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Gip receptor-active glucagon compounds

A peptide and composition technology, applied in the field of glucagon peptide analogs, can solve troublesome and dangerous problems

Inactive Publication Date: 2015-03-25
INDIANA UNIV RES & TECH CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

While the treatment is effective, it is cumbersome and dangerous for unconscious people

Method used

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  • Gip receptor-active glucagon compounds
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  • Gip receptor-active glucagon compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0423] General synthetic experiment guidelines:

[0424] Glucagon analogs were synthesized on a modified Applied Biosystem Model 430A peptide synthesizer using HBTU-activated "Fast Boc" single coupler starting from 0.2 millimolar Boc Thr(OBzl)Pam resin. Boc-amino acids and HBTU were purchased from Midwest Biotech (Fishers, IN). The side chain protecting groups used are: arginine (Tos), asparagine (Xan), aspartic acid (OcHex), cysteine ​​(pMeBzl), histidine (Bom), lysine acid (2Cl-Z), serine (OBzl), threonine (OBzl), tyrosine (2Br-Z), and tryptophan (CHO). The side chain protecting group on the histidine at the amino acid terminal is Boc.

[0425] Each completed peptidyl resin was treated with a 20% solution of piperidine in dimethylformamide (hereinafter referred to as DMF) to remove the formyl group from tryptophan. Liquid hydrogen fluoride (hydrofluoric acid, hereinafter referred to as HF) splitting is carried out in the presence of p-cresol and dimethyl sulfide. Dissoci...

Embodiment 1

[0430] Synthesis of Glucagon Cys17(1-29) and Similar Monocysteine ​​Analogs Using FastBoc HBTU-activated single coupler, 0.2 millimolar Boc Thr(OBzl)Pam resin ( SynChem Inc) and the following sequences were imported and performed on a modified Applied Biosystems 430A peptide synthesizer.

[0431] HSQGTFTSDYSKYLDSCRAQDFVQWLMNT (SEQ ID NO: 35)

[0432] The following side chain protecting groups were used: arginine (Tos), aspartic acid (OcHex), asparagine (Xan), cysteine ​​(pMeBzl), glutamic acid (OcHex), histidine (Boc), lysine (2Cl-Z), serine (Bzl), threonine (Bzl), tryptophan (CHO) and tyrosine (2Br-Z). The completed peptidyl resin was treated with 20% piperidine / dimethylformamide to remove the formyl protection of tryptophan, then transferred to an HF reaction vessel and dried in vacuo. Add 1.0 ml p-cresol and 0.5 ml dimethyl sulfide along with a magnetic stir bar. The vessel was connected to a HF apparatus (Pennisula Labs), cooled in a dry ice / methanol bath, evacuated, an...

Embodiment 2

[0435] Synthesis of Glucagon-Cex and Other Carboxy-Terminally Extended Analogues

[0436] 285 mg (0.2 mmol) of methoxybenzhydrylamine resin (Midwest Biotech) was placed in a 60 ml reaction vessel, and FastBoc HBTU-activated single coupler was used in the modified Applied Biosystems 430A peptide Enter and execute the following sequence on the synthesizer.

[0437] HSQGTFTSDYSKYLDSRRAQDFVQWLMNTGPSSGAPPPS (SEQ ID NO: 36)

[0438] The following side chain protecting groups were used: arginine (Tos), aspartic acid (OcHex), asparagine (Xan), cysteine ​​(pMeBzl), glutamic acid (OcHex), histidine (Boc), lysine (2Cl-Z), serine (Bzl), threonine (Bzl), tryptophan (CHO) and tyrosine (2Br-Z). The completed peptidyl resin was treated with 20% piperidine / dimethylformamide to remove the formyl protection of tryptophan, then transferred to an HF reaction vessel and dried in vacuo. Add 1.0 ml p-cresol and 0.5 ml dimethyl sulfide along with a magnetic stir bar. The vessel was connected to a ...

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Abstract

Glucagon peptides with increased GIP activity are provided, optionally with GLP-I and / or glucagon activity. In some embodiments, C-terminally extended glucagon peptides comprising an amino acid sequence substantially similar to native glucagon are provided herein.

Description

technical field [0001] The present invention provides a glucagon peptide analog that exhibits agonist activity on the gastric inhibin receptor (GIP). Methods of using the analogs are also presented herein. Background technique [0002] Pre-proglucagon is a 158-amino acid precursor polypeptide that is processed in different tissues to form many different proglucagon-derived peptides, including: pancreas Glucagon, glucagon-like peptide-1 (GLP-1), glucagon-like peptide-2 (GLP-2) and tomodulin (OXM; oxyntomodulin), which participate in various physiological functions, including Glucose homeostasis, insulin secretion, gastric emptying, and intestinal growth, and regulation of food intake. Glucagon (Glucagon) is a peptide containing 29 amino acids, which is composed of amino acids 33 to 61 corresponding to the preproglucagon, and glucagon-like peptide-1 (GLP-1) is produced as the corresponding It is a 37-amino acid peptide consisting of amino acids 72 to 108 in the preproglucag...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/605
CPCA61K38/00C07K14/605A61K38/26A61P1/00A61P3/04A61P3/08A61P43/00A61P3/10
Inventor 理查德·D.·迪马仕大卫·L.·斯迈利玛丽亚·迪马仕约瑟夫·沙贝内乔纳森·戴詹姆斯·帕特森布莱恩·P.·沃德马涛
Owner INDIANA UNIV RES & TECH CORP
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