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Epidermal growth factor receptor antagonists and application thereof

An epidermal growth factor and receptor technology, applied in the field of small molecule drugs

Inactive Publication Date: 2019-11-26
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition to lung cancer, it has also been reported that the ErbB family (especially ErbB1) is abnormally activated in breast cancer, ovarian cancer, prostate cancer and gastrointestinal tumors, manifested as gene amplification and protein overexpression, indicating that the epidermal growth factor receptor Antagonists may be effective therapies for the above cancers

Method used

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  • Epidermal growth factor receptor antagonists and application thereof
  • Epidermal growth factor receptor antagonists and application thereof
  • Epidermal growth factor receptor antagonists and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment

[0032] Experimental procedure

[0033] 1. Cell suspension preparation and seeding

[0034] a) All cells were cultured according to ATCC standards, and HEK293T was tested in exponential growth phase.

[0035] b) Discard the medium.

[0036] c) Wash the cells twice with PBS.

[0037] d) Add trypsin digestion solution to digest the cells, and stop the digestion with complete medium.

[0038] e) The cells were collected and centrifuged, and the cells were washed with PBS to remove phenol red in the medium.

[0039] f) Cells are collected and counted, and the experiment can only be performed when the cell viability is greater than 90%.

[0040] g) Kinds 5.5*10 6 HEK293T cells into 100mm cell culture dishes.

[0041] h) Place the culture dish in which the cells have been planted in a 37°C, 5% CO2 incubator for overnight culture.

[0042] 2. Cell transfection

[0043] a) Place the Trans-IT transfection reagent at room temperature to equilibrate;

[0044] b) Add Trans-IT tran...

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Abstract

The invention provides 3 epidermal growth factor receptor antagonist and application thereof. In vitro biological experiments have showed that the epidermal growth factor receptor antagonists have antagonistic activity to epidermal growth factor receptors.

Description

technical field [0001] The invention belongs to the field of small molecule medicines, and in particular relates to three epidermal growth factor receptor antagonists and applications thereof. Background technique [0002] Epidermal growth factor receptor (EGFR) is a member of the ErbB (ErbB1-4) family, namely ErbB1. Members of the ErbB family all contain common domains: an extracellular ligand-binding domain, a transmembrane α-helical domain and an intracytoplasmic tyrosine protein kinase domain. Ligands related to epidermal growth factor (EGF) bind to these receptors, forming receptor homologous or heterologous dimerization, which is the basis for ErbB family to cause downstream signal transmission. Dimerization activates the tyrosine kinase activity of these receptors, and specific tyrosine residues at the C-terminus of the cytoplasmic inner side provide binding sites for intracellular signaling molecules after autophosphorylation. ErbB1 differs from other family member...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K31/7048A61K31/12A61P35/00
CPCA61K31/12A61K31/352A61K31/7048A61P35/00C07C49/84C07D311/30C07H17/07
Inventor 林建平梁璐王目阔
Owner NANKAI UNIV