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Adipose tissue targeting polypeptide, preparation method and application thereof

A technology targeting peptides and adipose tissue, applied in the field of protein peptides, can solve problems such as increasing satiety, achieve less side effects, direct curative effect, and avoid common adverse reactions

Inactive Publication Date: 2017-06-23
ADLAI NORTYE BIOPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Strictly speaking, there are currently no weight-loss drugs that increase energy consumption clinically. However, in addition to suppressing appetite and increasing satiety, studies have also found that sibutramine can increase basal metabolic rate and promote thermogenic effects

Method used

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  • Adipose tissue targeting polypeptide, preparation method and application thereof
  • Adipose tissue targeting polypeptide, preparation method and application thereof
  • Adipose tissue targeting polypeptide, preparation method and application thereof

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preparation example Construction

[0053] The present invention also provides a method for preparing the adipose tissue targeting polypeptide, but not limited to the following methods:

[0054] The route of the present invention is described by taking CRGGRAKDC-GG-D (KLAKLAKKLAKLAK) as an example. Using solid-phase synthesis method, Wang resin or 2-chlorotrityl chloride resin (2-CTC resin) is used as the starting resin, and the peptide sequence of the main chain of the adipose tissue targeting polypeptide is sequentially coupled with N-terminal Fmoc Protected and side chain protected amino acids; finally, peptide resin cleavage, cyclization, purification, and lyophilization to obtain the target compound.

[0055] For this reason, the present invention provides two synthetic methods of adipose tissue targeting polypeptides, the steps of which are as follows:

[0056] method one:

[0057] (1) In the presence of an activator system, Fmoc-D-Lys(Boc)-resin is obtained by coupling a resin solid phase carrier and Fm...

Embodiment 1

[0166] Example 1 First, a chain-shaped SEQ34: CRGGRAKDC-GG-KLAKLAKKLAKLAK adipose tissue targeting polypeptide was prepared and synthesized, in which the amino acids from the 12th to the 25th were all D-type amino acids. Then, the side chain of the Cys at the 1st position and the side chain of the Cys at the 9th position are formed into a disulfide bonded ring through a cyclization process. Its preparation process is as follows:

[0167] 1) Weigh 0.1 mmol of Fmoc-D-Lys(Boc)-King resin with a degree of substitution of 0.45 mmol / g, add it to a solid-phase reaction column, wash once with DMF, and swell Fmoc-D-Lys(Boc) with DMF - Wang resin 30 minutes later, the Fmoc protection was removed with a mixed solution of DMF: piperidine with a volume ratio of 4:1 to obtain H-D-Lys(Boc)-Wang resin, which was washed 6 times with DMF.

[0168] 2) Weigh Fmoc-D-Ala-OH0.5mmol, HOBt0.5mmol, add DCM and DMF mixed solution with a volume ratio of 1:1, add 80μl DIC (0.5mmol) under ice-water bath t...

Embodiment 2

[0174] Example 2 First, the chain-like SEQ35: CHomo-RGGRAKDC-GG-KLAKLAKKLAKLAK adipose tissue targeting polypeptide was prepared and synthesized, in which the 12th to 25th amino acids were all D-type amino acids; The side chain of Cys at position 9 and the side chain of Cys at position 9 form a disulfide bonded ring, and the preparation process is as follows:

[0175] 1) Weigh 0.1 mmol of Fmoc-D-Lys(Boc)-King resin with a degree of substitution of 0.45 mmol / g, add it to a solid-phase reaction column, wash once with DMF, and swell Fmoc-D-Lys(Boc) with DMF - After 30 minutes of Wang resin, the Fmoc protection was removed with a mixed solution of DMF:piperidine with a volume ratio of 4:1, and then washed 6 times with DMF to prepare H-D-Lys(Boc)-Wang resin.

[0176] 2) Weigh Fmoc-D-Ala-OH0.5mmol, HOBt0.5mmol, add DCM and DMF mixed solution with a volume ratio of 1:1, add 80μl DIC (0.5mmol) under ice-water bath to activate, add the above-mentioned resin containing In the reaction ...

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Abstract

The invention relates to the field of protein polypeptides, and in particular relates to an adipose tissue targeting polypeptide as well as a preparation method and application thereof. The adipose tissue targeting polypeptide comprises a cell targeting polypeptide peptide fragment, a cell apoptosis polypeptide peptide fragment and a bridge chain for connecting the cell targeting polypeptide peptide fragment and the cell apoptosis polypeptide peptide fragment. The adipose tissue targeting polypeptide can specifically induce adipocyte apoptosis, so that the effect of reducing fat and losing weight is achieved. Moreover, due to the targeting action mechanism contained in the molecules, the common adverse reactions of existing weight-losing medicines can be avoided, and compared with the existing weight-reducing medicines, the adipose tissue targeting polypeptide has a more direct curative effect and less side effects.

Description

technical field [0001] The invention relates to the field of protein polypeptides, in particular to a class of adipose tissue-targeting polypeptides and a preparation method and application thereof. Background technique [0002] Obesity, as a common chronic endocrine and metabolic disease, has an increasing incidence year by year and has become a global public health problem. When the human body eats more calories than it consumes, it will be stored in the body in the form of fat, and more than 20% of the normal body weight is obesity. Obesity can occur at any age, but it is more common in those after the age of 40, and the incidence rate is higher in women. Obesity is divided into two types: one is simple obesity, the main manifestation of which is obesity, without obvious changes in the functions of the nervous system and endocrine system, but accompanied by metabolic regulation disorders, this type of obesity is the most common. The second is secondary obesity, often se...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K19/00C07K14/52C07K1/10C07K1/06A61K38/17A61P3/04
CPCA61K38/17C07K1/06C07K1/10C07K14/52C07K19/00Y02P20/55A61K38/00C07K2319/01
Inventor 张晓厉保秋路杨杨东晖何南海沈柯周俊
Owner ADLAI NORTYE BIOPHARMA CO LTD
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