GLP-1 analogs, and preparation method and application thereof

A technology of GLP-1 and analogs, which can be used in drug combinations, pharmaceutical formulations, animal/human proteins, etc., and can solve problems such as short half-life

Inactive Publication Date: 2013-04-24
TIANJIN JIAHONG TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004]Therefore, there is currently a need for methods that address the short in vivo half-life of GLP-1

Method used

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  • GLP-1 analogs, and preparation method and application thereof
  • GLP-1 analogs, and preparation method and application thereof
  • GLP-1 analogs, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0185] Example 2: Hypoglycemic function related to GLP-1 analogs (general formula II)

[0186] In this embodiment, the polypeptides used are as follows:

[0187] SEQ ID NO 7: HAEGT FTSDVS CYLEGQACK EFIAW LVKGR GAA;

[0188] SEQ ID NO 8: HAEGT FTSDVS CYLEGQACK EFIAW LVKGR GAAAAAA;

[0189] SEQ ID NO 9: HAEGT FTSDVS CYLEGQACK EFIAW LVKGR GYY;

[0190] SEQ ID NO 10: HAEGT FTSDVS CYLEGQACK EFIAW LVKGR GYYYYYYYY;

[0191] SEQ ID NO 11: HAEGT FTSDVS CYLEGQACK EFIAW LVKGR GYYYYYYYYYY;

[0192] SEQ ID NO 12: HAEGT FTSDVS CYLEGQACK EFIAW LVKGR GKK;

[0193] SEQ ID NO 13: HAEGT FTSDVS CYLEGQACK EFIAW LVKGR GKKKK;

[0194] SEQ ID NO 14: HAEGT FTSDVS CYLEGQACK EFIAW LVKGR GKKKKKK;

[0195] SEQ ID NO 15: HAEGT FTSDVS CYLEGQACK EFIAW LVKGR GKKKKKKKK;

[0196] SEQ ID NO 16: HAEGT FTSDVS CYLEGQACK EFIAW LVKGR GKKKKKKKKKK;

[0197] SEQ ID NO 17: HAEGT FTSDVS CYLEGQACK EFIAW LVKGR GKKKKKKKKKKKK;

[0198] SEQ ID NO 18: HAEGT FTSDVS CYLEGQACK EFIAW LVKGR GKKKKKKKKKKKKKKKK;

[0199] ...

Embodiment 3

[0219] Example 3: The hypoglycemic function related to GLP-1 analogs (general formula III).

[0220] In this embodiment, the polypeptides used are as follows:

[0221] SEQ ID NO 37: HAEGT FTSDVS SYLEGQA AK EFICW LCKGR GRR;

[0222] SEQ ID NO 38: HAEGT FTSDVS SYLEGQA AK EFICW LCKGR GRRRR;

[0223] SEQ ID NO 39: HAEGT FTSDVS SYLEGQA AK EFICW LCKGR GRRRRR;

[0224] SEQ ID NO 40: HAEGT FTSDVS SYLEGQA AK EFICW LCKGR GRRRRRRR;

[0225] SEQ ID NO 41: HAEGT FTSDVS SYLEGQA AK EFICW LCKGR GRRRRRRRRR;

[0226] SEQ ID NO 42: HAEGT FTSDVS SYLEGQA AK EFICW LCKGR GAA;

[0227] SEQ ID NO 43: HAEGT FTSDVS SYLEGQA AK EFICW LCKGR GAAAA;

[0228] SEQ ID NO 44: HAEGT FTSDVS SYLEGQA AK EFICW LCKGR GAAAAAA;

[0229] SEQ ID NO 45: HAEGT FTSDVS SYLEGQA AK EFICW LCKGR GAAAAAAAA;

[0230] SEQ ID NO 46: HAEGT FTSDVS SYLEGQA AK EFICW LCKGR GAAAAAAAAAAA;

[0231] SEQ ID NO 47: HAEGT FTSDVS SYLEGQA AK EFICW LCKGR GYY;

[0232] SEQ ID NO 48: HAEGT FTSDVS SYLEGQA AK EFICW LCKGR GYYYY;

[0233] S...

Embodiment 4

[0251] Example 4: Hypoglycemic function related to GLP-1 analogs (general formula IV)

[0252] In this embodiment, the polypeptides used are as follows:

[0253] SEQ ID NO 65: HAEGT FTSDVS SYLEGQA AK EFIAW LCKGR CRA;

[0254] SEQ ID NO 66: HAEGT FTSDVS SYLEGQA AK EFIAW LCKGR CRY;

[0255] SEQ ID NO 67: HAEGT FTSDVS SYLEGQA AK EFIAW LCKGR CRK;

[0256] SEQ ID NO 68: HAEGT FTSDVS SYLEGQA AK EFIAW LCKGR CRI;

[0257] SEQ ID NO 70: HAEGT FTSDVS SYLEGQA AK EFIAW LCKGR CRM;

[0258] SEQ ID NO 71: HAEGT FTSDVS SYLEGQA AK EFIAW LCKGR CRRAA;

[0259] SEQ ID NO 72: HAEGT FTSDVS SYLEGQA AK EFIAW LCKGR CRRRRAA;

[0260] SEQ ID NO 73: HAEGT FTSDVS SYLEGQA AK EFIAW LCKGR CRRRRRRYY;

[0261] SEQ ID NO 74: HAEGT FTSDVS SYLEGQA AK EFIAW LCKGR CRRRRRRKKKK;

[0262] SEQ ID NO 75: HAEGT FTSDVS SYLEGQA AK EFIAW LCKGR CRRRRRIIIIII;

[0263] SEQ ID NO 76: HAEGT FTSDVS SYLEGQA AK EFIAW LCKGR CRRRRRMM;

[0264] SEQ ID NO 77: HAEGT FTSDVS SYLEGQA AK EFIAW LCKGR CRRRRRRMMMMM;

[0265] SEQ ...

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Abstract

The invention discloses GLP-1 analogs, and a preparation method and an application thereof. The GLP-1 analogs have a following general formula A: <7>HAEX10TFTSDVSX18YLEX22QAX25KEFIX30WLX33KGRG<37>n1X1n2X2. With the GLP-1 analogs provided by the invention, GLP-1 blood half-life period can be effectively increased, such that a situation that GLP-1 cannot be clinically used due to short half-life period can be overcome. The GLP-1 analogs have application prospects in fields of medicines used for treating diabetes and obesity. The invention also discloses the preparation method and the application of the GLP-1 analogs.

Description

technical field [0001] The present invention relates to the field of drugs related to diabetes, in particular, the present invention relates to a GLP-1 analogue with prolonged in vivo half-life of glucagon-like peptide-1 (GLP-1). The present invention also relates to the preparation method of the GLP-1 analog and the application in the preparation of diabetes medicine. Background technique [0002] The GLP-1 amino acid (glucagon-likepeptide-1, hereinafter referred to as: GLP-1) involved in the present invention is a polypeptide composed of 37 mainly secreted by small intestinal L cells, and its active form is GLP-1(7-37) OH and GLP-1(7-36)NH2 (Mojsov S, J Clin Invest. 1987 Feb; 79(2): 616-9). GLP-1 significantly reduces blood sugar after meals, stimulates the production of insulin, and also has a certain weight loss effect, and will not cause hypoglycemia (Drucker D J, Diabetes. 1998 Feb; 47(2): 159-69 ). Recent studies have also shown that GLP-1 has a role in pancreatic ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/605A61K38/26A61P3/10A61P3/04
Inventor 李瑛
Owner TIANJIN JIAHONG TECH
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