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Polyethylene glycol modified matrix metalloprotease-2 inhibitor and its application

A matrix metal, polyethylene glycol technology, applied in the field of peptides

Inactive Publication Date: 2014-07-16
NANTONG CHENGXIN AMINO ACID
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The research on PEG modification of synthetic small molecule peptides started late, but it has attracted the attention of many researchers

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] IC50 of polyethylene glycol-modified matrix metalloproteinase-2 inhibitors on the growth and survival of tumor cells in vitro.

[0013] Using the MTT colorimetric method. The logarithmic growth of U937 cells was added to a 96-well culture plate at 1.0×105, and cultured for 24 hours. Different concentrations of the experimental drug polyethylene glycol-modified matrix metalloproteinase-2 inhibitor and Positive control drug paclitaxel; add the same volume of solvent to the blank group. Set up five duplicate wells per well, culture for 48h, add MTT to each well at 0h, 2h, 8h, 14h, 20h, 24h, 36h, and 48h respectively, add DMSO after 4h, incubate for 30min, and incubate at 620nm in a microplate reader. Measure the absorbance A value, according to the formula tumor cell growth inhibition rate=(1-absorbance value of the experimental group / absorbance value of the control group)×100%. The calculated IC50 of the test drug was 7.64 μM.

Embodiment 2

[0015] In vivo activity of polyethylene glycol-modified matrix metalloproteinase-2 inhibitors was tested in a tumor model.

[0016] The U937 tumor model was established, and the positive control drug paclitaxel was added; the same volume of solvent was added to the blank group, and 3 doses were set to the experimental group: 0.75, 1.5 μM, and 3 μM mg / Kg. After 21 days, the number of surviving mice was observed, and the survival rate was calculated. The results showed that the polyethylene glycol-modified matrix metalloproteinase-2 inhibitor could effectively protect mice and improve the survival rate of tumor-bearing mice, with the survival rate reaching 76.09%.

[0017] Nantong Chengxin Amino Acid Co., Ltd.

[0018] A polyethylene glycol-modified matrix metalloproteinase-2 inhibitor polypeptide and its application

[0019]

[0020] 1

[0021] PatentIn version 3.3

[0022] 1

[0023] 5

[0024] PRT

[0025] Artificial sequence

[0026] 1

[0027] mPEG-SC 1...

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PUM

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Abstract

The invention relates to the field of medicines, and concretely relates to a polypeptide having matrix metalloprotease-2 inhibition activity and capable of treating acute lymphocytic leukemia. The polypeptide is modified by polyethylene glycol, the sequence of the polypeptide is mPEG-SC10k-PRO-THR-THR-ASN-ARG which is a brand new sequence, and the polypeptide can inhibit the activity of the matrix metalloprotease-2 in vitro, can improve the survival rate of tumor-bearing mice in in-vivo tests, and has potential new drug exploitation values.

Description

technical field [0001] The invention relates to polyethylene glycol-modified matrix metalloproteinase-2 inhibitor and application thereof, in particular to a polypeptide capable of inhibiting matrix metalloproteinase-2 activity and capable of treating solid tumors. Background technique [0002] In recent years, with the deepening of medical research, it has been found that matrix metalloproteinases play an important role in the growth of solid tumors. Matrix metalloproteinases are a group of more than 20 structurally similar and functionally related endoproteinases. They can perform normal physiological functions, such as egg cell implantation, bone growth and organ development; these enzymes can also play pathological roles in such as inflammation, wound healing and tumor cell metastasis. Matrix metalloproteinases are more regarded as regulators of these pathological processes. In the matrix metalloproteinase family, MMP-2 and MMP-9 are important members of the MMP family...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K38/08A61K47/48A61P35/00
Inventor 邢将军许刘华彭立军任世阔华俊国曹铭刘加根刘明明汪士金施新华刘伟峰严明
Owner NANTONG CHENGXIN AMINO ACID
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