Introduction of RXFP4
Relaxin-3 Receptor 2 (RXFP4), also known as GPCR142 or GPR100, is encoded by the RXFP4 gene. It belongs to the G-protein-coupled receptor (GPCR) family, and is a high-affinity receptor for INSL5. It opened a new area for the research of the insulin-like peptides. It also acts as a receptor for RLN3/relaxin-3, as well as bradykinin and kallidin. RXFP4 and RXFP3 share about 40% amino acid identity and overall share 50% homology.
|Basic Information of RXFP4|
|Protein Name||Relaxin-3 Receptor 2|
|Aliases||RLN3R2, GPCR142, GPCR100|
|Organism||Homo sapiens (Human)|
Function of RXFP4 Membrane Protein
G proteins, resulting in the activation of adenylyl cyclase and elevating intracellular cAMP, mediate the activity of RXFP4. RXFP4 was activated by nanomolar concentrations of relaxin-3 but was completely unresponsive to all other known insulin-like peptides. Reverse transcriptase-PCR shows the expression of RXFP4 mRNA in a variety of human tissues and found that it is expressed in brain, kidney, testis, thymus, placenta, prostate, salivary gland, thyroid, and colon. Some scholars believe it may be involved in the regulation of glucose and lipid metabolism.
Fig.1 Relaxin family peptide receptors RXFP3 and RXFP4.
Application of RXFP4 Membrane Protein in Literature
Author’s team identified the insulin-like peptide relaxin-3 (aka INSL7) as the endogenous ligand for an orphan G-protein-coupled receptor. RXFP4 could also respond to relaxin-3 or related insulin-like molecules.
This article suggests that INSL5 is an endogenous ligand for RXFP4.
This article reveals that GPR100 was expressed predominantly in tissues like pancreas, heart, skeletal muscle, salivary gland, bladder, kidney, liver, placenta, stomach, jejunum, thyroid gland, ovary, and bone marrow, but smaller amounts were also detected in the brain and in cell lines derived from tumours of various origins.
This article suggests that the N-terminus and EL2 domains of RXFP3 and RXFP4 are involved in ligand binding while TM2, 3, and 5 are critical for receptor activation.
This article proposes probable electrostatic interactions between INSL5 and RXFP4: the B-chain central B13Arg of INSL5 interacts with both Asp104 and Glu182 of RXFP4, meanwhile the B-chain C-terminal B23Arg of INSL5 interacts with both Glu100 and Asp104 of RXFP4.
RXFP4 Preparation Options
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