Specific inhibitor for toxic protein granzyme M of human immune system, preparation method and application

A technology of inhibitors and uses, applied in the field of new human immune system toxic protein granzyme M inhibitors

Inactive Publication Date: 2010-01-13
INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, there is no serine protease inhibitor that can well inhibit the activity of granzyme M (Rukamp et al., 2004), so we are committed to designing granzyme M according to the special structure of granzyme M specific inhibitor

Method used

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  • Specific inhibitor for toxic protein granzyme M of human immune system, preparation method and application
  • Specific inhibitor for toxic protein granzyme M of human immune system, preparation method and application
  • Specific inhibitor for toxic protein granzyme M of human immune system, preparation method and application

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Experimental program
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Embodiment 1

[0027] Synthesis, purification and identification of the compound of embodiment 1 formula (I)

[0028] The synthesis of the amino acid sequence Lys-Val-Pro-Leu in the compound of formula (I) can be carried out according to the solid phase synthesis technique known to those skilled in the art (for example, refer to "Solid Phase Organic Synthesis-Principles and Application Guidelines, edited by Wang Dexin, Chemical Industry Press, September 2004"). The acetylation modification of the N-terminal of the peptide and the CMK modification of the C-terminal are also known to those skilled in the art (Bell et al., 2003; Marzo et al., 1998).

[0029] The synthesis of the compound of formula (I) was entrusted to Hangzhou Zhongpei Biochemical Co., Ltd., and the results of synthesis, purification and identification can be found in figure 1 and 2 , wherein the modified peptide is separated and purified by C18 hydrophobic chromatography, and the obtained peptide is identified by mass spect...

Embodiment 2

[0032] The compound of embodiment 2 formula (I) inhibits the activity of human granzyme M

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Abstract

The invention relates to a novel compound shown in a formula (I), wherein ACE (acetyl, ACE) is acetyl; CMK (chloromethyl ketone, CMK) is chloromethyl ketone; and Lys, Val, Pro and Leu represent four amino acids, namely lysine, valine, proline and leucine respectively. The compound shown in the formula (I) can be used as a granzyme M inhibitor for related scientific research, and has potential application value of being applied to clinical organ transplantation, the treatment of autoimmune diseases and the like.

Description

technical field [0001] The present invention relates to a novel human immune system toxic protein granzyme M inhibitor, its preparation method and use. Background technique [0002] Natural killer cells (NK) are the main effector cells of innate immunity, and play an important role in anti-virus and intracellular bacterial infection, organ transplant rejection, anti-tumor immune response and autoimmune diseases (Vivier et al. , 2008). There are two ways for NK cells to kill target cells: direct release of cytotoxic granules or binding to death receptors on target cells (Fas / FasL or TNF / TNFR pathway). The contents of cytotoxic granules mainly include perforin and serine protease family granzymes. Granzymes are a class of highly conserved serine proteases. So far, five species of granzymes (A, B, K, H, and M) have been found in humans (Chowdhury and Lieberman, 2008). Granzyme M, a very specific member that cleaves its substrate specifically after methionine, leucine, or nor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/11C07K1/107C07K1/20A61K38/07A61P37/06A61P37/02A61P35/00
Inventor 范祖森吴连锋孙飞王丽华国强刘侃杨轩李翀翟羽佳
Owner INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES
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