Journal article

Real-time examination of cAMP activity at relaxin family peptide receptors using a BRET-based biosensor

Adam L Valkovic, Miranda B Leckey, Alice R Whitehead, Mohammed A Hossain, Asuka Inoue, Martina Kocan, Ross AD Bathgate

PHARMACOLOGY RESEARCH & PERSPECTIVES | JOHN WILEY & SONS LTD | Published : 2018

Abstract

Relaxin family peptide (RXFPs) 1-4 receptors modulate the activity of cyclic adenosine monophosphate (cAMP) to produce a range of physiological functions. RXFP1 and RXFP2 increase cAMP via Gαs, whereas RXFP3 and RXFP4 inhibit cAMP via Gαi/o. RXFP1 also shows a delayed increase in cAMP downstream of Gαi3. In this study we have assessed whether the bioluminescence resonance energy transfer (BRET)-based biosensor CAMYEL (cAMP sensor using YFP-Epac-Rluc), which allows real-time measurement of cAMP activity in live cells, will aid in understanding ligand- and cell-specific RXFP signaling. CAMYEL detected concentration-dependent changes in cAMP activity at RXFP1-4 in recombinant cell lines, using ..

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Grants

Awarded by Japan Agency for Medical Research and Development


Awarded by Japan Society for the Promotion of Science


Awarded by National Health and Medical Research Council


Funding Acknowledgements

Japan Agency for Medical Research and Development, Grant/Award Number: JP17gm5910013; Japan Society for the Promotion of Science, Grant/Award Number: 17K08264; National Health and Medical Research Council, Grant/Award Number: 1043750, 1100676; Victorian Government Operational Infrastructure Support Program