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Addex scientists discover GLP-1 induced interaction between GLP-1 and GIP receptors
Date:11/28/2011

ubtypes. Furthermore, the pharmacology of this GLP-1-induced heteromeric receptor complex was found to be affected in presence of GIP. In addition, the heteromer's intracellular signaling through beta-arrestin or calcium second messenger was shown to be modified when compared to receptor homodimers, suggesting a form of allosteric regulation between the receptors.

"This research demonstrates how our pioneering allostery platform technology is able to observe specific interactions at the receptor level that have not been seen with conventional state-of-the-art techniques," noted Laurent Galibert, head of metabolic disease programs at Addex Pharmaceuticals. "An orally available small molecule targeting GLP1R would have a significant impact on the treatment of Type 2 diabetes. We now have the opportunity to explore and characterize this receptor further, paving the way for a better understanding of the signaling pathways implicated in diabetes and metabolism, which may offer novel therapeutic targets for allosteric modulation."

GLP-1 is an important metabolic hormone and a proven therapeutic ligand for treatment of diseases, such as Type II diabetes and obesity. Addex is leading the effort towards the development of orally available small molecule GLP1R activators, called positive allosteric modulators or PAM, which have potential to offer multiple advantages over marketed injectable peptide therapeutics targeting GLP1R.

Addex has previously disclosed that it achieved the first in vivo preclinical proof of concept demonstrating that an oral small molecule GLP1R PAM could increase the release of insulin and improve glucose control in preclinical diabetes models. Addex GLP1R PAMs are in lead generation phase for Type 2 diabetes and could become the first-in-class orally available small molecule therapeutic agents against this target.


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Contact: Mike Sinclair
msinclair@halsin.com
44-207-318-2955
Halsin Partners
Source:Eurekalert

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