Anti-tumor polypeptide targeting PKM2 protein and application of anti-tumor polypeptide

An anti-tumor and protein technology, applied in the biological field, can solve the problems of poor water solubility and limited affinity of the target protein, and achieve the effect of large sample content, abundant quantity and variety, and overcoming cumbersome steps.

Active Publication Date: 2021-03-12
SUN YAT SEN UNIV SHENZHEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to overcome the shortcomings of existing PKM2 non-polypeptide organic synthetic small molecule drugs such as poor water solubility and limited affinity with target proteins, the purpose of the first aspect of the present invention is to provide an anti-tumor polypeptide targeting PKM2 protein

Method used

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  • Anti-tumor polypeptide targeting PKM2 protein and application of anti-tumor polypeptide
  • Anti-tumor polypeptide targeting PKM2 protein and application of anti-tumor polypeptide
  • Anti-tumor polypeptide targeting PKM2 protein and application of anti-tumor polypeptide

Examples

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Effect test

Embodiment 1

[0047] Example 1 Screening of anti-tumor polypeptides targeting a PKM2 protein

[0048] (1) Synthesis of phosphorylated tyrosine polypeptide library

[0049] The structural formula of phosphorylated tyrosine polypeptide compound is synthesized by the synthesis of Titan 357 (AAPPTEC) synthesizers Titan 357 (AAPPTEC), and the structural form of phosphorylated tyrosine polypeptide library is: AA 5 AA 4 -py-aa 2 AA 1 -PEG-R (AA represents any type of L-type natural amino acid). The phosphorylated tyrosine polypeptide is synthesized on the Tentagel S-NH2 resin by a method of tentagel s-NH2 resin by a method of tentagel S-NH2 resin.

[0050] First, a certain amount of resin is placed in a polymerizing container (CV) swells 2 h with N-methylpyrrolidone (NMP) solution, and then adds 1 degree amount of FMOC-amino acid (FMOC-MET), 2 times equivalent O - Benzotriazole-N, N, N ', N' - tetramethylurea tetrafluororate (TBTU), 5 times the amount of diisopropylidelamine (Diea), reaction for 30min...

Embodiment 2

[0066] A kit for diagnosing tumors, including Kg-Py-Eq, Kg-PY-IW, HW-PY-KW, NK-PY-GE, RD-PY-LY, HV-PY-SR, PE-PY-YR At least one of DE-PY-FQ; the tumor is at least one of liver cancer and breast cancer.

[0067] A drug for treating tumors comprising Kg-Py-Eq, Kg-PY-IW, HW-PY-KW, NK-PY-GE, RD-PY-LY, HV-PY-SR, PE-PY-YR, At least one of DE-PY-FQ; at least one of the tumors is liver cancer, breast cancer; the drug further comprises a pharmaceutically acceptable excipient.

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Abstract

The invention discloses an anti-tumor polypeptide targeting PKM2 protein and application of the anti-tumor polypeptide. The amino acid sequence of the polypeptide is at least one of KG-pY-EQ, KG-pY-IW, HW-pY-KW, NK-pY-GE, RD-pY-LY, HV-pY-SR, PE-pY-YR and DE-pY-FQ, wherein pY represents phosphorylated tyrosine. The anti-tumor polypeptide targeting the PKM2 protein has an inhibiting effect on growthand proliferation of liver cancer cells and breast cancer cells, and can be used for treating tumors.

Description

Technical field [0001] The present invention belongs to the biotechnology field, and more particularly to anti-tumor polypeptides targeting PKM2 proteins and their applications. Background technique [0002] Malignant tumors (cancer) have become one of the main public health issues that have seriously threatened human health, and developed a more high-efficiency drug for the diagnosis and treatment of tumors to become an important task of medical researchers. Protein kinase is considered to be an important target group of anticancer drugs in humans, protein kinases are closely involved in various life activities such as intracellular signal transduction and energy exchange, and play an essential role in maintaining cellular function and human metabolism. [0003] Unlike normal cells, the energy metabolism of cancer cells is an oxygen-sugar yeast. This low-capacity metabolic manifestation makes cancer cells as high-level glucose intake, and the intermediate product of glycolysis i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06G01N33/574A61K38/08A61P35/00
CPCC07K7/06G01N33/574A61P35/00A61K38/00
Inventor 高理钱谢刘幸谈思佳王璇李孟础杨芬贾艳肖奇才沈君
Owner SUN YAT SEN UNIV SHENZHEN
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