Application of KPNB1 inhibitor and protein degradation pathway inhibitor in preparation of anti-tumor drugs

Abstract

The invention relates to an application of a KPNB1 inhibitor and a protein degradation pathway inhibitor in the preparation of anti-tumor drugs. According to the invention, the KPNB1 inhibitor and theprotein degradation pathway inhibitor are used in combination so as to have extremely excellent inhibition effect on treating tumors, particularly glioma. The aim of killing more tumor cells can be achieved by drug combination.

Description

technical field [0001] The invention relates to the field of biotechnology, in particular to the application of KPNB1 inhibitors and protein degradation pathway inhibitors in the preparation of antitumor drugs. Background technique [0002] Tumor is one of the diseases that threaten human health. So far, there is a lack of ideal treatment methods and drugs, and the development of new drugs is imminent. As an emerging method, gene therapy may become an effective means of tumor treatment in the near future. [0003] Glioma is a tumor that occurs in the brain or spinal cord. The most common site is the brain. It is called glioma because of its origin in glial cells. Glioma accounts for 30% of brain and central nervous system tumors and 80% of malignant brain tumors, and is a serious threat to human health. Glioma is usually treated with a combination of surgery, radiotherapy and chemotherapy. Glioma often occurs in the brain, and surgery requires a craniotomy, which takes a ...

AI Technical Summary

Problems solved by technology

However, the toxicity of KPNB1 inhibition on normal tissue cells still needs to be carefully evaluated.

Currently, the lack of KPNB1 inhibitors is a major limiting factor for targeting KPNB1 in cancer therapy

Recently, some small molecule peptide KPNA / KPNB inhibitors have been used to study nuclear translocation, however these inhibitors are not cell permeable

Ivermectin is a broad-spectrum KPNA / KPNB inhibitor but cannot inhibit KPNB1-mediated nuclear translocation alone

Karyostatin 1A is the first KPNB1 inhibitor discovered, but its anticancer efficacy and off-target effects are still inconclusive

Overall, drugs that inhibit KPNB1-mediated nuclear translocation are still limited

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