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Application of UPK1A-AS1 inhibitor in preparation of antitumor drugs

The technology of UPK1A-AS1 and 1.UPK1A-AS1 is applied in the application field of UPK1A-AS1 inhibitor in the preparation of anti-tumor drugs, which can solve the problem of few people benefiting from treatment, and achieve the effect of excellent anti-tumor effect.

Active Publication Date: 2021-10-08
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Targeted drug therapy such as sorafenib and lenvatinib is the first-line treatment for advanced liver cancer, but the number of patients benefiting from the treatment is small, and patients often develop acquired drug resistance after treatment; The effective rate is only about 20%

Method used

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  • Application of UPK1A-AS1 inhibitor in preparation of antitumor drugs
  • Application of UPK1A-AS1 inhibitor in preparation of antitumor drugs
  • Application of UPK1A-AS1 inhibitor in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Example 1 Silencing effect of UPK1A-AS1 inhibitor (locked nucleic acid of UPK1A-AS1) on UPK1A-AS1 and effect on proliferation of liver cancer cells

[0071] 1. Experimental materials

[0072] Liver cancer cell lines: Liver cancer cell lines MHCC-97H and SK-Hep-1 were purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences, and placed in DMEM medium containing 10% serum in 5% CO 2 , cultured in an incubator at 37°C, after the cell density reached about 85%, subculture and follow-up experiments were performed, and the medium was changed every 1 to 2 days.

[0073] Drug: LNA-i-UPK1A-AS1-1 (sequence is AGCAGACCTTCCTAAC, SEQ ID NO.1, molecular weight is: 5205.2Da, LNA-i-AS1-1), LNA-i-UPK1A-AS1-2 (sequence is AACAGCACTGTCAAGG , SEQ ID NO.2, molecular weight is: 5280.2Da, LNA-i-AS1-2), LNA-i-UPK1A-AS1-3 (sequence is TCTTTGCCCACTTTAC, SEQ ID NO.3, molecular weight is: 5139.1Da, LNA-i -AS1-3) and LNA-i-NC (LNA-i-NC), purchased from Exiqon, Cat. No.: 300600, De...

Embodiment 2

[0089] Example 2 UPK1A-AS1 inhibitor (locked nucleic acid of UPK1A-AS1) in the treatment of BALB / c nude mouse liver cancer subcutaneous tumor model experiment

[0090] 1. Experimental materials

[0091] BALB / c nude mice: BALB / c nude mice (4-6 weeks old, male), provided by the Experimental Animal Center of Southern Medical University, were raised in the SPF animal room of Nanfang Hospital, Southern Medical University, and the cages and utensils used were strictly controlled. Disinfect, feed and drink pure water ad libitum; observe whether the nude mice have clinical symptoms before the experiment, and set aside.

[0092]Drug: LNA-i-UPK1A-AS1-3 (the sequence is TCTTTGCCCACTTTAC, SEQ ID NO.3, the molecular weight is: 5139.1Da, LNA-i-AS1-3) and LNA-i-NC (LNA-i-NC), Purchased from Exiqon Company, article number: 300600, DesignID: 683533-3. Drug configuration for injection in the experimental group: first dissolve 50 mg of LNA-i-UPK1A-AS1-3 in 4 mL of PBS, make a 12.5 mg / mL stock ...

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Abstract

The invention belongs to the technical field of medicines, and discloses application of a UPK1A-AS1 inhibitor in preparation of antitumor drugs. The invention discloses application of the UPK1A-AS1 inhibitor or pharmaceutically acceptable salt thereof in preparation of antitumor drugs for the first time based on the fact that the inventor finds that proliferation of tumor cells and tumor tissues can be inhibited by inhibiting expression and / or activity of UPK1A-AS1. The weight of a drug-administered animal is not remarkably influenced, and meanwhile, during drug administration, no drug treatment side effect is observed; and it is indicated that the UPK1A-AS1 inhibitor or the pharmaceutically acceptable salt thereof can inhibit the proliferation of tumor tissues, has no side effect, and can be used for preparing the antitumor drugs.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the application of UPK1A-AS1 inhibitors in the preparation of antitumor medicines. Background technique [0002] Primary hepatocellular carcinoma (Hepatocellular carcinoma, HCC, referred to as liver cancer) is one of the most common malignant tumors in clinical practice, with the incidence rate ranking fourth among malignant tumors and the mortality rate ranking third. Liver cancer has the characteristics of insidious onset and rapid progression. Most patients are diagnosed at an advanced stage and lose the opportunity for radical treatment such as surgery. The 5-year survival rate is only 14.1%, which seriously threatens the lives and health of our people. Targeted drug therapy such as sorafenib and lenvatinib is the first-line treatment for advanced liver cancer, but the number of patients benefiting from the treatment is small, and patients often develop acquired...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/7088A61K31/7115A61K31/712A61P35/00
CPCA61K45/00A61K31/7088A61K31/7115A61K31/712A61P35/00
Inventor 张冬艳吴德华刘莉邹雪晶宋旸张雅璇
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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