Geneva, Switzerland, 28 November 2011 Addex Pharmaceuticals (SIX:ADXN), a leading biopharmaceutical company pioneering allosteric modulation-based drug discovery and development, announced today that its scientists have demonstrated that, in the presence of GLP-1, glucagon-like-peptide-1 receptor (GLP1R) can form a heterodimer receptor complex with gastric-inhibitory-peptide-receptor (GIPR). The discovery of this novel interaction between the two G-protein-coupled receptors (GPCR) has the potential to trigger the discovery of novel therapies for the treatment of diabetes. The findings were published online in the peer-reviewed journal Molecular Pharmacology (Lateral Allosterism in the Glucagon Receptor Family: GLP-1 Induces GPCR Heteromer Formation [Schelshorn et al., Molecular Pharmacology, Published online, doi: 10.1124/mol.111.074757]).
"GIPR and GLP1R are found together in pancreatic and nerve cells, and their roles in Type 2 diabetes make them important targets for drug development. Further research is needed to determine the pharmacological relevance of such heteromers but understanding their role may open the door to more refined therapies, particularly in metabolic disorders," explained Robert Lutjens, head of biology at Addex Pharmaceuticals and co-author of the publication. "This study demonstrates that Addex' allosteric modulation platform is a powerful tool for elucidating fundamental biological processes in addition to being the most sensitive method available for identifying allosteric modulators."
In the present study, the researchers at Addex used Bioluminescence Resonance Energy Transfer (BRET) techniques, calcium flux measurements, and microscopy to study receptor interactions within the glucagon receptor family of GPCRs. Through these techniques, a GLP-1-induced heteromer formation was exclusively observed in cells co-expressing GLP-1 with GIP receptors, but not with other receptors of the glucagon receptor s
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