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Tubulin depolymerizing agent polypeptides and application thereof

A technology of tubulin and depolymerizing agent, applied in tubulin depolymerizing agent polypeptide 1 and its application field, can solve the problem of lack of specificity of small molecule depolymerizing agent, and achieve the effect of increasing survival rate and improving survival rate

Inactive Publication Date: 2013-08-21
河北佑仁生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Many successful small-molecule depolymerization agents can inhibit the activity of tubulin at the nanomolar level, but small-molecule depolymerization agents lack specificity. If long-term use of tubulin depolymerization agents lacking specificity in chronic diseases may cause produce major side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Inhibition rate calculation: Inhibition rate (%) = (control tube "OD" value - dosing tube "OD" value) / control tube "OD"

[0018] Five doses were set in the experimental group: 0.75 μM, 1.5 μM, 3 μM, 12 μM, 24 μM, the dose of vincristine in the positive control group was 3 μM, and an equal volume of solvent DMSO was added to the blank group; the absorbance was measured according to the above operation. The results showed that with the increase of the concentration of tubulin depolymerizing agent polypeptide 1, the polymerization inhibition rate decreased gradually, indicating that the polymerization ability of tubulin decreased continuously with the increase of drug concentration.

[0019] Example 2

[0020] IC50 of tubulin depolymerizer polypeptide 1 on the growth and survival of tumor cells cultured in vitro.

Embodiment 2

[0022] Example 3

[0023] In vivo activity of tubulin depolymerizer polypeptide 1 was tested in a tumor model.

Embodiment 3

[0025]

[0026] SEQUENCE LISTING

[0027]

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PUM

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Abstract

The invention relates to tubulin depolymerizing agent polypeptides and application thereof, particularly polypeptides capable of inhibiting polymerization of tubulin and treating acute lymphatic leukemia. The invention is characterized in that the sequence of the tubulin depolymerizing agent polypeptides 1 is CRALERLV disclosed as SEQ NO.1. The invention also relates to application of the tubulin depolymerizing agent polypeptides 1 in preparation of medicines for treating acute lymphatic leukemia. A solid-phase synthesis method is utilized to chemically synthesize the tubulin depolymerizing agent polypeptides 1; and the polypeptides with the bran-new sequence can inhibit tubulin in vitro and treat acute lymphatic leukemia.

Description

technical field [0001] The present invention relates to tubulin depolymerizing agent polypeptide 1 and its application, in particular to a polypeptide capable of inhibiting tubulin polymerization 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, tubulin plays an important role in acute lymphoblastic leukemia. [0003] Microtubules are the main...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K38/08A61P35/02
Inventor 罗瑞雪
Owner 河北佑仁生物科技有限公司