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Optimized GIP peptide analogs

A technology of analogs and insulin-stimulating peptides, applied in the field of peptide analogs, can solve problems such as inappropriate drug administration

Pending Publication Date: 2022-07-15
ANTAG THERAPEUTICS APS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, GIP(3-30) is poorly soluble at a neutral pH of about 7.5, and is therefore not suitable for pharmaceutical administration

Method used

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  • Optimized GIP peptide analogs
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Experimental program
Comparison scheme
Effect test

Embodiment

[0672] The embodiments of the present invention support the following conclusions:

[0673] 1) GIP peptide analogs comprising substitutions A13Aib and / or N24E according to embodiments of the present disclosure have increased solubility and / or stability, such as physical stability.

[0674] 2) Individual amino acid substitutions at certain positions, such as Aib at position 13, lead to improved antagonism of GIP receptors.

[0675] 3) Several acylation sites show great potential for GIP(3-30)+Z with substitutions A13Aib and / or N24E, such as position 18.

[0676] Materials and methods

[0677] WO 2016 / 034186 discloses the production and action of the GIP(3-30) peptide itself.

[0678] Material

[0679] Human GIP (1-42) was purchased from Phoenix Pharmaceuticals Inc., while the remaining GIP peptide analogs were synthesized by Caslo TM (Lingby, Denmark) and Almac Group (Craigavon, UK), Peptides & Elephants GmbH (Henningsdorf, Germany) and WuXi AppTec, China. The cDNA for the...

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PUM

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Abstract

Disclosed are peptide analogs derived from glucose dependent insulinotropic peptide (GIP), which are antagonists of the GIP receptor. These GIP peptide analogs are modified by comprising amino acid substitutions A13Aib and / or N24E and fatty acid conjugation is carried out with / without the use of linkers, thereby having improved solubility and / or physical stability.

Description

technical field [0001] The present invention relates to glucose-dependent insulinotropic peptide (GIP) derived peptide analogs which are antagonists of the GIP receptor. These GIP peptide analogs are optimized by inclusion of amino acid substitutions A13Aib and / or N24E and fatty acid conjugation with / without linkers resulting in improved solubility and / or physical stability while retaining or even improving Antagonism of GIP receptors. Background technique [0002] Glucose-dependent insulinotropic peptide (GIP) is a postprandial hormone secreted from intestinal K cells 1 . Like its sister hormone glucagon-like peptide 1 (GLP-1), GIP is a potent insulin secretagogue 2 . Glucagon inhibition with GLP-1 3，4 Conversely, GIP has been shown to exhibit glucagon-releasing properties under certain conditions ( 3，5-13 ). Association between rodent GIPR (GIP receptor) and obesity reinforces interest in understanding biology of GIP 14-21 . In humans, although less clear, there i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/435C07K14/605
CPCA61K38/00C07K14/575A61K38/22A61P3/00C07K14/645
Inventor M·M·罗森基尔德A·H·斯巴尔-乌尔里希D·里伯S·J·三尼
Owner ANTAG THERAPEUTICS APS
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