence titration and isothermal calorimetry were used to detect the direct combination of LRPPRC and GAA.

[0042] 1. Fluorescence titration assay for direct binding of GAA to LRPPRC protein

[0043] 1) In vitro prokaryotic expression and purification of the RNA-binding region C-domain protein (60ug / ml) of LRPPRC;

[0044] 2) The stock solution concentration of GAA is configured to be 50mM;

[0045] 3) Add concentration gradients of GAA to the LRPPRC protein solution, respectively 0, 0.25, 0.5, 1.0, 2.0, 4.0, 8.0, 16, 32uM;

[0046]4) FLS980fluorescence spectrometer (Edinburgh Instruments, Ltd.) was used to detect the change of fluorescence value of LRPPRC protein in the 300-380nm band. Draw the fluorescence spectrum changes of LRPPRC protein under different GAA concentrations, specifically as Figure 4 shown, from Figure 4 It can be seen that with the increase of GAA concentration, the autofluorescence of LRPPRC protein gradually decreases. ...

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Abstract

The embodiment of the invention discloses an LRPPRC negative regulating agent and application thereof. According to the implementation manner of the LRPPRC negative regulating agent, compared with theprior art, high-expression LRPPRC in tumor cells is taken as a therapeutic target, gossypol acetate is taken as a targeted therapeutic drug, and through specific binding of the therapeutic target andthe targeted therapeutic drug, the aim of inhibiting growth of the tumor cells can be achieved; meanwhile, the gossypol acetate is a clinically applicable compound, so that the LRPPRC negative regulating agent is high in safety, simple in mode of administration, wide in raw material resource, low in price and capable of reducing the treatment costs for the patient.

Description

technical field [0001] The embodiment of the present invention relates to the field of biotechnology, in particular to a LRPPRC negative regulator and its application. Background technique [0002] Cancer is a major disease that causes human death, and the number of deaths due to cancer is about 7 million worldwide every year. Due to the lack of early cancer diagnosis and screening technology at this stage, a large number of cancer patients are already in the advanced stage of tumor when they first see a doctor, and they have lost the chance of surgical resection and cure. Chemotherapy and radiotherapy are still the main treatment methods for advanced tumors at this stage. However, this treatment method has limited efficacy, and most patients will eventually relapse. In addition, this method has very large side effects, which greatly reduces the quality of life of patients. [0003] Targeted tumor therapy is aimed at functional molecules specifically expressed by tumors, a...

Claims

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Application Information

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IPC IPC(8): A61K31/11A61P35/00
CPCA61K31/11A61P35/00
Inventor 方晓红周卫宋咏梅徐丽
Owner INST OF CHEM CHINESE ACAD OF SCI
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