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Highly potent ligands of the ghrelin receptor to influence food intake

Country of Origin: Germany
Reference Number: TODE20190305002
Publication Date: 13 March 2019

Summary

A German University has developed synthesized short peptides that show high inverse agonist potency towards the ghrelin receptor, which is useful in the treatment of feeding-related disorders, such as obesity. The endogenous ligand ghrelin is the only known orexigenic gastrointestinal peptide and plays a central role in the regulation of appetite and energy homeostasis. The university is looking for partners from industry for further R&D and license agreements.

Description

The research institute of a German University was found in 2003 and promotes the networking of research within the university while simultaneously utilizing emerging interdisciplinary synergies.

A research group of the institute developed synthesized short peptides that show high inverse agonist potency towards the ghrelin receptor, which is useful in the treatment of feeding-related disorders, such as obesity. The endogenous ligand ghrelin is the only known orexigenic gastrointestinal peptide, which plays a central role in the regulation of appetite and energy homeostasis.

The ghrelin receptor is a G protein-coupled receptor (GPCR) mainly expressed in the brain, but also in other tissues such as stomach, liver and heart. The receptor possesses a high constitutive activity. It was suggested to induce constant appetite and to trigger food intake in between meals. Its endogenous ligand ghrelin is the only known orexigenic gastrointestinal peptide and plays a central role in the regulation of appetite and energy homeostasis. Reducing the basal activity of the ghrelin receptor could be an innovative strategy to develop anti-obesity drugs. Although obesity is a worldwide steadily increasing problem so far there are only few pharmaceuticals available, most presenting moderate benefits, poor tolerance and strong side effects. Therefore developing highly potent inverse agonists for the ghrelin receptor may be useful in the treatment of feeding-related disorders.
The group was able to synthesize short peptides that show high inverse agonist potency toward the ghrelin receptor.
Potential fields of application are appetite or eating disorders, obesity and obesity-associated disorders, metabolic and/or endocrine disorders, addictive disorders, chronic liver disease and cardiovascular disorders.
The university is looking for partners from industry for further R&D to pursue the implementation of a product development and for license agreement, respectively, to focus the market launch.

Advantages and Innovations

The peptides are capable of increasing or decreasing the constitutive activity of ghrelin receptor by at least 10%. Based on these peptides drugs for a multitude of diseases, obesity e.g.,could be developed

Stage Of Development

Under development/lab tested

Stage Of Development Comment

Intracerebroventricular administration of peptide 3 to rats. The food intake 
of rats was decreased almost 5-fold in comparison to
rats injected with vehicle solution.

Requested partner

The university is looking for partners from industry for further research and development in order to improve therapies against food disorders and to pursue the implementation of a product development and for license agreements to focus the market launch.

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