Agonist of spexin-based galanin type 2 receptor and use thereof

Abstract

The present invention relates to spexin-based agonists specific for galanin receptor type 2 and use thereof. More specifically, the present invention provides peptide-based agonists with high specificity for galanin receptor type 2 and improved stability. The peptide-based agonists are involved in the regulation of in vivo physiological functions, such as food intake, anxiety, emotion, and addiction, for which galanin receptors type 2 is responsible, to effectively suppress appetite, help recover from anxiety disorder, and reduce pleasure addiction. Therefore, the peptide-based agonists can be used to prevent or treat galanin receptor type 2-mediated diseases.

Description

REFERENCE TO A SEQUENCE LISTING SUBMITTED ELECTRONICALLY[0001]The content of the electronically submitted sequence listing (Name: 3763_0080001_Seqlisting_ST25.txt; Size: 17,330 bytes; and Date of Creation: Mar. 25, 2019) submitted in this application is incorporated herein by reference in its entirety.TECHNICAL FIELD[0002]The present invention relates to spexin-based agonists specific for galanin receptor type 2 (GALR2) and their use for preventing or treating GALR2-mediated diseases.BACKGROUND ART[0003]The novel neuropeptide spexin (Spexin / NQ / NPQ / SPX), which is encoded by the C12orf39 (chromosome 12 open reading frame 39) gene, was originally discovered using bioinformatics tools. The mature spexin peptide sequence consists of 14 amino acids formed as a result of cleavage of dibasic amino acids by a proprotein convertase and is very well conserved in typical vertebrate species as well as humans [Mirabeau et al., Genome Res, 2007, 17:320-327]. Spexin expression at the mRNA and / or pr...

AI Technical Summary

Benefits of technology

The peptide-based agonists described in this patent have a high affinity for the galanin receptor type 2 and are more stable than previous versions. These agonists are involved in regulating various physiological functions including appetite, anxiety, emotion, and addiction. They can effectively suppress appetite, help recover from anxiety disorder, and reduce pleasure addiction. Therefore, these agonists can be used to prevent or treat diseases caused by malfunctions of the galanin receptor type 2.

Problems solved by technology

Spexin mRNA levels are markedly decreased in the fat of obese humans, and administration of spexin leads to weight loss in diet-induced obese rodents.

The precise roles of spexin in these processes, however, are not well understood due to a lack of information on the spexin receptor.

Despite numerous efforts to develop several species of galanin receptor subtype-specific agonists in the previous studies, treatment with high concentrations of the agonists was found to cause specificity problems.

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