Glucagon-like peptide-1 (GLP-1) analogue monomer and dimer, preparation method therefor and application thereof

A technology of glucagon and analogues, applied in GLP-1 dimer, the application field of medicine, can solve the problems of short half-life of liraglutide, short half-life of GLP-1, inconvenient clinical use, etc.
CN102718858AActive Publication Date: 2012-10-10TIANJIN INSTITUTE OF PHARMA RESEARCH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
TIANJIN INSTITUTE OF PHARMA RESEARCH
Publication Date
2012-10-10

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Abstract

The invention provides a GLP-1 dimer, a preparation method therefore and an application thereof. The GLP-1 dimer is formed by two GLP-1 monomers containing cysteine connected via a disulfide bond formed by cysteine. The general formula of the GLP-1 monomer containing cysteine is 7HAEX10T FTSX15V SSYLE X22X23AAKEFIX30W LX33KGR G37; wherein X10 is aglycine or cysteine, X15 is aspartic acid or cysteine, X22 is glycine or cysteine, X23 is leucine or cysteine, X30 is alanine or cysteine, X33 is valine or cysteine, and only one among X10, X15, X22, X23, X30 and X33 is cysteine. The GLP-1 dimer in the invention has an in vivo half-life of more than 8 to 96 hours, thus greatly facilitating clinical promotion and application.
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Description

technical field

[0001] The present invention relates to the field of medicines related to diabetes, in particular, the present invention relates to a GLP-1 dimer with prolonged in vivo half-life of glucagon-like peptides (GLP-1). The present invention also relates to the preparation method of the GLP-1 dimer and its application in the preparation of medicines for treating diabetes, and treating and / or preventing obesity. Background technique

[0002] Glucagon-like peptide-1 (hereinafter referred to as: GLP-1) is a polypeptide composed of 37 amino acids mainly secreted by small intestinal L cells, and its active form is GLP-1(7-37 )OH and GLP-1(7-36)NH 2 (Mojsov S, J Clin Invest. 1987 Feb;79(2):616-9). GLP-1 can significantly reduce the blood sugar after meals, can stimulate the production of insulin, and can also play a certain role in weight loss, and will not cause hypoglycemia (Drucker D J, Diabetes.1998 Feb; 47 (2): 159-69 ). Recent studies have also shown that GLP-1...

Claims

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