Recombinant Human Relaxin receptor 1 (RXFP1)

1. Binding of relaxin to RXFP1 recruits G proteins with subsequent activation of adenylyl cyclase and elevation of cAMP. PMID:27310652
2. The decreased expression of the endometrial RLX receptor in women with implantation failures, both in vitro fertilization failure and recurrent pregnancy loss, suggests that RLX may play a crucial role in the structural and functional changes of the endometrium during the window of implantation. PMID:26761440
3. Hormone receptor expression was concentrated in the fibroblasts, and RXFP1 was also evident in blood vessels and nerves PMID:28076930
4. The complex binding mode of the peptide hormone H2 relaxin to its receptor RXFP1 has been deciphered. PMID:27088579
5. RXFP1 gene expression was dysregulated in the anterior cingulate of bipolar patients. PMID:26238605
6. H2 relaxin amide is fully active at the relaxin receptor RXFP1 and thus dimerization is not required for biological activity. PMID:25547165
7. Synthetic covalently linked dimeric form of H2 relaxin retains native RXFP1 activity and has improved in vitro serum stability. PMID:25685807
8. Using cells stably expressing RXFP1, we found that relaxin regulation of PPARgamma activity requires accumulation of cAMP and subsequent activation of cAMP-dependent protein kinase (PKA). PMID:25389293
9. RXFP-1 receptors are present at the ligament, cartilage, and synovium of the TM joint, indicating that it is a potential target for relaxin. This suggests that circulating relaxin may impact joint stability. PMID:24797570
10. To create a tool to investigate the low-affinity interaction, a protein scaffold system displaying exoloops 1 and 2 from RXFP1 was designed. PMID:24640555
11. RXFP1, is a complex G-protein coupled receptor (GPCR)and has a rhodopsin-like 7 transmembrane helix region and a large ecto-domain containing Leucine-rich repeats and a Low Desnsity Lipoprotein Class-A module at the N-terminus. PMID:24640556
12. We have developed and assessed four microRNA against human RXFP1. PMID:24640558
13. The development of a quantitative high-throughput platform for an RXFP1 agonist screen. PMID:23212924
14. Report increased expression of RXFP1 in placenta of patients with placenta accreta. PMID:23302396
15. the RXFP1 receptor lacking the LDLa module binds ligand normally but cannot signal through any characterized G protein-coupled receptor signaling pathway PMID:23926099
16. These results provide new mechanistic insights into the binding and activation events of RXFP1 and RXFP2 by their native hormone ligands. PMID:22973049
17. Identification of key residues essential for the structural fold and receptor selectivity within the A-chain of human gene-2 (H2) relaxin PMID:23024363
18. The decreased cellular expression of relaxin-2 receptor RXFP1 in scleroderma skin might represent a pro-fibrotic factor and contribute to the substantial inefficacy of relaxin treatment in systemic sclerosis, as reported in the literature. PMID:23043266
19. relaxin-2 and its receptors RXFP1 and RXFP2 are expressed in GSV and their expression is significantly decreased in varicose GSV PMID:22737225
20. [review] The relaxin receptor RXFP1 localizes in the acrosomal region of sperm. PMID:22180889
21. Decrease in the expression of relaxin receptor in the placenta is related with the occurrence and development of preeclampsia. PMID:18843967
22. LGR7 is constitutively expressed in human endometrium, and an increased LGR7 immunostaining is demonstrated in the secretory phase, confirming the involvement of relaxin in the physiology of endometrium and suggesting its role in implantation. PMID:21324453
23. Endometrial expression of relaxin and relaxin receptor in endometriosis. PMID:20655530
24. Uncovered is a pre-assembled, constitutively active G-protein-coupled receptor signalosome, that couples the relaxin receptor, relaxin family peptide receptor 1 (RXFP1), to cAMP following receptor stimulation with sub-picomolar concentrations of peptide. PMID:20664520
25. These results suggest that relaxin activates PPARgamma activity and increases the overall response in the presence of PPARgamma agonists, and that this activation is dependent on the presence of RXFP1. PMID:19712722
26. capable of mediating the action of relaxin through an adenosine 3',5'-monophosphate (cAMP)-dependent pathway PMID:11809971
27. Gene expression pattern and protein localization of LGR7 receptor in human endometrium throughout the menstrual cycle. PMID:14742692
28. Binding to and gene expression of the LGR7 relaxin receptor changes markedly with the phases of the menstrual cycle, suggesting a specific role for the hormone in the physiology of the human uterus. PMID:15240635
29. Substitution of the relaxin-3 A-chain with the A-chain from insulin-like peptide 5 results in a chimeric peptide that selectively activates GPCR135 and GPCR142 over LGR7. PMID:15465925
30. mouse and rat LGR7 share 85.2 and 85.7% identity with human LGR7 PMID:15566402
31. Data describe the conformation of the relaxin-binding site of the leucine-rich G-protein-coupled receptor 7. PMID:15695505
32. Relaxin receptor (LGR7) increases the transcription of IGFBP-1 and prolactin in decidual and endometrial stromal cells through the promoter region containing multiple CCAAT/enhancer-binding proteins (C/EBP) binding sites. PMID:15722441
33. human LGR7 LDL-A module NMR studies; demonstration that calicum is required for the module to form a stable and correctly folded structure PMID:15956684
34. increase in LGR7 expression and H2 relaxin binding in the secretory phase of the menstrual cycle suggests a specific role for relaxin after ovulation in the human uterus PMID:15956698
35. Amino acid sequence analysis of the LGR7 C-terminal tail and intracellular loops revealed multiple putative phosphorylation sites, suggesting that signal switching from Gs to Gi may occur after receptor phosphorylation PMID:15956719
36. LGR7.10 splice variant is expressed at the cell surface, LGR7.2 is predominantly retained within cells and LGR7.1 is partially secreted. None stimulates cAMP production. PMID:16051677
37. Relaxin stimulates leukocyte adhesion and migration through a relaxin receptor LGR7-dependent mechanism PMID:16303766
38. The essential role of the LDLa module in LGR7 and LGR8 function is reported. PMID:16963451
39. Specific residues in the N-terminal region of the RXFP1 receptor low density lipoprotein receptor class A (LDLa) module play a key role in receptor activation. PMID:17148455
40. The LDL-A module of LGR7 influences receptor maturation, cell surface expression, and relaxin-activated signal transduction. PMID:17158203
41. The dominant-negative effects of the LGR7 splice variants expressed in the chorion and decidua could be functionally significant in the peripartal period. PMID:18079195
42. analysis of truncated human relaxin-2 and -3 (H2 and H3) relaxin peptides and their binding and cAMP activities on RXFP1, RXFP2, and RXFP3 PMID:18434306
43. N-glycosylation at Asn-303 of RXFP1 was required for optimal intracellular cAMP signaling PMID:18533687
44. RXFP1 is a constitutive dimer with negative cooperativity in ligand binding, and dimerization occurs through the 7TM domain, and that the ectodomain has a stabilizing effect on this interaction. PMID:18723073
45. The autocrine/paracrine actions of relaxin in the decidua are under additional controls at the level of expression of its receptor on the surface of its target cells. PMID:19116340
46. The apparent lack of classical regulation for RXFP1 and RXFP2 provides the molecular basis for the prolonged signaling and physiological actions of relaxin and related peptides PMID:19279230
47. Point mutations of conserved residues or complete deletion of the LDL-A module resulted in loss of the cAMP response to relaxin PMID:19416160
48. Ligand-mediated activation of RXFP1 and RXFP2 is a complex process involving various domains of the receptors PMID:19416161
49. Relaxin binds to RXFP2 with high affinity, although INSL3 has a very poor affinity for RXFP1 PMID:19416162
50. Data tested the hypothesis that relaxin plays a role in endometriosis by comparing the expression of relaxin mRNA and its LGR7 (RXFP1) receptor mRNA in normal human endometrium to those in samples from patients with endometriosis. PMID:19416175

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HGNC: 19718

UNIGENE: Hs.591686

KEGG: hsa:59350

STRING: 9606.ENSP00000303248

OMIM: 606654