Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Novel proto-oncoprotein SET inhibitor and fusion polypeptide and application thereof

A fusion of polypeptide and oncoprotein technology, applied in the field of medicine, to achieve the effect of inhibiting estrogen response and inhibiting tumor cell proliferation

Active Publication Date: 2021-02-19
CHINA PHARM UNIV
View PDF1 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the epigenetic and molecular biological mechanisms of SET's involvement in transcriptional regulation still need to be further explored.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Novel proto-oncoprotein SET inhibitor and fusion polypeptide and application thereof
  • Novel proto-oncoprotein SET inhibitor and fusion polypeptide and application thereof
  • Novel proto-oncoprotein SET inhibitor and fusion polypeptide and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 SET protein inhibitors and fusion polypeptides inhibit the proliferation of various tumor cells

[0035] MTT method was used to detect the inhibitory effect of SET protein inhibitors on the proliferation of various tumor cells, including melanoma cell B16F10, gastric cancer cell MGC-803, lung cancer cell A549, liver cancer cell Hep-G2, breast cancer cell MDA-MB-231, Breast cancer MCF-7, breast cancer MCF-10CA1A, colon cancer HCT-116, human glioma U87, cervical cancer Hela.

[0036] Tumor cells were incubated at 37°C, 5% CO 2 When cultured in an incubator with a density of more than 90%, it was digested with trypsin and collected, and the cells were resuspended in culture medium and counted under a microscope, and the cell concentration was adjusted to 3.0×10 4 cells / mL, seed the cell suspension into a 96-well plate, 100 μL per well, and inoculate at 37°C, 5% CO 2 Incubate overnight in the incubator. Dilute the SET protein inhibitor and the positive drug Tax...

Embodiment 2 3

[0043] Example 2 Three-dimensional transwell method to detect the activity of CPCY-3 in inhibiting the migration of human umbilical vein endothelial cells

[0044] Take CPCY-3 as an example for detection:

[0045] Human umbilical vein endothelial cells (HUVEC) were incubated with endothelial cell culture medium containing 5% fetal bovine serum and 1×ECGS at 37°C, 5% CO 2 When cultured in the incubator to a confluence of more than 90%, the transwell method was used to detect the activity of the SET protein inhibitor to inhibit the migration of endothelial cells. The endothelial cell HUVEC only used the 2nd to 8th passages, and the specific operations were as follows:

[0046] (1) Dilute 10mg / mL Matrigel with DMEM medium at a rate of 1:4, spread on the transwell chamber membrane, and air-dry at room temperature;

[0047] (2) Digest the HUVEC cells cultivated to the logarithmic growth phase with 0.2% EDTA, collect, wash twice with PBS, resuspend with endothelial cell culture med...

Embodiment 3

[0059] Example 3 CPCY-3 Coupled FITC Cell Localization Verification

[0060] Human breast cancer cell MCF-7 was incubated at 37°C, 5% CO 2 When cultured in an incubator with a density of more than 90%, it was digested with trypsin and collected, and the cells were resuspended in culture medium and counted under a microscope, and the cell concentration was adjusted to 3.0×10 4 Cells / mL, the cells were inoculated into 24-well plates, 400ul per well, and cultured overnight. After co-incubating FITC-CPCY-3 with the cells at a final concentration of 10ug / ml for 1 hour, the green fluorescent position was observed under a fluorescence microscope. The experimental results are attached Figure 4 , CPCY-3 can be clearly localized in the nucleus.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention belongs to the field of medicines, and particularly discloses a novel proto-oncoprotein SET inhibitor and a fusion polypeptide and application thereof. The amino acid sequence of the proto-oncoprotein SET inhibitor is shown as SEQ ID NO.1, SEQ ID NO.2 or SEQ ID NO.3. The amino acid sequence of the corresponding fusion polypeptide is shown as SEQ ID NO.4, SEQ ID NO.5 or SEQ ID NO.5. The SET protease inhibitor can inhibit SET protein-mediated cell proliferation at a concentration level of 1 micromole, and a good tumor inhibition effect is realized in-vitro and in-vivo experiments,with potential new drug development value.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a proto-oncoprotein SET inhibitor fusion polypeptide CY-1, CY-2, CY-3 and application thereof, which has the function of inhibiting SET-mediated tumor cell proliferation and related functions. [0002] technical background [0003] Tumor has always been a serious medical problem, and tumor metastasis is the main reason for its high lethality. In 2018, there were 18.1 million new cancer cases and 9.6 million deaths worldwide. The medical community has been devoting itself to the study of effective means of tumor treatment. Numerous small molecule inhibitors and immunotherapy drugs have been scrambled to develop, which relatively prolongs the survival time of tumor patients. [0004] SET protein is a multifunctional proto-oncoprotein, which is widely expressed in various cells. SET protein participates in the regulation of cell cycle, cell movement, cell apoptosis and other cell...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K19/00A61K38/08A61K47/64A61P35/00
CPCC07K7/06A61P35/00C07K2319/10A61K38/00
Inventor 郭长缨于丽婷顾亚茹
Owner CHINA PHARM UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com