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Application of carfilzomib in preparation of medicine for treating osteosarcoma

A technology for carfilzomib and osteosarcoma, applied in drug combinations, antineoplastic drugs, pharmaceutical formulations, etc.

Active Publication Date: 2021-12-28
XI AN JIAOTONG UNIV
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  • Claims
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Problems solved by technology

In recent years, with the advancement of surgical techniques, the research of effective chemotherapy drugs, and the application of adjuvant chemotherapy and radiotherapy before and after surgery, the 5-year survival rate of osteosarcoma patients has been greatly improved. However, recurrent and metastatic osteosarcoma Cancer is still an incurable disease that needs to be overcome urgently

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  • Application of carfilzomib in preparation of medicine for treating osteosarcoma
  • Application of carfilzomib in preparation of medicine for treating osteosarcoma
  • Application of carfilzomib in preparation of medicine for treating osteosarcoma

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Embodiment Construction

[0022] The invention discloses the new function that the proteasome inhibitor carfilzomib can be used for treating osteosarcoma. Carfilzomib can not only induce apoptosis of osteosarcoma cells, but also low concentration of carfilzomib can induce osteogenic differentiation of osteosarcoma cells, specifically manifested as increased calcified nodules in osteosarcoma cells F5M2 and U-2 OS; Alkaline phosphatase activity increased; expression of osteogenic differentiation markers (ALP, OPN, Runx2) increased.

[0023] The present invention uses Annexin V-FITC / 7-AAD double-staining flow cytometry to detect the killing effect of carfilzomib on osteosarcoma cells. Alizarin red staining experiment was used to detect the effect of low concentration carfilzomib on the formation of calcified nodules in osteosarcoma cells. The Gomori calcium-cobalt staining experiment was used to detect the effect of low concentration carfilzomib on alkaline phosphatase activity in osteosarcoma cells. We...

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Abstract

The application of carfilzomib in the preparation of drugs for treating osteosarcoma, the invention proposes a new function of proteasome inhibitor carfilzomib: it can induce directional osteogenic differentiation of osteosarcoma, and can be used for treating osteosarcoma. It has been confirmed by experiments that medium and high doses of carfilzomib can induce apoptosis of osteosarcoma cells, and low concentration of carfilzomib can also effectively induce osteogenic differentiation of osteosarcoma cells, specifically manifested as: causing osteosarcoma cells F5M2, Increased calcified nodules; increased alkaline phosphatase activity; increased expression of osteogenic differentiation markers (ALP, OPN, Runx2) in U‑2OS.

Description

technical field [0001] The invention relates to the application of carfilzomib in the preparation of drugs for treating osteosarcoma Background technique [0002] The ubiquitin-proteasome pathway (UPP) is an important proteolytic pathway in living cells. The hydrolysis process mainly occurs in the 26S proteasome, which consists of two 19S regulatory complexes and a 20S catalytic core body. The 20S catalytic core is responsible for decomposing polyubiquitinated substrate proteins into polypeptide fragments. It is a tubular structure composed of stacked six-leafed rings containing different α and β subunits, and the active subunit is β1 , β2 and β5. Studies have confirmed that the proteasome participates in the degradation of various proteins (such as NF-κB, p53, cyclin, etc.), and indirectly regulates biological processes such as cell mitosis, apoptosis, signal transduction, and protein transmembrane localization. It is closely related to many diseases such as schizophreni...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/08A61P35/00
CPCA61K38/08A61P35/00
Inventor 胡劲松张丹雷莉陈萍贾茜
Owner XI AN JIAOTONG UNIV
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