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Focal adhesion kinase inhibitor polypeptide and its application

A technology for focal adhesion kinases and inhibitors, applied in the field of focal adhesion kinase inhibitor polypeptides and their applications, can solve the problems of limited development, short half-life in vivo, and lack of specificity of small molecule inhibitors, so as to improve survival rate, The effect of increasing the survival rate

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 preparation and use of macromolecular inhibitors limits their development, such as the short in vivo half-life of recombinant human focal adhesion kinase inhibitor
Many successful small-molecule inhibitors can inhibit the activity of FAK at the nanomolar level, but small-molecule inhibitors lack specificity, and long-term use of FAK inhibitors lacking specificity in chronic diseases may produce major side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Effect of focal adhesion kinase inhibitor polypeptide 3 on focal adhesion kinase activity in vitro.

[0016] Take fresh bovine brain tissue, peel off the meninges and large blood vessels, cut into pieces, wash 1-2 times with cold MES buffer, add MES buffer at a ratio of 0.5-1ml per gram of brain tissue, at 4°C, use electric Homogenize with a homogenizer; centrifuge at 105,000 g for 1 hour at 4°C, take the supernatant, add an equal volume of microtube polymerization buffer, and incubate in a water bath at 37°C for 30 minutes. Centrifuge at 105,000g at 26°C for 1 hour, take the precipitate, add about 1 / 10 of the homogenate volume of cold MES buffer, stir gently or crush the precipitate with a homogenizer; place the suspension in an ice bath for 30 minutes to dissolve the precipitate completely. Protein content was determined by Lowry's method (SDS polyamide gel electrophoresis). Adhesion kinase was diluted to 4-5mg / ml with MES buffer and stored in liquid nitrogen. Take ...

Embodiment 2

[0020] IC50 of focal adhesion kinase inhibitor polypeptide 3 on the growth and survival of tumor cells cultured in vitro.

[0021] The MTT colorimetric method was used. The logarithmic growth of U937 cells was added to a 96-well culture plate at 1.0×105, and cultured for 24 hours. The experimental wells and the positive drug control wells were respectively added with different concentrations of the experimental drug focal adhesion kinase inhibitor polypeptide 3 and the positive control drug Changchunxin base; 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 of action, incubate for 30min, and place 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 IC...

Embodiment 3

[0023] The in vivo activity of focal adhesion kinase inhibitor polypeptide 3 was detected by tumor model.

[0024] The U937 tumor model was established, and the positive control drug vincristine was added; the same volume of solvent was added to the blank group, and three doses were set in 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 focal adhesion kinase inhibitor polypeptide 3 could effectively protect mice and improve the survival rate of tumor-bearing mice, with the survival rate reaching 73.2%.

[0025]

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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 focal adhesion kinase inhibition activity and capable of treating acute lymphocytic leukemia. The sequence of the polypeptide is FRLCSHLRSEECVHW which is a brand new sequence, and the polypeptide can inhibit the focal adhesion kinase activity 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 present invention relates to a focal adhesion kinase inhibitor polypeptide 3 and its application, in particular to a polypeptide capable of inhibiting the focal adhesion kinase activity and treating acute lymphocytic leukemia. Background technique [0002] Acute lymphoblastic leukemia (ALL) is a progressive malignant disease characterized by large numbers of immature white blood cells that resemble lymphoblasts. These cells can be found in the blood, bone marrow, lymph nodes, spleen and other organs. Acute lymphoblastic leukemia accounts for 80% of acute leukemia in children, and the peak incidence is between 3 and 7 years old. ALL can also occur in adults and accounts for 20% of all adult leukemias. In recent years, with the deepening of medical research, great progress has been made in the understanding and treatment of acute lymphoblastic leukemia. Among them, focal adhesion kinase plays an important role in acute lymphoblastic leukemia. [...

Claims

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Application Information

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IPC IPC(8): C07K7/08A61K38/10A61P35/02
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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