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Matrix metalloproteinase-2 polypeptide inhibitor and application

A technology of peptide inhibitors and matrix metals, applied in the field of matrix metalloproteinase-2 polypeptides, can solve problems such as side effects and lack of specificity of small molecule inhibitors

Active Publication Date: 2013-09-18
GUANGZHOU FOREVERGEN BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation and use of macromolecular inhibitors has limited their development, for example recombinant human matrix proteinase tissue inhibitor of metalloproteinase-3 has an in vivo half-life of only 4 minutes
Many successful small molecule inhibitors, such as Marimastat, can inhibit the activity of matrix metalloproteinases at the nanomolar level, but small molecule inhibitors lack specificity. produce side effects

Method used

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  • Matrix metalloproteinase-2 polypeptide inhibitor and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The polypeptide can be synthesized and obtained by applying the above chemical conditions, and the sequence is Trp-Ser-Asn-Val-Gly-Gly-Gly-Gly-Glu-Lys-Met, which is a completely new sequence.

[0019] You can also entrust Shanghai Sangong Synthetic Co., Ltd.

[0020] Example 2

[0021] IC50 values ​​of polypeptide inhibitors against several target enzymes in vitro: matrix metalloproteinase-3, -8, -2 and tumor necrosis factor releasing enzyme (both purchased from sigma company).

Embodiment 2

[0023] Recombinant human matrix metalloproteinase-8 is detected similarly to that of -2 and uses the same fluorogenic substrate. Reactions were also performed in 100 μl reactions at 37°C. Add 20 μl recombinant human matrix metalloproteinase-8 (2 ng / μl) to the reaction system during detection. The final concentration of substrate was 10 μM. The measured IC50 value is 14.78 μmol.

[0024] Recombinant human matrix metalloproteinase-3 uses another fluorescent substrate Mca-Arg-Pro-Lys-Pro-Val-Glu-Nval-Trp-Arg-Lys(Dnp)-NH 2 to detect (excitation wavelength = 320 nm, emission wavelength = 405 nm). Reactions were performed in 100 μl reactions at 37°C. At the beginning of the reaction, add 10 μl matrix metalloproteinase-3 storage solution (1 ng / μl) to the reaction system, and the final concentration of the substrate is 10 μM. The measured IC50 value is 33.66 μmol.

[0025] The activity of TNF-releasing enzyme was detected by cleaving the fluorescent substrate Mca-Pro-Leu-Ala-Gln...

Embodiment 3

[0029] SEQUENCE LISTING

[0030] Suzhou Proda Biotechnology Co., Ltd.

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Abstract

The invention relates to the field of drugs and in particular relates to polypeptides capable of inhibiting matrix metalloproteinase-2 and tumor necrosis factor liberase and also capable of relieving damage of acute inflammatory reaction to an organism. The sequence of the polypeptides is Trp-Ser-Asn-Val-Gly-Gly-Gly-Gly-Glu-Lys-Met, which is a brand new sequence; the polypeptides are capable of inhibiting the activities of matrix metalloproteinase-2 and the tumor necrosis factor liberase in vitro on the level of 1 micromole, and also capable of increasing the survival rate of endotoxic shock mice in in vivo tests; the polypeptides have potential new drug development value.

Description

technical field [0001] The invention relates to a matrix metalloproteinase-2 polypeptide and its application, in particular to a polypeptide capable of inhibiting matrix metalloproteinase-2 and reducing acute inflammatory response damage to the body. [0002] Background technique [0003] Sepsis has always been a serious medical problem. Early sepsis without timely and effective treatment can progress to severe sepsis and septic shock, with mortality rates of 20% to 30% and 40% to 70%, respectively. The medical community has been studying effective treatments, such as early symptomatic treatment, activated protein C, and corticosteroid treatment. In recent years, with the deepening of medical research, great progress has been made in the understanding and treatment of sepsis. Among them, matrix metalloproteinase-2 (MMP-2) plays an important role in endotoxin shock. [0004] Matrix metalloproteinases are a group of more than 20 structurally similar and functionally relat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K38/08A61P29/00
Inventor 罗瑞雪
Owner GUANGZHOU FOREVERGEN BIOTECH CO LTD
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