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Small molecule inhibitor with anti-tumour activity targeting PD-1/PD-L1 interaction, and application of small-molecule inhibitor

A technology of PD-L1 and PD-1, applied in the research and development and application of anti-tumor drugs, can solve the problems of large immunogenic side effects, high drug production costs, high molecular weight, etc., and achieve a broad anti-cancer effect

Inactive Publication Date: 2020-12-25
LANZHOU UNIVERSITY
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Problems solved by technology

Although monoclonal antibodies have achieved unprecedented success in the field of cancer immunotherapy, because monoclonal antibodies are biological agents with high molecular weight, high drug production costs, and large immunogenic side effects (9), peptide inhibitors and The development of small molecule compounds still has huge room for development, which will provide new opportunities for tumor immunotherapy

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  • Small molecule inhibitor with anti-tumour activity targeting PD-1/PD-L1 interaction, and application of small-molecule inhibitor
  • Small molecule inhibitor with anti-tumour activity targeting PD-1/PD-L1 interaction, and application of small-molecule inhibitor
  • Small molecule inhibitor with anti-tumour activity targeting PD-1/PD-L1 interaction, and application of small-molecule inhibitor

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Embodiment Construction

[0041] The present invention will be further described below through specific examples, but it should not be understood that the scope of the above subject of the present invention is limited to the following examples. All technologies realized based on the above content of the present invention belong to the scope of the present invention.

[0042] In the present invention, based on the crystal structure (5J89) of the complex of hPD-L1 and small molecule BMS-202, the applicant used Schrödinger software ( LLC, New York, United States, 2015) screened and docked the small molecule pharmacophore from the Specs compound library, selected the docked advantageous structure for experimental verification, and finally screened out the APBC small molecule compound of the present invention (PECS, No.AG-690 / 11449006) has good hPD-1 / hPD-L1 inhibitory activity and belongs to the biphenylamide class. The applicant commissioned Shanghai Taosu Biochemical Technology Co., Ltd. to synthesize t...

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Abstract

The invention relates to an anti-tumour small molecule inhibitor targeting PD-1 / PD-L1 interaction, and application of the anti-tumour small molecule inhibitor. According to the small-molecule inhibitor in the invention, N-[2-(aminocarbonyl)phenyl][1,1'-biphenyl]-4-carboxamide can reactivate the immune response of T cells by inhibiting PD-1 / PD-L1 interaction, so as to efficiently kill tumour cellsin a targeted manner. The small molecule inhibitor can be used as a new anti-tumour drug and has important clinical treatment value.

Description

Technical field: [0001] The invention relates to a small molecule inhibitor with PD-1 / PD-L1 inhibitory activity and application thereof, belonging to the technical field of research and development and application of antitumor drugs. Background technique: [0002] Tumor immunotherapy (Tumor immunotherapy) inhibits and kills tumor cells by activating the body's own immune system (1), has the potential to treat various types of tumors, and has durable responses and low toxicity, which can substantially improve the overall survival of patients This period is the beginning of the hope that the tumor will be cured. Due to its excellent curative effect and innovation, in 2013 Science magazine listed tumor immunotherapy as the top ten scientific breakthroughs of the year (2). Immune checkpoint inhibitors, by blocking the transmission of inhibitory signals between antigen-presenting cells and T cells, reactivate the immune response of T cells, and eliminate tumor cells (3), opening...

Claims

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Application Information

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IPC IPC(8): A61K31/166A61P35/00A61P37/04
CPCA61K31/166A61P35/00A61P37/04
Inventor 姚小军王凤玲朱永昌韩建庭刘焕香
Owner LANZHOU UNIVERSITY
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