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Application of rafoxanide and closantel in preparing anti-tumor drugs

A closentel and drug technology, which is applied to the application field of rafenide and closentel in the preparation of antitumor drugs, and can solve problems such as drug treatment effect limitation and the like

Inactive Publication Date: 2016-06-22
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the emergence of drug resistance limits the therapeutic effect of drugs, and the research on the mechanism of drug resistance, the development of new drugs, and the prevention or delay of drug resistance have become the key issues that need to be solved at present.

Method used

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  • Application of rafoxanide and closantel in preparing anti-tumor drugs
  • Application of rafoxanide and closantel in preparing anti-tumor drugs
  • Application of rafoxanide and closantel in preparing anti-tumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: For BRAF V600E Virtual screening by enzymes

[0026] 1. Experimental materials

[0027] (1) Main data: 1634 molecular structures of halogen-containing drugs (from Comprehensive Medicinal Chemistry, CMC), B-Raf protein target structure (from RCSB Protein Data Bank, PDB, PDB ID: 1UWJ and 3C4C)

[0028] (2) Main experimental equipment: one supercomputer (SGIAltix4700, 256 CPUs), one cluster computer (Dell, 32 CPUs), 5 blade servers (each with 16 CPUs)

[0029] (3) Software: D 3 DOCKxb (software copyright registration number: 2013SR109950, used for molecular docking of halogen-containing drugs), software (commercial software, LLC, New York, NY, 2010)

[0030] 2. Experimental method

[0031] (1) Virtual screening process

[0032] 1) Prepare the molecular structure of the halogen-containing drug for molecular docking: use the LigPrep module (version2.4, LLC, NewYork, NY, 2010) prepared 1634 molecular structures of halogen-containing drugs for molecular d...

Embodiment 2

[0041] Example 2: BRAF of Drugs V600E Kinase inhibitory activity

[0042] 1. Experimental materials

[0043] (1) Main reagents: SF-900IISFM (Gibco), Ni-NTASuperflow affinity chromatography resin (QIAGEN), ATP disodium salt (Solarbio), p-MEK antibody (CellSignalingTechnology), glutathione-embedded 96-well plate (Pierce), enzyme-labeled rabbit secondary antibody (Jackson).

[0044] (2) Main instruments: FlexStation3 multifunctional microplate reader (Molecular Devices), TS-211C horizontal constant temperature oscillator (Shanghai Tiancheng Experimental Instrument Manufacturing Co., Ltd.).

[0045] 2. Experimental method

[0046] (1) BRAF V600E Expression and purification of kinase and substrate MEK protein

[0047] 1) BRAF V600E Kinase preparation: expression of BRAF on a recombinant plasmid in sf9 cells using the Bac-to-Bac system V600E Kinase, expand and collect sf9 insect cells, sonicate, centrifuge to get supernatant, use nickel column affinity chromatography to purify ...

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Abstract

The invention provides novel application of rafoxanide and closantel in the pharmacy filed. The two compounds are BRAFV600E enzyme inhibitors, and the purpose of treating various tumors by inhibiting BRAFV600E enzyme activity is achieved. Rafoxanide and closantel can be applied to preparation of drugs for preventing and / or treating diseases such as melanoma, colorectal neoplasms and thyroid neoplasms, and have significant application prospects.

Description

technical field [0001] The invention relates to the application of rafoxanide and closantel in the preparation of antitumor drugs. Background technique [0002] BRAF is one of the most important proto-oncogenes in humans, and about 8% of human tumors have BRAF mutations. Most mutated forms of BRAF are BRAF V600E Mutations, mainly in melanoma, colon and thyroid cancers. This mutation leads to continuous activation of the downstream MEK-ERK signaling pathway, which is critical to tumor growth, proliferation, invasion and metastasis, and is one of the effective targets for anti-melanoma and other V600E mutant tumors. In 2011, the first BRAF V600E The targeted inhibitor vemurafenib is approved by the FDA for the treatment of BRAF V600E For patients with advanced melanoma with mutations, it effectively prolongs the progression-free survival and overall survival of patients, and has achieved breakthrough therapeutic effects. It is also a typical targeted therapy drug based on ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/167A61K31/277A61P35/00
CPCA61K31/167A61K31/277
Inventor 朱维良徐志建李亦苏王贺瑶郭彬彬李波张鑫贲蔡婷婷
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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