Relaxin/insulin-like family peptide receptor 1

Protein-coding gene in the species Homo sapiens

RXFP1

Available structures

Ortholog search: PDBe RCSB

List of PDB id codes
2JM4, 2M7P

Identifiers

Aliases

RXFP1, LGR7, RXFPR1, Relaxin/insulin-like family peptide receptor 1, relaxin/insulin like family peptide receptor 1, relaxin family peptide receptor 1

External IDs

OMIM: 606654; MGI: 2682211; HomoloGene: 11007; GeneCards: RXFP1; OMA:RXFP1 - orthologs

Gene location (Human)

Chr.	Chromosome 4 (human)

Band	4q32.1	Start	158,315,311 bp
Band	4q32.1	End	158,653,372 bp

Gene location (Mouse)

Chr.	Chromosome 3 (mouse)

Band	3\|3 E3	Start	79,548,918 bp
Band	3\|3 E3	End	79,645,187 bp

RNA expression pattern

Bgee

Human

Mouse (ortholog)

Top expressed in

decidua

endothelial cell

endometrium

Brodmann area 46

testicle

prefrontal cortex

Brodmann area 9

superior frontal gyrus

Brodmann area 23

cingulate gyrus

Top expressed in

uterus

genital tubercle

primary visual cortex

superior frontal gyrus

cervix

dentate gyrus of hippocampal formation granule cell

atrioventricular valve

muscle of thigh

hippocampus proper

cerebellar cortex

More reference expression data

BioGPS

n/a

Gene ontology
Molecular function	G protein-coupled receptor activity protein binding signal transducer activity metal ion binding G protein-coupled peptide receptor activity
Cellular component	integral component of membrane membrane plasma membrane intracellular anatomical structure integral component of plasma membrane
Biological process	signal transduction adenylate cyclase-modulating G protein-coupled receptor signaling pathway G protein-coupled receptor signaling pathway adenylate cyclase-activating G protein-coupled receptor signaling pathway activation of adenylate cyclase activity hormone-mediated signaling pathway
Sources:Amigo / QuickGO

Orthologs

Species

Human

Mouse

Entrez


59350


381489

Ensembl


ENSG00000171509


ENSMUSG00000034009

UniProt


Q9HBX9


Q6R6I7

RefSeq (mRNA)

NM_001253727 NM_001253728 NM_001253729 NM_001253730 NM_001253732
NM_001253733 NM_021634 NM_001363776


NM_212452

RefSeq (protein)

NP_001240656 NP_001240657 NP_001240658 NP_001240659 NP_001240661
NP_001240662 NP_067647 NP_001350705


NP_997617

Location (UCSC)

Chr 4: 158.32 – 158.65 Mb

Chr 3: 79.55 – 79.65 Mb

PubMed search

Wikidata

View/Edit Human

View/Edit Mouse

Relaxin/insulin-like family peptide receptor 1, also known as RXFP1, is a human G protein coupled receptor that is one of the relaxin receptors. It is a rhodopsin-like GPCR which is unusual in this class as it contains a large extracellular binding and signalling domain. Some reports suggest that RXFP1 forms homodimers, however the most recent evidence indicates that relaxin binds a non-homodimer of RXFP1.

References

^ GRCh38: Ensembl release 89: ENSG00000171509 – Ensembl, May 2017
^ GRCm38: Ensembl release 89: ENSMUSG00000034009 – Ensembl, May 2017
"Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
"Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
"Entrez Gene: RXFP1 relaxin/insulin-like family peptide receptor 1".
Sethi A, Bruell S, Patil N, Hossain MA, Scott DJ, Petrie EJ, et al. (April 2016). "The complex binding mode of the peptide hormone H2 relaxin to its receptor RXFP1". Nature Communications. 7 (1): 11344. Bibcode:2016NatCo...711344S. doi:10.1038/ncomms11344. PMC 4837482. PMID 27088579.
Svendsen AM, Zalesko A, Kønig J, Vrecl M, Heding A, Kristensen JB, et al. (December 2008). "Negative cooperativity in H2 relaxin binding to a dimeric relaxin family peptide receptor 1" (PDF). Molecular and Cellular Endocrinology. 296 (1–2): 10–7. doi:10.1016/j.mce.2008.07.014. PMID 18723073. S2CID 32739782.
Kern A, Hubbard D, Amano A, Bryant-Greenwood GD (March 2008). "Cloning, expression, and functional characterization of relaxin receptor (leucine-rich repeat-containing g protein-coupled receptor 7) splice variants from human fetal membranes". Endocrinology. 149 (3): 1277–94. doi:10.1210/en.2007-1348. PMC 2275365. PMID 18079195.
Hoare BL, Bruell S, Sethi A, Gooley PR, Lew MJ, Hossain MA, et al. (January 2019). "Multi-Component Mechanism of H2 Relaxin Binding to RXFP1 through NanoBRET Kinetic Analysis". iScience. 11: 93–113. Bibcode:2019iSci...11...93H. doi:10.1016/j.isci.2018.12.004. PMC 6309025. PMID 30594862.
Hoare BL, Kocan M, Bruell S, Scott DJ, Bathgate RA (August 2019). "Using the novel HiBiT tag to label cell surface relaxin receptors for BRET proximity analysis". Pharmacology Research & Perspectives. 7 (4): e00513. doi:10.1002/prp2.513. PMC 6667744. PMID 31384473.

Bathgate RA, Ivell R, Sanborn BM, Sherwood OD, Summers RJ (May 2005). "Receptors for relaxin family peptides". Annals of the New York Academy of Sciences. 1041 (1): 61–76. Bibcode:2005NYASA1041...61B. doi:10.1196/annals.1282.010. PMID 15956688. S2CID 1185573.
Bathgate RA, Ivell R, Sanborn BM, Sherwood OD, Summers RJ (March 2006). "International Union of Pharmacology LVII: recommendations for the nomenclature of receptors for relaxin family peptides". Pharmacological Reviews. 58 (1): 7–31. doi:10.1124/pr.58.1.9. PMID 16507880. S2CID 7466039.
Hsu SY, Kudo M, Chen T, Nakabayashi K, Bhalla A, van der Spek PJ, et al. (August 2000). "The three subfamilies of leucine-rich repeat-containing G protein-coupled receptors (LGR): identification of LGR6 and LGR7 and the signaling mechanism for LGR7". Molecular Endocrinology. 14 (8): 1257–71. doi:10.1210/me.14.8.1257. PMID 10935549.
Bartsch O, Bartlick B, Ivell R (September 2001). "Relaxin signalling links tyrosine phosphorylation to phosphodiesterase and adenylyl cyclase activity". Molecular Human Reproduction. 7 (9): 799–809. doi:10.1093/molehr/7.9.799. PMID 11517286.
Hsu SY, Nakabayashi K, Nishi S, Kumagai J, Kudo M, Sherwood OD, Hsueh AJ (January 2002). "Activation of orphan receptors by the hormone relaxin". Science. 295 (5555): 671–4. Bibcode:2002Sci...295..671H. doi:10.1126/science.1065654. PMID 11809971. S2CID 32693420.
Sudo S, Kumagai J, Nishi S, Layfield S, Ferraro T, Bathgate RA, Hsueh AJ (March 2003). "H3 relaxin is a specific ligand for LGR7 and activates the receptor by interacting with both the ectodomain and the exoloop 2". The Journal of Biological Chemistry. 278 (10): 7855–62. doi:10.1074/jbc.M212457200. PMID 12506116.
Ivell R, Balvers M, Pohnke Y, Telgmann R, Bartsch O, Milde-Langosch K, et al. (November 2003). "Immunoexpression of the relaxin receptor LGR7 in breast and uterine tissues of humans and primates". Reproductive Biology and Endocrinology. 1: 114. doi:10.1186/1477-7827-1-114. PMC 293425. PMID 14633277.
Luna JJ, Riesewijk A, Horcajadas JA, Van Os RD, Domínguez F, Mosselman S, et al. (February 2004). "Gene expression pattern and immunoreactive protein localization of LGR7 receptor in human endometrium throughout the menstrual cycle". Molecular Human Reproduction. 10 (2): 85–90. doi:10.1093/molehr/gah019. PMID 14742692.
Bond CP, Parry LJ, Samuel CS, Gehring HM, Lederman FL, Rogers PA, Summers RJ (July 2004). "Increased expression of the relaxin receptor (LGR7) in human endometrium during the secretory phase of the menstrual cycle". The Journal of Clinical Endocrinology and Metabolism. 89 (7): 3477–85. doi:10.1210/jc.2003-030798. PMID 15240635.
Liu C, Chen J, Kuei C, Sutton S, Nepomuceno D, Bonaventure P, Lovenberg TW (January 2005). "Relaxin-3/insulin-like peptide 5 chimeric peptide, a selective ligand for G protein-coupled receptor (GPCR)135 and GPCR142 over leucine-rich repeat-containing G protein-coupled receptor 7". Molecular Pharmacology. 67 (1): 231–40. doi:10.1124/mol.104.006700. PMID 15465925. S2CID 25164369.
Scott DJ, Layfield S, Riesewijk A, Morita H, Tregear GW, Bathgate RA (November 2004). "Identification and characterization of the mouse and rat relaxin receptors as the novel orthologues of human leucine-rich repeat-containing G-protein-coupled receptor 7". Clinical and Experimental Pharmacology & Physiology. 31 (11): 828–32. doi:10.1111/j.1440-1681.2004.04075.x. PMID 15566402. S2CID 22463239.
Büllesbach EE, Schwabe C (April 2005). "The trap-like relaxin-binding site of the leucine-rich G-protein-coupled receptor 7". The Journal of Biological Chemistry. 280 (14): 14051–6. doi:10.1074/jbc.M500030200. PMID 15695505.
Tang M, Mazella J, Zhu HH, Tseng L (April 2005). "Ligand activated relaxin receptor increases the transcription of IGFBP-1 and prolactin in human decidual and endometrial stromal cells". Molecular Human Reproduction. 11 (4): 237–43. doi:10.1093/molehr/gah149. PMID 15722441.
Hopkins EJ, Bathgate RA, Gooley PR (May 2005). "The human LGR7 low-density lipoprotein class A module requires calcium for structure". Annals of the New York Academy of Sciences. 1041 (1): 27–34. Bibcode:2005NYASA1041...27H. doi:10.1196/annals.1282.006. PMID 15956684. S2CID 12876694.
Bond CP, Parry LJ, Samuel CS, Gehring HM, Lederman FL, Rogers PA, Summers RJ (May 2005). "Increased expression of the relaxin receptor (LGR7) in human endometrium during the secretory phase of the menstrual cycle". Annals of the New York Academy of Sciences. 1041 (1): 136–43. Bibcode:2005NYASA1041..136B. doi:10.1196/annals.1282.020. PMID 15956698. S2CID 38242216.
Halls ML, Bathgate RA, Summers RJ (May 2005). "Signal switching after stimulation of LGR7 receptors by human relaxin 2". Annals of the New York Academy of Sciences. 1041 (1): 288–91. Bibcode:2005NYASA1041..288H. doi:10.1196/annals.1282.042. PMID 15956719. S2CID 42606513.
Muda M, He C, Martini PG, Ferraro T, Layfield S, Taylor D, et al. (August 2005). "Splice variants of the relaxin and INSL3 receptors reveal unanticipated molecular complexity". Molecular Human Reproduction. 11 (8): 591–600. doi:10.1093/molehr/gah205. PMID 16051677.

v t e PDB gallery
2jm4: The solution NMR structure of the relaxin (RXFP1) receptor LDLa module.

External links

"Relaxin Family Peptide Receptors: RXFP1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2016-03-03. Retrieved 2008-12-09.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

Cell surface receptor: G protein-coupled receptors

Class A: Rhodopsin-like

Neurotransmitter

Adrenergic	α1 (A B D) α2 (A B C) β1 β2 β3
Purinergic	Adenosine (A1 A2A A2B A3) P2Y (1 2 4 5 6 8 9 10 11 12 13 14)
Serotonin	(all but 5-HT3) 5-HT1 (A B D E F) 5-HT2 (A B C) 5-HT (4 5A 6 7)
Other	Acetylcholine (M1 M2 M3 M4 M5) Dopamine D1 D2 D3 D4 D5 GHB receptor Histamine H1 H2 H3 H4 Melatonin (1A 1B 1C) TAAR (1 2 5 6 8 9)

Metabolites and
signaling molecules

Eicosanoid	CysLT (1 2) LTB4 1 2 FPRL1 OXE Prostaglandin DP (1 2), EP (1 2 3 4), FP Prostacyclin Thromboxane
Other	Bile acid Cannabinoid (CB1 CB2, GPR (18 55 119)) EBI2 Estrogen Free fatty acid (1 2 3 4) Hydroxycarboxylic acids 1 2 3 Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Oxoglutarate PAF Sphingosine-1-phosphate (1 2 3 4 5) Succinate

Peptide

Neuropeptide

B/W (1
2)
FF (1
2)
S
Y (1
2
4
5)
Neuromedin (B
U (1
2))
Neurotensin (1
2)

Other

Anaphylatoxin (C3a
C5a (1
2))
Angiotensin (1
2)
Apelin
Bombesin
- BRS3
- GRPR
- NMBR)
- Bradykinin (B1
- B2)
Chemokine
Cholecystokinin (A
B)
Endothelin
- A
- B
Formyl peptide (1
2
3)
FSH
Galanin (1
2
3)
Gonadotropin-releasing hormone (1
2)
Ghrelin
Kisspeptin
Luteinizing hormone/choriogonadotropin
MAS (1
1L
D
E
F
G
X1
X2
X3
X4)
Melanocortin (1
2
3
4
5)
MCHR (1
2)
Motilin
Opioid (Delta
Kappa
Mu
Nociceptin & Zeta, but not Sigma)
Orexin (1
2)
Oxytocin
Prokineticin (1
2)
Prolactin-releasing peptide
Relaxin (1
2
3
4)
Somatostatin (1
2
3
4
5)
Tachykinin (1
2
3)
Thyrotropin
Thyrotropin-releasing hormone
Urotensin-II
Vasopressin (1A
1B
2)

Miscellaneous

Taste, bitter	TAS2R 1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60 Vomeronasal receptor type 1
Orphan	GPR (1 3 4 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 78 81 82 83 84 85 87 88 92 101 103 109A 109B 119 120 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183)
Other	Adrenomedullin Olfactory Opsin (3 4 5 1LW 1MW 1SW RGR RRH) Protease-activated (1 2 3 4) SREB (1 2 3)

Class B: Secretin-like

Adhesion	ADGRB Brain-specific angiogenesis inhibitor 1 2 3 ADGRC Cadherin 1 2 3 ADGRE EMR 1 2 3 CD97 ADGRG 1 2 3 4 5 6 7 ADGRL Latrophilin 1 2 3 ELTD1
Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)
Other	Calcitonin CALCRL Corticotropin-releasing hormone (1 2) Glucagon (GR GIPR GLP1R GLP2R) Growth-hormone-releasing hormone PACAPR1 GPR Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C: Metabotropic glutamate / pheromone

Taste, sweet	TAS1R 1 2 3 Vomeronasal receptor, type 2
Other	Calcium-sensing receptor GABA_B (1 2) Glutamate receptor (Metabotropic glutamate (1 2 3 4 5 6 7 8)) GPRC6A GPR (156 158 179) RAIG (1 2 3 4)

Class F: Frizzled & Smoothened

Frizzled	Frizzled (1 2 3 4 5 6 7 8 9 10)
Smoothened	Smoothened

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