Application of mercaptopurine and derivatives thereof in preparation of drugs for removing malignant tumor immunosuppression

A technology for malignant tumors and immunosuppression, applied in the direction of antineoplastic drugs, drug combinations, active ingredients of heterocyclic compounds, etc., to achieve the effect of releasing tumor immunosuppression, inhibiting the occurrence and development, and reducing protein levels
CN112656800APending Publication Date: 2021-04-16KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI
Publication Date
2021-04-16

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Abstract

The invention discloses new application of mercaptopurine and derivatives thereof, namely application of mercaptopurine and derivatives thereof in preparation of drugs for removing malignant tumor immunosuppression, mercaptopurine and thioguanine act on tumor cells of human lung cancer, colorectal cancer, liver cancer, melanoma, breast cancer and the like. The expression of glycosyltransferase GLT8D1 can be remarkably reduced. Further, the protein level and glycosylation level of PDL1 are inhibited, so that the killing effect of peripheral blood mononuclear cells on tumor cells is improved, and the purpose of inhibiting tumors is achieved; the invention finds that mercaptopurine / thioguanine which interferes with nucleic acid biosynthesis and is widely applied to anti-leukemia drugs can inhibit glycosyltransferase GLT8D1 and a programmed cell death ligand 1 (PDL1) in a targeting manner to enhance tumor killing of T cells so as to achieve the purpose of drugs for treating various tumors; The invention provides a new therapeutic drug for treating various tumors.
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Description

technical field

[0001] The invention belongs to the field of tumor treatment, specifically relates to the application of mercaptopurine and its derivatives in the preparation of drugs for releasing immunosuppression of malignant tumors, and belongs to the technical field of biomedicine. Background technique

[0002] According to the calculation of the proportion of all cancers, including non-melanoma skin cancers, in all age groups and genders, it is estimated that there will be 18.1 million new cancer cases and 9.6 million cancer deaths worldwide in 2018. Asia accounted for nearly 50% of the 18.1 million new cancer patients and nearly 70% of the 9.6 million cancer deaths. The highest incidence of new cancers in the world are: lung cancer (11.6%), breast cancer (11.6%), colorectal cancer (10.2%), prostate cancer (7.1%), gastric cancer (5.7%); the highest mortality rate in the world Cancers are: lung cancer (18.4%), colorectal cancer (9.2%), gastric cancer (8.2%), liver canc...

Claims

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