Pharmaceutical application of polyribonucleotide nucleoside transferase 1 inhibitor
A technology of inhibitors and drugs, applied in the field of biomedicine, can solve the problems of no PNPT1, no PNPT1 inhibitor for anti-tumor and other problems
Active Publication Date: 2022-07-08
CHINA PHARM UNIV
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At present, there are very few studies on PNPT1 in tumors, and there are no PNPT1 inhibitors
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Abstract
The invention discloses a pharmaceutical application of a polyribonucleotide nucleoside transferase 1 inhibitor. According to the invention, active small molecules capable of inhibiting PNPT1 protein functions are screened out, and the effectiveness of the active small molecules of PNPT1 is represented by the level of dsRNAs in cytoplasm. The compound chemdiv ID: G756-0627 is screened out from active small molecules through JS2 staining of dsRNAs in cytoplasm, and the compound chemdiv ID: G756-0627 is screened out from the active small molecules. Western Blot is used for investigating that an active small molecule can inhibit the expression of PNPT1, and CCK-8 and Annexin V/PI staining are used for detecting cell proliferation and apoptosis; besides, through verification on nude mice with A549 transplanted tumors, the growth of tumors can be effectively inhibited by giving the active small molecule NO.G756-0627 to the mice, so that the anti-tumor effect is achieved.
Description
technical field [0001] The invention belongs to the technical field of biomedicine, in particular to the pharmaceutical application of a polyribonucleotide nucleoside transferase 1 inhibitor. Background technique [0002] Lung cancer is one of the malignant tumors with the highest morbidity and mortality in the world. In 2020, there will be 2.2 million new cases of lung cancer worldwide and 1.8 million deaths. China is the country with the largest number of new lung cancers and deaths in the world. In 2020, there were 820,000 new lung cancer cases and 710,000 deaths in China. To make matters worse, the incidence of lung cancer is expected to increase further in the next few years as the population grows, life expectancy increases and the population ages. Non-small cell lung cancer (NSCLC) is the most common type of lung cancer, accounting for about 80% of all lung cancers. More than half of the patients are in the middle and advanced stages when they are found, and the 5-ye...
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IPC IPC(8): A61K31/519A61P35/00
CPCA61K31/519A61P35/00
Inventor 梁宏伟曾科黄海王嘉凡
Owner CHINA PHARM UNIV
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