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FLASH GENE
Symbol RXFP1 contributors: mct/npt - updated : 29-11-2014
HGNC name relaxin/insulin-like family peptide receptor 1
HGNC id 19718
PROTEIN
PHYSICAL PROPERTIES
STRUCTURE
motifs/domains
  • a low density lipoprotein receptor cysteine-rich motif, class A (LDL-A) module at the N terminus, influencing receptor maturation, cell surface expression, and relaxin-activated signal transduction, and essential for receptor activation
  • 10 LRR domains
  • six putative Asn-linked glycosylation sites in the ectodomain at positions Asn-14, Asn-105, Asn-242, Asn-250, Asn-303, and Asn-346 (Yan 2008)
  • seven transmembrane region
  • a unique C-terminal tail with LDLa module and a phosphorylation site, important in agonist-stimulated receptor internalization (Kern 2009), and four acidic AAs in the C-terminal region of the RXFP1 LDLa with the ligand binding domain (LB2) modules whose ligation of a Ca2+ is crucial for maintaining structural integrity
  • secondary structure
  • large extracellular domain containing the characteristic leucine-rich repeats formed by alph-helices and beta-sheets (
  • mono polymer homomer , dimer
    HOMOLOGY
    Homologene
    FAMILY
  • leucine-rich repeat containing G protein-coupled receptors subgroup C
  • CATEGORY receptor membrane G
    SUBCELLULAR LOCALIZATION     plasma membrane
        intracellular
    intracellular,cytoplasm,organelle,endosome
    intracellular,cytoplasm,cytosolic,vesicle
    text
  • homodimerization of WT-LGR7 has been shown here to take place in the endoplasmic reticulum (Kern 2008)
  • nonsecretory adaptor protein that localizes to endosomal vesicles (Del Fattore2008)
  • basic FUNCTION
  • relaxin receptor having rhodopsin-like receptor activity
  • forms dimers/oligomers during its biosynthesis and trafficking to the plasma membrane (Kern 2009)
  • membrane receptor, critically involved in relaxin agonist interaction with glucocorticoid receptor (GR) (Dschietzig 2009)
  • on spermatids and Sertoli cells may be important in spermatogenesis (Filonzi 2007)
  • cognate relaxin receptor that mainly signals through cyclic AMP second messenger.
  • RXFP1 and RXFP2 are unique in both the leucine-rich repeat-containing GPCR and GPCR family in that they have a low density lipoprotein receptor (LDLr) class A (LDLa) module at their N termini (pMID: 23926099)
  • CELLULAR PROCESS
    PHYSIOLOGICAL PROCESS
    PATHWAY
    metabolism
    signaling
    a component
    INTERACTION
    DNA
    RNA
    small molecule
    protein
  • receptor for relaxins (RLN1 and RLN2)
  • RLN3 is thought to act in the brain via the RXFP3 receptor, although the RXFP1 receptor may also play a role
  • RLN3 exerts antifibrotic actions via RXFP1 and may enhance the collagen-inhibitory effects of RLN2
  • relaxin mediated activation of RXFP1 requires multiple, coordinated interactions between the ligand and various receptor domains including a high affinity interaction involving the LRRs, and a predicted lower affinity interaction involving the extracellular loops (ELs)
  • cell & other
    REGULATION
    induced by relaxin in osteoclasts (Ferlin 2010)
    Other regulated by the LDLa module (essential role in RXFP2 and RXFP1 function)
    regulated by N-glycosylation (N-glycosylation is essential for the transport of the receptor to the cell surface and likely glycosylation is also essential for the conformational changes required for G-protein coupling and subsequent cAMP signaling) (Yan 2008)
    ASSOCIATED DISORDERS
    corresponding disease(s)
    Other morbid association(s)
    TypeGene ModificationChromosome rearrangementProtein expressionProtein Function
    constitutional     --over  
    in endometrium during the secretory phase of the menstrual cycle
    constitutional     --low  
    in scleroderma skin, with a lack of staining in most cells
    Susceptibility
    Variant & Polymorphism
    Candidate gene
    Marker
    Therapy target
    ANIMAL & CELL MODELS