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PTP1B polypeptide inhibitor and preparation method and application thereof

A peptide inhibitor and sequence technology, applied in the field of biomedicine

Active Publication Date: 2019-06-21
MARINE BIOMEDICAL RES INST OF QINGDAO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] In addition, PTP1B inhibitors do not have side effects such as fluid retention, weight gain, obesity and other side effects of thiazolidinediones. Therefore, PTP1B is considered to be an ideal target for the treatment of type II diabetes

Method used

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  • PTP1B polypeptide inhibitor and preparation method and application thereof
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  • PTP1B polypeptide inhibitor and preparation method and application thereof

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Embodiment Construction

[0036] The following will clearly and completely describe the technical solutions in the embodiments of the present invention with reference to the drawings in the embodiments of the present invention.

[0037] The present invention provides a class of PTP1B polypeptide inhibitors, the sequence of which is one of the following sequences:

[0038] (1) Ac-Ile-Ala-Lys-Lys-Leu-Arg-Arg-Ile-Gly-Asp-Lys-Phe-NH 2 ;

[0039] (2) Ac-Ile-Lys-Lys-Lys-Leu-Arg-Arg-Ile-Lys-Asp-Lys-Phe-NH 2 ;

[0040] (3) Ac-Ile-Lys-Lys-Lys-Leu-Lys-Lys-Ile-Lys-Asp-Lys-Phe-NH 2 ;

[0041] (4) Ac-Lys-Ile-Ala-Leu-Lys-Leu-Ala-Leu-Lys-Gly-Asp-Glu-Phe-NH 2 ;

[0042] (5) Ac-Lys-Leu-Ile-Ala-Leu-Lys-Leu-Ala-Leu-Ile-Gly-Asp-Glu-Phe-NH 2 ;

[0043] (6) Ac-Lys-Leu-Ile-Ala-Leu-Lys-Leu-Ala-Leu-Ile-Gly-Asp-Glu-Phe-OH;

[0044] (7) Pal-Lys-Leu-Ile-Ala-Leu-Lys-Leu-Ala-Leu-Ile-Gly-Asp-Glu-Phe-OH;

[0045] (8) Pal-Ile-Ala-Gln-Glu-Leu-Arg-Arg-Ile-Gly-Asp-Glu-Phe-NH 2 ;

[0046] (9) Pal-Ile-Ala-Gln-Glu-Leu-Arg-Arg-Il...

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Abstract

The invention discloses a PTP1B polypeptide inhibitor, a chemical synthesis method thereof and application of the PTP1B polypeptide inhibitor in development of anti-type II diabetes drugs. The PTP1B polypeptide inhibitor is prepared by a solid-phase synthesis method. The polypeptide compound has a good treatment effect on insulin resistance type II diabetes by inhibiting the activity of protein tyrosine phosphorylase 1B and enhancing insulin sensitivity, and has potential application value in the development of anti-type II diabetes drugs.

Description

technical field [0001] The invention belongs to the field of biomedicine, in particular to a PTP1B polypeptide inhibitor and its preparation method and application. Background technique [0002] With the change of human living environment and lifestyle, the number of diabetic patients worldwide has increased dramatically. According to the latest data released by the International Diabetes Federation (IDF) in the sixth edition of Diabetes Map (December 2013, Melbourne, Australia), there are currently about 382 million diabetic patients in the world, and it is estimated that the number of diabetic patients will increase to 592 million in 2035. It is estimated that about 6 people die of diabetes every minute in the world, and the number of deaths due to diabetes and its complications is second only to cancer and cardiovascular and cerebrovascular diseases. Diabetes has become the most important disease that threatens human health in the 21st century. Diabetes is mainly divided...

Claims

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Application Information

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IPC IPC(8): C07K7/08C07K1/06C07K1/04C12N9/16A61K38/10A61P3/10
CPCY02P20/55
Inventor 张传亮王树林路晓吴丽娟柳晓春蔡兵管华诗
Owner MARINE BIOMEDICAL RES INST OF QINGDAO CO LTD
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