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Relaxin GPCR Assays

Background of Relaxin Receptors

The relaxin family peptide (RXFP) receptors are a family of G protein-coupled receptors, that mediate the hormonal and neuropeptide actions on their endogenous ligands relaxin family peptides and insulin-like peptides (INSL). Relaxin is characterized by vasodilatory, anti-fibrotic, angiogenic, anti-apoptotic, and anti-inflammatory properties, which has therapeutic effects on organ damage prevention, cardiovascular diseases, renal disease, and asthma. Chronic RXFP1 targeting therapies are under development.

Structural features of the relaxin family peptide receptor RXFP1. Fig.1 Structural features of the relaxin family peptide receptor RXFP1. (Bathgate, 2013)

Distributions and Functions of Relaxin Receptors

The RXFP receptors are involved in the regulation of the cardiovascular system, formation of connective tissue and bone, reproduction, stress responses, anxiety and mood, arousal, spatial and social memory, and motivation. They are broadly distributed in the brain, reproductive tissues in both males and females, including semen, testis, ovary, pubic symphysis, cervix, uterus, and mammary glands, as well as in the heart, kidney, lung, thyroid, and colon.

Subtypes and Mechanisms of Relaxin Receptors

The family of RXFP receptors has 4 subtypes of G protein-coupled receptors, including RXFP1, RXFP2, RXFP3, and RXFP4 receptors. They promote signal transduction through Gs and Gi/Go proteins.

Receptor Gene Mechanism Agonists Antagonists
RXFP1 receptor RXFP1
  • RXFP1 receptor couples with Gs protein to stimulate adenylyl cyclase
  • RXFP1 receptor couples with Gi/Go protein to inhibit adenylyl cyclase
  • RXFP1 receptor couples to Gi3, activating AC5 through Gβγ-PI3K-PKCζ pathway
  • [33P]relaxin
  • europium-labelled relaxin
  • INSL-3
  • TamRLX
  • coumpound54
  • B-R13/17K relaxin
RXFP2 receptor RXFP2
  • RXFP2 receptor couples with Gs protein to stimulate adenylyl cyclase
  • RXFP2 receptor couples with Gi/Go protein to inhibit adenylyl cyclase
  • [33P]relaxin
  • [125I]INSL3
  • NanoLuc-INSL3
  • relaxin
  • relaxin-1
  • relaxin-3
  • TamRLX
  • A(9-26)INSL3
  • A(10-24)INSL3
  • A(C10/15S)INSL3
  • INSL3 B chain dimer analogue 8
  • A(Δ10/15C)INSL3
  • cyclic INSL3 B-chain analogue 6
RXFP3 receptor RXFP3
  • RXFP3 receptor couples with Gi/Go protein to inhibit adenylyl cyclase
  • RXFP3 receptor activation leads to GTPγS binding as well as ERK1/2 and p38MAP kinase phosphorylation
  • RXFP3 receptor couples to Gi2 in CHO cells, while in HEK293 cells couples to Gi3, GOB, or GOA proteins
  • [125I]relaxin-3
  • [125I]relaxin-3-B/INSL5 A chimera
  • R3/I5- SmBiT
  • DOTA/Eu relaxin-3
  • B1-27
  • H3 14s18 stapled B-chain
  • europium-labelled R3(B1-22R)
  • minimised relaxin-3 analogue 3
  • R3 B1-22R
  • R3(BΔ23-27)R/I5 chimeric peptide
RXFP4 receptor RXFP4
  • RXFP4 receptor couples with Gi/Go protein to inhibit adenylyl cyclase
  • RXFP4 receptor activation leads to ERK1/2, p38MAPK, Akt Ser473 and Thr308, and S6RP phosphorylation
  • [125I]relaxin-3
  • [125I]relaxin-3-B/INSL5 A chimera
  • R3/15
  • ΔR3/I5
  • compound 7a
  • R3(BΔ23-27)R/I5 chimeric peptide
  • INSL5-A13NR
  • minimised relaxin-3 analogue 3


RXFP1 RXFP3 RXFP4
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX856 Magic™ Rabbit RXFP1 In Vitro cAMP Assay CHO-K1 cAMP Assay
S01YF-1122-KX857 Magic™ Rat RXFP1 In Vitro cAMP Assay CHO-K1 cAMP Assay
S01YF-1122-KX853 Magic™ Dog RXFP1 In Vitro cAMP Assay CHO-K1 cAMP Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX858 Magic™ Human RXFP3 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX860 Magic™ Human RXFP3 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX861 Magic™ Human RXFP4 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
[35S]GTPγS Binding Assay
S01YF-1122-KX863 Magic™ Human RXFP4 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay
S01YF-1122-KX864 Magic™ Mouse RXFP4 In Vitro [35S]GTPγS binding Assay CHO-K1 [35S]GTPγS binding Assay

Reference

  1. Bathgate, R. A. D.; et al. Relaxin family peptides and their receptors. Physiological reviews. 2013, 93(1): 405-480.
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