Magdalena M Scharf, Antonella Di Pizio, Ines Liebscher, Hannes Schihada, and Gunnar Schulte et al. on

August 2022 Gαs and Gαq/11 protein coupling bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic diabetes insipidus "Loss-of-function mutations of the arginine vasopressin receptor 2 gene (AVPR2) cause Nephrogenic diabetes insipidus (NDI). AVPR2 is a kind of G protein coupled receptor (GPCR) and mainly couples with Gαs protein leading to cAMP accumulation in the cell as a secondary messenger. Recent studies showed that some AVPR2 mutations could cause biased Gαq/11 protein coupling rather than Gαs. Investigation into the characterization of biased receptors may give insights into the relationship between the conformational change of the receptor because of the mutation and related downstream signaling. In this study, R68W and V162A were analyzed to whether they show a bias to Gαs or Gαq/11 proteins. Their functionality in terms of cAMP production via Gαs protein coupling was decreased compared to the wild-type receptor. On the other hand, they showed the ability to couple with Gαq/11 protein and make Ca2+ mobilization at different levels in the cell. R68W showed bias to coupling with Gαq/11 protein rather than V162A and wild-type receptor. Studies about the Gα protein coupling bias of mutant AVPR2s may broaden our understanding of the relationship between the changed conformation of the receptor and consequently activated signaling pathways, and also may shed light on the development of more effective new therapeutics." Read more at the source #DrGPCR #GPCR #IndustryNews

According with the National Institute on Drug Abuse (NIDA) nearly 92, 000 Americans died from drug-involved

Antonella Di Pizio About this episode In this episode of the Dr. GPCR podcast , we meet with Dr. Antonella Di Pizio, an independent research group leader at the Leibniz Institute for Food Systems Biology Antonella then moved to Israel, where she first started working on bitter taste GPCRs in Dr. Today, Antonella has expanded her research to olfactory GPCRs and trace amine receptors. Antonella Di Pizio on the web Leibniz-Institute for Food Systems Biology at the Technical University

Antonella Di Pizio, an independent research group leader at the Leibniz Institute for Food Systems Biology Antonella trained as a medicinal chemist in Italy, followed by a Ph.D. in computational medicinal chemistry Antonella then moved to Israel, where she first started working on bitter taste GPCRs in Dr. Today, Antonella has expanded her research to olfactory GPCRs and trace amine receptors. Antonella Di Pizio on the web Leibniz-Institute for Food Systems Biology at the Technical University

includes: Brendan Wilkins Graeme Milligan Lukas Grätz Antony Boucard Benjamin Myers Ines Liebscher Antonella