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Ann N Y Acad Sci. 2005 May;1041:288-91.

Signal switching after stimulation of LGR7 receptors by human relaxin 2.

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Department of Pharmacology, Monash University, Clayton, Victoria 3800, Australia.


Previous studies have described a biphasic cAMP response after stimulation of LGR7 by human gene 2 (H2) relaxin, involving both adenylate cyclase and PI3-kinase activity. The current study identifies the upstream involvement of Gi in the PI3-kinase-mediated response, likely the result of receptor signal switching. Amino acid sequence analysis of the LGR7 C-terminal tail and intracellular loops revealed multiple putative phosphorylation sites, suggesting that signal switching from Gs to Gi may occur after receptor phosphorylation. This study supports a time-dependent biphasic cAMP response: an initial short Gs-adenylate cyclase-mediated cAMP response is followed by receptor signal switching to a Gi-PI3-kinase-mediated response.

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