Signalling profiles of H3 relaxin, H2 relaxin and R3(BΔ23-27)R/I5 acting at the relaxin family peptide receptor 3 (RXFP3).

ABSTRACT:

Background and purpose

Relaxin family peptide receptor 3 (RXFP3) is expressed in brain areas important for processing sensory information and feeding, suggesting that it may be a target for anti-anxiety and anti-obesity drugs. We examined the effects of H3 relaxin, the biased agonist H2 relaxin and the antagonist, R3(BΔ23-27)R/I5, on RXFP3 signalling to establish their suitability as tools to assess the physiological roles of RXFP3.

Experimental approach

The signalling profile of the RXFP3 ligands was determined using reporter gene assays, multiplexed signalling assays and direct examination of receptor-G protein and receptor-β-arrestin interactions using BRET.

Key results

H2 relaxin activated p38MAPK and ERK1/2 with lower efficacy than H3 relaxin, but had similar eff

SUBMITTER: Kocan M 

PROVIDER: S-EPMC4243858 | biostudies-literature | 2014 Jun

REPOSITORIES: biostudies-literature