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Application of beta-pentagalloylglucose in tumor resistance

A pentagalloyl glucose, anti-tumor technology, applied in the field of anti-tumor drug research and development and application, can solve problems such as interfering with interaction, affecting HR repair function, etc., to achieve the effect of broad anti-cancer spectrum and inhibiting growth

Pending Publication Date: 2022-04-12
韩记昌
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Any nucleotide change in WD40 domain may interfere with PALB2-BRCA2 interaction and affect its HR repair function

Method used

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  • Application of beta-pentagalloylglucose in tumor resistance
  • Application of beta-pentagalloylglucose in tumor resistance
  • Application of beta-pentagalloylglucose in tumor resistance

Examples

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Embodiment Construction

[0025] In order to make the technical means, creative features, goals and effects of the present invention easy to understand, the following examples will specifically illustrate the application of β-pentagalloylglucose in the anti-tumor of the present invention in conjunction with the accompanying drawings.

[0026]

[0027] In this example, based on the crystal structure (3EU7) of the PALB2-BRCA2 complex, the applicant used Maestro 11.4 software performs high-throughput virtual screening on HTS Compound Library (HTS Library, containing 2,116K compounds) and MCE Bioactive Compound Library Plus (MCE Library, containing 11.6K compounds). Then use the NanoBiT system to perform secondary screening on the screened dominant compounds, and finally screen out β-pentagalloyl glucose (1,2,3,4,6-Penta-O-Galloyl-β-D-Glucose, referred to as PGG, PubChem CID:65238) has better PALB2-BRCA2 inhibitory activity.

[0028] The chemical formula of β-pentagalloylglucose is as follows:

[0029...

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Abstract

The invention relates to the technical field of research, development and application of anti-tumor drugs, in particular to application of beta-pentagalloylglucose (PGG) in tumor resistance, and tumors are tumor cells with PALB2-BRCA2 binding characteristics. PGG and PALB2 have high affinity, have good biological activity on cell and animal levels, and can block a DNA homologous recombination repair pathway by inhibiting the interaction of PALB2-BRCA2, thereby enhancing the sensitivity of tumor cells to a PARP (Poly (ADP-ribose) polymerase) inhibitor and radiotherapy. The PGG can penetrate through the blood brain barrier and has no obvious toxic or side effect. The PGG can be effectively used for treating cancers such as breast cancer, lung cancer, liver cancer, brain glioma and the like by being combined with a PARP inhibitor or radiotherapy, and has a wide development prospect as a natural product.

Description

technical field [0001] The invention relates to the technical field of research and development and application of antitumor drugs, in particular to the application of β-pentagalloylglucose in antitumor. Background technique [0002] DNA double-strand breaks (Double-strand breaks, DSBs) are the most serious type of DNA damage in eukaryotic cells, which mainly rely on homologous recombination (Homologous recombinant, HR) pathway for repair. BRCA1 / 2 (Breast cancersusceptibility gene 1 / 2) and PALB2 (Partner and localizer of BRCA2) are key factors in this repair pathway. During HR, PALB2 acts as an important bridge between BRCA1 and BRCA2, promoting the recruitment of RAD51 recombinase to DNA damage sites and its assembly into nuclear filaments to initiate DSBs repair. The Human PALB2 gene is located on the short arm of chromosome 16 (16p12.2) and contains 13 exons. The encoded PALB2 protein contains 1186 amino acid residues and a molecular weight of 131 kDa. RAD51) is a bridg...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7024A61K45/06A61P35/00
Inventor 韩记昌刘兆瑞
Owner 韩记昌
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