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Genomes and Genes | RXFP3SummaryGene Symbol: RXFP3 Description: relaxin/insulin-like family peptide receptor 3 Alias: GPCR135, RLN3R1, RXFPR3, SALPR, G-protein coupled receptor GPCR135, G-protein coupled receptor SALPR, RLN3 receptor 1, g protein-coupled receptor SALPR, relaxin 3 receptor 1, relaxin family peptide receptor 3, relaxin-3 receptor 1, somatostatin and angiotensin-like peptide receptor, somatostatin- and angiotensin-like peptide receptor Species: human Top Publications
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Publications
Distribution of G-protein-coupled receptor (GPCR)135 binding sites and receptor mRNA in the rat brain suggests a role for relaxin-3 in neuroendocrine and sensory processingSteven W Sutton
Neuroscience Group, Johnson and Johnson Pharmaceutical Research and Development, LLC, 3210 Merryfield Row, San Diego, CA 92121, USA
Neuroendocrinology 80:298-307. 2004G-protein-coupled receptor 135 (GPCR135), a former orphan GPCR also known as SALPR, has recently been shown to be modulated by relaxin-3 (R3)...
Relaxin-3: improved synthesis strategy and demonstration of its high-affinity interaction with the relaxin receptor LGR7 both in vitro and in vivoRoss A D Bathgate
Howard Florey Institute, University of Melbourne, Melbourne, Victoria 3010, Australia
Biochemistry 45:1043-53. 2006..Although the highest activity was demonstrated on the human relaxin-3 receptor (GPCR135), the peptide also showed high activity on relaxin receptors (LGR7) from various species and variable activity on ..
Roles of the receptor, the ligand, and the cell in the signal transduction pathways utilized by the relaxin family peptide receptors 1-3Roger J Summers
Department of Pharmacology, Monash Institute of Pharmaceutical Sciences, Monash University, Clayton, Victoria, Australia
Ann N Y Acad Sci 1160:99-104. 2009..RXFP1 and 2 are characterized by large extracellular domains containing leucine-rich repeats, whereas RXFP3 and 4 closely resemble small-peptide-liganded GPCRs...
Relaxin receptors--new drug targets for multiple disease statesE T van der Westhuizen
Department of Pharmacology, Monash University, Wellington Road, Clayton, Victoria 3800, Australia
Curr Drug Targets 8:91-104. 2007..The recent de-orphanisation of four receptors LGR7, LGR8, GPCR135 (SALPR) and GPCR142 (GPR100) that respond to and bind at least one of the three forms of relaxin identified to ..
Relaxin-3 systems in the brain--the first 10 yearsCraig M Smith
Florey Neuroscience Institutes, The University of Melbourne, Victoria, Australia
J Chem Neuroanat 42:262-75. 2011..of the peptide, including the identification of its cognate receptor (a type 1 G-protein coupled receptor, GPCR135 or RXFP3), an understanding of its structure-activity and associated cellular signalling, and the elucidation of ..
Addition of a carboxy-terminal green fluorescent protein does not alter the binding and signaling properties of relaxin family Peptide receptor 3Emma T Van der Westhuizen
Department of Pharmacology, Monash Institute of Pharmaceutical Sciences, Monash University, Clayton, Victoria 3800, Australia
Ann N Y Acad Sci 1160:105-7. 2009The relaxin family peptide receptor 3 (RXFP3) is the cognate receptor for the neuropeptide relaxin-3...
Probing the functional domains of relaxin-3 and the creation of a selective antagonist for RXFP3/GPCR135 over relaxin receptor RXFP1/LGR7Changlu Liu
Johnson and Johnson Pharmaceutical Research and Development, LLC, San Diego, California 92121, USA
Ann N Y Acad Sci 1160:31-7. 2009Both relaxin-3 and its receptor (RXFP3, also known as GPCR135) are predominantly expressed in brain regions known to play important roles in processing sensory signals...
Structural properties of relaxin chimerasLinda M Haugaard-Jönsson
School of Pure and Applied Natural Sciences, University of Kalmar, Kalmar, Sweden
Ann N Y Acad Sci 1160:27-30. 2009Relaxin-3 interacts with high potency with three relaxin family peptide receptors (RXFP1, RXFP3, and RXFP4)...
De novo design and synthesis of cyclic and linear peptides to mimic the binding cassette of human relaxinMohammed Akhter Hossain
Howard Florey Institute, University of Melbourne, Parkville, Victoria, Australia
Ann N Y Acad Sci 1160:16-9. 2009..None showed any binding affinity for RXFP1, RXFP2, or RXFP3, indicating that the key residues were either incorrectly oriented or that additional residues are required for ..
Structure and activity in the relaxin family of peptidesGeoffrey W Tregear
Department of Biochemistry and Molecular Biology, Howard Florey Institute, University of Melbourne, Parkville, Victoria, Australia
Ann N Y Acad Sci 1160:5-10. 2009..on structure and function relates to the relaxin-RXFP1, insulin-like peptide 3 (INSL3)-RXFP2, and relaxin-3-RXFP3 systems, with information accumulating not only on the critical ligand structures but also the domains and ..
Solid phase synthesis and structural analysis of novel A-chain dicarba analogs of human relaxin-3 (INSL7) that exhibit full biological activityMohammed Akhter Hossain
Howard Florey Institute, University of Melbourne, Victoria, 3010, Australia
Org Biomol Chem 7:1547-53. 2009..Both peptides demonstrated binding affinities that were equivalent to native H3 relaxin on RXFP1 and RXFP3 expressing cells...
The structural and functional role of the B-chain C-terminal arginine in the relaxin-3 peptide antagonist, R3(BDelta23-27)R/I5Mohammed Akhter Hossain
Howard Florey Institute, University of Melbourne, Melbourne, Victoria 3010, Australia
Chem Biol Drug Des 73:46-52. 2009..It is highly expressed in the brain and is the endogenous ligand for the receptor RXFP3. As relaxin-3 also interacts with the relaxin receptor RXFP1, selective agonists and antagonists are crucial for ..
Relaxin-3 and RXFP3 expression, and steroidogenic actions in the ovary of teleost fishBrian C Wilson
Department of Biology, Acadia University, Wolfville, Nova Scotia, Canada
Comp Biochem Physiol A Mol Integr Physiol 153:69-74. 2009..Ovarian expression of relaxin-3a, d and f genes, and the relaxin-3 receptor gene Rxfp3, was studied in Danio rerio using RT-PCR...
Relaxin family peptide receptors--from orphans to therapeutic targetsEmma T Van der Westhuizen
Department of Pharmacology, Monash University, Clayton, 3800 Vic, Australia
Drug Discov Today 13:640-51. 2008..are the cognate ligands for 4 G-protein-coupled relaxin family peptide receptors (RXFPs; formerly LGR7, LGR8, GPCR135, GPCR142)...
Identification of the domains in RXFP4 (GPCR142) responsible for the high affinity binding and agonistic activity of INSL5 at RXFP4 compared to RXFP3 (GPCR135)Jessica Zhu
Johnson and Johnson Pharmaceutical Research and Development, L L C, 3210 Merryfield Row, San Diego, CA 92121, USA
Eur J Pharmacol 590:43-52. 2008Relaxin-3 is a potent agonist for both G-protein coupled receptors (GPCR) RXFP3 (also known as GPCR135) and RXFP4 (also known as GPCR142) while insulin-like peptides 5 (INSL5) is a selective RXFP4 agonist...
Structure of the R3/I5 chimeric relaxin peptide, a selective GPCR135 and GPCR142 agonistLinda M Haugaard-Jönsson
School of Pure and Applied Natural Sciences, University of Kalmar, SE 391 82 Kalmar, Sweden
J Biol Chem 283:23811-8. 2008..relaxin family ancestor, relaxin-3, which is an agonist for three of the four currently known relaxin receptors: GPCR135, GPCR142, and LGR7...
Synthesis, conformation, and activity of human insulin-like peptide 5 (INSL5)Mohammed Akhter Hossain
Howard Florey Institute, University of Melbourne, Victoria 3010, Australia
Chembiochem 9:1816-22. 2008..In contrast, it had no activity on the human RXFP3 receptor...
Relaxin family peptides and receptors in mammalian brainAndrew L Gundlach
Howard Florey Institute, Florey Neuroscience Institutes, University of Melbourne, Victoria, Australia
Ann N Y Acad Sci 1160:226-35. 2009..Here we review progress in mapping RXFP1, RXFP2, and RXFP3 (mRNAs and proteins) and their respective ligands and discuss some of the putative functions for these peptides ..
Metabolic and neuroendocrine responses to RXFP3 modulation in the central nervous systemSteven W Sutton
Johnson and Johnson Pharmaceutical Research and Development, LLC, San Diego, California 92121, USA
Ann N Y Acad Sci 1160:242-9. 2009..the rodent nucleus incertus (NI), project widely into a large number of areas expressing the relaxin-3 receptor (RXFP3), and these data suggest relaxin-3/RXFP3 signaling modulates sensory, emotional, and neuroendocrine processing...
Design, synthesis, and characterization of a single-chain peptide antagonist for the relaxin-3 receptor RXFP3Linda M Haugaard-Kedström
School of Natural Sciences, Linnaeus University, SE 391 82 Kalmar, Sweden
J Am Chem Soc 133:4965-74. 2011..that is the ancestral member of the relaxin peptide family and, together with its G protein-coupled receptor RXFP3, is highly expressed in the brain...
Nucleus incertus--an emerging modulatory role in arousal, stress and memoryPhilip J Ryan
Howard Florey Institute and Florey Neuroscience Institutes, The University of Melbourne, Victoria 3010, Australia
Neurosci Biobehav Rev 35:1326-41. 2011..of structurally-related, chimeric peptides that selectively activate or inhibit the relaxin-3 receptor, RXFP3, is facilitating studies of relaxin-3/RXFP3 networks and associated GABA and CRF systems...
The roles of the A- and B-chains of human relaxin-2 and -3 on their biological activityMohammed Akhter Hossain
Florey Neuroscience Institutes, University of Melbourne, Victoria 3010, Australia
Curr Protein Pept Sci 11:719-24. 2010..The native receptor for H3 relaxin is the unrelated receptor, RXFP3; however, it also has high affinity for another related receptor, RXFP4...
H3 relaxin demonstrates antifibrotic properties via the RXFP1 receptorMohammed Akhter Hossain
Howard Florey Institute, School of Chemistry, and Department of Biochemistry and Molecular Biology, The University of Melbourne, Parkville, Victoria 3010, Australia
Biochemistry 50:1368-75. 2011..While its effects as a neuromodulator are being increasingly studied through its primary receptor, RXFP3, its actions via other RXFPs are poorly understood...
Relaxin-3/insulin-like peptide 7, a neuropeptide involved in the stress response and food intakeMasaki Tanaka
Department of Basic Geriatrics, Kyoto Prefectural University of Medicine, Kamikyo ku, Kyoto, Japan
FEBS J 277:4990-7. 2010..On the other hand, relaxin-3-expressing nerve fibers and the relaxin-3 receptors, RXFP3 and RXFP1, are widely distributed in the forebrain, with the hypothalamus being one of the most densely-innervated ..
Distribution of relaxin-3 and RXFP3 within arousal, stress, affective, and cognitive circuits of mouse brainCraig M Smith
Florey Neuroscience Institutes, The University of Melbourne, Victoria 3010, Australia
J Comp Neurol 518:4016-45. 2010Relaxin-3 (RLN3) and its native receptor, relaxin family peptide 3 receptor (RXFP3), constitute a newly identified neuropeptide system enriched in mammalian brain...
A simple approach for the preparation of mature human relaxin-3Xiao Luo
Institute of Protein Research, Tongji University, 1239 Siping Road, Shanghai 200092, China
Peptides 31:2083-8. 2010..The recombinant mature relaxin-3 was fully active in both RXFP3 binding and activation assays...
Promoter hypermethylation of CIDEA, HAAO and RXFP3 associated with microsatellite instability in endometrial carcinomasYi Wen Huang
Human Cancer Genetics Program, Comprehensive Cancer Center, The Ohio State University, Columbus, OH 43210, USA
Gynecol Oncol 117:239-47. 2010..The purpose of this study is to identify novel hypermethylated loci associated with clinicopathologic variables in endometrioid endometrial carcinomas...
H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3)Emma T Van der Westhuizen
Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Parkville, Victoria, Australia
Mol Pharmacol 77:759-72. 2010Relaxin family peptide 3 receptors (RXFP3) are activated by H3-relaxin to inhibit forskolin-stimulated cAMP accumulation and stimulate extracellular signal-regulated kinase (ERK) 1/2 phosphorylation...
Membrane receptors: structure and function of the relaxin family peptide receptorsRoy C K Kong
Florey Neuroscience Institutes, University of Melbourne, Victoria 3010, Australia
Mol Cell Endocrinol 320:1-15. 2010..and INSL5 interact with another class of type I GPCRs which lack a large ectodomain, the peptide receptors GPCR135 and GPCR142, respectively...
Localization of relaxin-3 in brain of Macaca fascicularis: identification of a nucleus incertus in primateSherie Ma
Florey Neuroscience Institutes, The University of Melbourne, Victoria 3010, Australia
J Comp Neurol 517:856-72. 2009..and pharmacological studies suggest that RLN3 is the cognate ligand for the relaxin family peptide-3 receptor (RXFP3). The distribution of RLN3/RXFP3 networks has been determined in rat and mouse brain, but not in higher species...
Verification of a relaxin-3 knockout/LacZ reporter mouse as a model of relaxin-3 deficiencyCraig M Smith
Howard Florey Institute, University of Melbourne, Victoria, Australia
Ann N Y Acad Sci 1160:259-60. 2009..Anatomical studies have yielded important information on the distribution of relaxin-3 and its cognate receptor (RXFP3) within the brain, while functional studies have implicated relaxin-3 as a modulator of feeding and stress ..
Distribution of relaxin-3 mRNA and immunoreactivity and RXFP3-binding sites in the brain of the macaque, Macaca fascicularisSherie Ma
Howard Florey Institute, University of Melbourne, Victoria, Australia
Ann N Y Acad Sci 1160:256-8. 2009This study examined the presence and distribution of relaxin-3 (RLN3) and its receptor, RXFP3, throughout the brain of Macaca fascicularis...
Relaxin-3 and its role in neuroendocrine functionBarbara M C McGowan
Department of Investigative Medicine, Division of Investigative Science, Imperial College London, Hammersmith Hospital, London, UK
Ann N Y Acad Sci 1160:250-5. 2009..incertus of the brainstem, which has projections to the hypothalamus and is thought to act in the brain via the RXFP3 receptor, although the RXFP1 receptor may also play a role...
Relaxin-3 stimulates the hypothalamic-pituitary-gonadal axisB M McGowan
Dept of Investigative Medicine, Division of Investigative Science, Imperial College London, Hammersmith Campus, Du Cane Road, London, UK
Am J Physiol Endocrinol Metab 295:E278-86. 2008..Relaxin-3 is thought to act in the brain via the RXFP3 receptor, although the RXFP1 receptor may also play a role...
The A-chain of human relaxin family peptides has distinct roles in the binding and activation of the different relaxin family peptide receptorsMohammed Akhter Hossain
Howard Florey Institute and Department of Biochemistry and Molecular Biology, University of Melbourne, Victoria, Australia
J Biol Chem 283:17287-97. 2008..classes of G-protein-coupled receptors (GPCRs), leucine-rich repeat-containing GPCRs LGR7 and LGR8 together with GPCR135 and GPCR142, now referred to as the relaxin family peptide (RXFP) receptors 1-4, respectively...
Insulin-relaxin family peptide signaling and receptors in mouse brain membranes and neuronal cellsStefanie Ortinau
Howard Florey Institute of Experimental Physiology and Medicine, The University of Melbourne, Victoria 3010, Australia
Ann N Y Acad Sci 1041:211-5. 2005Several orphan G-protein-coupled receptors (GPCRs), LGR7 and LGR8, GPCR135 and GPCR142, were recently identified as putative, native receptors for different relaxin-family peptides, and their cell signaling mechanisms were elucidated in ..
Localization of LGR7 (relaxin receptor) mRNA and protein in rat forebrain: correlation with relaxin binding site distributionTanya C D Burazin
Howard Florey Institute of Experimental Physiology and Medicine, The University of Melbourne, Victoria 3010, Australia
Ann N Y Acad Sci 1041:205-10. 2005..relaxin and relaxin-3, and molecular studies have identified former-orphan, G-protein-coupled receptors LGR7 and GPCR135 as their native receptors...
Receptors for relaxin family peptidesRoss A Bathgate
Howard Florey Institute of Experimental Physiology and Medicine, University of Melbourne, Victoria 3010, Australia
Ann N Y Acad Sci 1041:61-76. 2005..receptors with LGR7 (RXFP1) and LGR8 (RXFP2) being type C leucine-rich repeat-containing receptors, whereas GPCR135 (RXFP3) and GPCR142 (RXFP4) resemble receptors that respond to small peptides such as somatostatin and ..
Recent progress in relaxin-3-related researchChanglu Liu
Johnson and Johnson Pharmaceutical Research and Development, LLC, San Diego, CA 92121
Ann N Y Acad Sci 1041:47-60. 2005..We recently identified R3 as a ligand for two orphan G-protein coupled receptors, GPCR135 and GPCR142...
Central relaxin-3 administration causes hyperphagia in male Wistar ratsB M C McGowan
Endocrine Unit, Imperial College School of Medicine, Hammersmith Hospital, London W12 ONN, United Kingdom
Endocrinology 146:3295-300. 2005..Relaxin-3 binds with high affinity to the LGR7 receptor and to the previously orphan G protein-coupled receptor GPCR135. GPCR135 mRNA is expressed predominantly in the central nervous system, particularly in the paraventricular ..
INSL5 is a high affinity specific agonist for GPCR142 (GPR100)Changlu Liu
Johnson and Johnson Pharmaceutical Research and Development, San Diego, California 92121, USA
J Biol Chem 280:292-300. 2005..However, unlike relaxin-3, which is also a potent agonist for GPCR135 and LGR7, INSL5 does not activate either GPCR135 or LGR7...
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 7Changlu Liu
Johnson and Johnson Pharmaceutical Research and Development, L L C, San Diego, CA 92121, USA
Mol Pharmacol 67:231-40. 2005..of relaxin/insulin family, is an agonist for leucine-rich repeat-containing G protein-coupled receptor (LGR)7, GPCR135, and GPCR142...
Pharmacological characterization of relaxin-3/INSL7 receptors GPCR135 and GPCR142 from different mammalian speciesJingcai Chen
Johnson and Johnson Pharmaceutical Research and Development, L L C, 3210 Merryfield Row, San Diego, CA 92121, USA
J Pharmacol Exp Ther 312:83-95. 2005Relaxin-3 has recently been identified as a ligand for two structurally related G-protein-coupled receptors, human GPCR135 and GPCR142...
Identification of a mouse orthologue of the G-protein-coupled receptor SALPR and its expression in adult mouse brain and during developmentKatrin Boels
Zentrum für Molekulare Neurobiologie, Universitat Hamburg, Martinistrasse 52, 20246 Hamburg, Germany
Brain Res Dev Brain Res 152:265-8. 2004The mouse orthologue of somatostatin and angiotensin-like peptide receptor (SALPR) was amplified from cDNA of the hippocampal cell line HT22...
Identification and characterisation of GPR100 as a novel human G-protein-coupled bradykinin receptorKatrin Boels
Zentrum für Molekulare Neurobiologie, Universitat Hamburg, Martinistrasse 52, Hamburg 20246, Germany
Br J Pharmacol 140:932-8. 2003....
Identification of relaxin-3/INSL7 as an endogenous ligand for the orphan G-protein-coupled receptor GPCR135Changlu Liu
Johnson and Johnson Pharmaceutical Research and Development, L L C, San Diego, California 92121, USA
J Biol Chem 278:50754-64. 2003b>GPCR135, publicly known as somatostatin- and angiotensin-like peptide receptor, is expressed in the central nervous system and its cognate ligand(s) has not been identified...
Identification of relaxin-3/INSL7 as a ligand for GPCR142Changlu Liu
Johnson and Johnson Pharmaceutical Research and Development, L L C, San Diego, California 92121, USA
J Biol Chem 278:50765-70. 2003..the insulin-like peptide relaxin-3 (aka INSL7) as the endogenous ligand for an orphan G-protein-coupled receptor, GPCR135 (aka somatostatin- and angiotensin-like peptide receptor)...
Responses of GPCR135 to human gene 3 (H3) relaxin in CHO-K1 cells determined by microphysiometryEmma T Van der Westhuizen
Department of Pharmacology, Monash University, Clayton 3168, Australia
Ann N Y Acad Sci 1041:332-7. 2005..porcine relaxin, and human INSL3 in the cytosensor microphysiometer, using CHO-K1 cells stably expressing human GPCR135. CHO-K1 cells stably expressing GPCR135 were generated by the serial dilution method and receptor properties were ..
Evolution of the signaling system in relaxin-family peptidesSheau Yu Teddy Hsu
Division of Reproductive Biology, Department of Obstetrics and Gynecology, Stanford University School of Medicine, Stanford, CA 94305 5317, USA
Ann N Y Acad Sci 1041:520-9. 2005..In addition, INSL7/relaxin3 signals through two orphan GPCRs, GPCR135 and GPCR142, whereas INSL5 is a select ligand for GPCR142...
Fine mapping of the 5p13 locus linked to schizophrenia and schizotypal personality disorder in a Puerto Rican familyIrina N Bespalova
Department of Psychiatry, Mount Sinai School of Medicine, New York, NY 10029, USA
Psychiatr Genet 15:205-10. 2005..8 Mb. G-protein-coupled receptor gene [somatostatin and angiotensin-like peptide receptor (SALPR)] is one of the candidate genes within the critical interval...
Relaxin-3, INSL5, and their receptorsChanglu Liu
Johnson and Johnson Pharmaceutical Research and Development, LLC, San Diego, California 92121, USA
Results Probl Cell Differ 46:213-37. 2008..We recently identified R3 as a ligand for two orphan G-protein coupled receptors, GPCR135 (aka SALPR) and GPCR142 (aka GPR100), which are class-A GPCRs and typical neuropeptide receptors...
Relaxin-family peptide and receptor systems in brain: insights from recent anatomical and functional studiesSherie Ma
Howard Florey Institute, The University of Melbourne, Victoria 3010, Australia
Adv Exp Med Biol 612:119-37. 2007..the identification of a new relaxin family peptide, known as relaxin 3 and its type I G-protein-coupled receptor--GPCR135. Relaxin 3 was subsequently found to be highly conserved throughout evolution and to be the likely ancestral gene/..
The evolution of the relaxin peptide family and their receptorsTracey N Wilkinson
Howard Florey Institute, University of Melbourne, Victoria 3010, Australia
Adv Exp Med Biol 612:1-13. 2007..repeat containing G protein-coupled receptors (LGR), LGR7 and LGR8 respectively; and the two relaxin-3 receptors, GPCR135 and GPCR142...
R3(BDelta23 27)R/I5 chimeric peptide, a selective antagonist for GPCR135 and GPCR142 over relaxin receptor LGR7: in vitro and in vivo characterizationChester Kuei
Johnson and Johnson Pharmaceutical Research and Development, LLC, San Diego, California 92121, USA
J Biol Chem 282:25425-35. 2007Both relaxin-3 and its receptor (GPCR135) are expressed predominantly in brain regions known to play important roles in processing sensory signals...
The relaxin family peptide receptor 3 activates extracellular signal-regulated kinase 1/2 through a protein kinase C-dependent mechanismEmma T Van der Westhuizen
Department of Pharmacology, PO Box 13E, Monash University, Clayton, Victoria, Australia
Mol Pharmacol 71:1618-29. 2007..The relaxin family peptide receptor 3 (RXFP3, formerly GPCR135 or SALPR) was characterized as the receptor for H3 relaxin, functionally ..
Relaxin family peptide receptors--former orphans reunite with their parent ligands to activate multiple signalling pathwaysM L Halls
Department of Pharmacology, Monash University, Clayton, Victoria, Australia
Br J Pharmacol 150:677-91. 2007..The leucine-rich repeat containing RXFP1 and RXFP2 and the small peptide-like RXFP3 and RXFP4 are the physiological targets for relaxin, insulin-like (INSL) peptide 3, relaxin-3 and INSL5, ..
Hypothalamic mapping of orexigenic action and Fos-like immunoreactivity following relaxin-3 administration in male Wistar ratsB M McGowan
Department of Metabolic Medicine, Imperial College London, 6th Floor Commonwealth Bldg, Hammersmith Hospital, Du Cane Road, London W12 0NN, UK
Am J Physiol Endocrinol Metab 292:E913-9. 2007..family peptide receptor 1, which also binds relaxin-1, and a previously orphaned G protein-coupled receptor, RXFP3. These receptors are extensively expressed in the hypothalamus...
Relaxin-3 in GABA projection neurons of nucleus incertus suggests widespread influence on forebrain circuits via G-protein-coupled receptor-135 in the ratS Ma
Howard Florey Institute, The University of Melbourne, Melbourne, Victoria 3010, Australia
Neuroscience 144:165-90. 2007..studies have demonstrated that RLX3 is a high affinity, selective ligand for G-protein-coupled receptor-135 (GPCR135, now classified as relaxin family peptide-3 receptor; RXFP3)...
G-protein-coupled receptor (GPCR)-142 does not contribute to relaxin-3 binding in the mouse brain: further support that relaxin-3 is the physiological ligand for GPCR135Steven W Sutton
Johnson and Johnson Pharmaceutical Research and Development, LLC, San Diego, CA 92121, USA
Neuroendocrinology 82:139-50. 2005..We have recently described a chimeric R3/I5 peptide that selectively activates GPCR135 and GPCR142, but lacks affinity for LGR7...
Relaxin-a pleiotropic hormone and its emerging role for experimental and clinical therapeuticsThomas Dschietzig
Medizinische Klinik m S Kardiologie und Angiologie, Charite Universitatsmedizin Berlin, Campus Mitte, Schumannstr 20 21, 10117 Berlin, Germany
Pharmacol Ther 112:38-56. 2006..current state of insight into this rapidly evolving field, which has further been expanded by the discovery of GPCR135 and GPCR142 as receptors for Rlx-3...
International Union of Pharmacology LVII: recommendations for the nomenclature of receptors for relaxin family peptidesRoss A Bathgate
Howard Florey Institute, University of Melbourne, Victoria, Australia
Pharmacol Rev 58:7-31. 2006..the receptors for relaxin (LGR7) and those for the related peptides insulin-like peptide 3 (LGR8), relaxin-3 (GPCR135), and insulin-like peptide 5 (LGPCR142) be named the relaxin family peptide receptors 1 through 4 (RXFP1-4)...
Solution structure and novel insights into the determinants of the receptor specificity of human relaxin-3K Johan Rosengren
Institute for Molecular Bioscience, University of Queensland, Brisbane, Queensland 4072, Australia
J Biol Chem 281:5845-51. 2006..This structural feature is likely important for the activation of its endogenous receptor, GPCR135.
The novel G-protein coupled receptor SALPR shares sequence similarity with somatostatin and angiotensin receptorsM Matsumoto
Molecular Medicine Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co, Ltd, 21 Miyukigaoka, Tsukuba, Ibaraki, Japan
Gene 248:183-9. 2000..This putative seven-transmembrane domain receptor of 469 amino acids was designated SALPR (Somatostatin- and Angiotensin- Like Peptide Receptor)...
Research Grants
- PHYSIOLOGY OF RELAXIN-INSULIN-LIKE FACTORSSheau Yu Hsu; Fiscal Year: 2002..Additionally, knowledge gathered from the proposed experiments would help the diagnosis and treatment of diseases associated with the dysfunction of these novel relaxin/insulin-like factors. ..
- Identification of Relaxin Receptor AntagonistsSheau Yu Hsu; Fiscal Year: 2005..These antagonists could be used to block relaxin action during preterm labor as well as provide a tool for further research on the role of LGR7 and LGR8 in reproductive tract physiology. ..
- Role of RAMPs in Intermedin SignalingSheau Yu Hsu; Fiscal Year: 2009....
- Role of RAMPs in Intermedin SignalingSheau Yu Teddy Hsu; Fiscal Year: 2010....
