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Analog of Exendin 4

A technology of analogs and drugs, applied in the field of peptides of Exendin4 analogs, can solve problems such as long half-life

Active Publication Date: 2006-03-15
SHANGHAI HUAYI BIO LAB CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Compared with GLP-1, for the clinical application of Ex4, the dose is 5-10 μg twice a day, while GLP-1 is about 200 μg, and Ex4 is not affected by DPPIV dipeptidase in the blood, and its half-life is longer than that of GLP -1 is long, but there are also deficiencies. Ex4 comes from monitor lizards, and GLP-1 is the endogenous substance of people. Clinical trials report that 52% of patients with Ex4 produce antibodies (Diabetes (1997) 46 , 433-439; Diabetes Care (2002) 25 , 330-336; JAMA (2002) 287 , 373-379; Diabetes (1995) 44 , 1249-1258; Diabetes (2002) 51 2796-2803; Diabetes Care (2000) 23 64-69, N. Engl. J. Med (2002) 346 , 393-463, Lancet (1998) 352 , 837-853)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1: Production of HGEGTFTSDLSKQMEEEAVKLFI EWLKN by genetic engineering method PPSR 32

[0036] Material

[0037]Cloning vector containing lac promoter plasmid; host strain JM103: Promega; T4 polynucleotide kinase kit: Promega; T4 ligase kit: Promega; restriction enzymes EcoRI, Sal I, Bgl II, BamH I Kit: Promega Company; molecular weight standard λDNA, φ×174DNA: Promega Company; low molecular weight standard protein: Shanghai Siji Biological Products Co., Ltd.; ATP (Adenosine-5'-triphosphate, adenosine-5'-triphosphate): Boehringer Mannheim Company; Acrylamide: E.Merck; Methylene bisacrylamide: Fluka; Ethidum bromid: Serva; Tris: A.R Shanghai Siji Biological Products Co., Ltd. (imported packaging); SDS: A.R Shanghai Siji Biological Products Co., Ltd. (import repackaging).

[0038] LB culture medium: tryptone (Tryptone): Oxoid, yeast extract powder: Oxoid, sodium chloride (A.R): China Pharmaceutical Group Shanghai Chemical Reagent Station.

[0039] Other che...

Embodiment 2

[0061] Embodiment 2, synthesize Em32 with solid phase synthesis

[0062]

Em32

HGEGTFTSDLSKQ LEEEAVKLFIEWLKN PPS -OH

HGEGTFTSDLSKQ LEEEAVKLFIEWLKN PPS -NH 2

[0063] Solid Phase Resin Selection

[0064] When the C-terminus of the polypeptide is a carboxyl group

[0065] The conventional Wang resin (Wang Resin, purchased from Shanghai Jier Biochemical Co., Ltd.) was selected for solid-phase synthesis. After the synthesis is completed, the obtained polypeptide resin with side chain protecting groups is cleaved (i.e. deprotection and cutting of the resin are completed in one step), and the C-terminal of the polypeptide is cleaved from the Wang resin to form a carboxyl group.

[0066] When the C-terminus of the polypeptide is an amide

[0067] A conventional amino resin (Fmoc-PAL-PEG-PS Resin, purchased from PE Applied Biosystem Company) was selected for solid-phase synthesis. After the synthesis is finished, the obtained polypeptide r...

Embodiment 3

[0124] Example 3: Hypoglycemic effect of Exendin4 analogs

[0125] Nine C57 mice (Shanghai Animal Center, Chinese Academy of Sciences), 8 weeks old (body weight: 20 g), were taken and divided into 3 groups. Water only and no food overnight.

[0126] At 0 o'clock in the control group, 30 μl of blood was collected from the eye sinus, placed in 0.3ml 0.9% NaCl solution, and then 200 μl of 20% glucose solution was injected intraperitoneally. 200 μl of 20% glucose was injected intraperitoneally once. After the blood sample was centrifuged at 3000rpm for 5 minutes, the blood cells were precipitated, and all the centrifuged supernatant was taken, and the blood glucose was measured with the blood glucose measurement kit produced by the Ministry of Health and Shanghai Institute of Biological Products.

[0127] Ex4 group, according to the same method as the control group, after taking blood at 0 o'clock, intraperitoneally inject 200 μl of 20% glucose solution, and subcutaneously injec...

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PUM

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Abstract

Polypeptide as Exendin4 analogs and its production by chemical synthesis and recombinant DNA are disclosed. The analogs can be used to decrease blood sugar and treat ó�type diabetes.

Description

field of invention [0001] The invention relates to a polypeptide of Exendin4 analogue, which has the effect of lowering blood sugar and can be used for treating type II diabetes. The invention also provides methods for producing these polypeptides by chemical synthesis and recombinant DNA production techniques. Background technique [0002] The number of diabetic patients in the world is increasing year by year. Now there are 40 million in China, 60 million in India, 18 million in the United States, and 6 million in Japan. Diabetic patients are divided into two types, one is insulin-dependent diabetes (type I diabetes) and non-insulin-dependent diabetes (II Diabetes). Among them, type II diabetes accounts for more than 90% of diabetic patients. [0003] Patients with type II diabetes show many characteristics, such as insufficient postprandial insulin secretion, delayed insulin secretion, and hyperglycemia. The insulin receptor sensitivity of peripheral cells of obese pat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/435A61K38/17A61P3/10
Inventor 孙玉琨张培璋周波
Owner SHANGHAI HUAYI BIO LAB CO LTD
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