RXFP3

Summary

Gene 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

  1. ncbi 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 processing
    Steven W Sutton
    Neuroscience Group, Johnson and Johnson Pharmaceutical Research and Development, LLC, 3210 Merryfield Row, San Diego, CA 92121, USA
    Neuroendocrinology 80:298-307. 2004
  2. ncbi Relaxin-3: improved synthesis strategy and demonstration of its high-affinity interaction with the relaxin receptor LGR7 both in vitro and in vivo
    Ross A D Bathgate
    Howard Florey Institute, University of Melbourne, Melbourne, Victoria 3010, Australia
    Biochemistry 45:1043-53. 2006
  3. ncbi Roles of the receptor, the ligand, and the cell in the signal transduction pathways utilized by the relaxin family peptide receptors 1-3
    Roger J Summers
    Department of Pharmacology, Monash Institute of Pharmaceutical Sciences, Monash University, Clayton, Victoria, Australia
    Ann N Y Acad Sci 1160:99-104. 2009
  4. ncbi Relaxin receptors--new drug targets for multiple disease states
    E T van der Westhuizen
    Department of Pharmacology, Monash University, Wellington Road, Clayton, Victoria 3800, Australia
    Curr Drug Targets 8:91-104. 2007
  5. ncbi Relaxin-3 systems in the brain--the first 10 years
    Craig M Smith
    Florey Neuroscience Institutes, The University of Melbourne, Victoria, Australia
    J Chem Neuroanat 42:262-75. 2011
  6. ncbi Addition of a carboxy-terminal green fluorescent protein does not alter the binding and signaling properties of relaxin family Peptide receptor 3
    Emma 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. 2009
  7. ncbi Probing the functional domains of relaxin-3 and the creation of a selective antagonist for RXFP3/GPCR135 over relaxin receptor RXFP1/LGR7
    Changlu Liu
    Johnson and Johnson Pharmaceutical Research and Development, LLC, San Diego, California 92121, USA
    Ann N Y Acad Sci 1160:31-7. 2009
  8. ncbi Structural properties of relaxin chimeras
    Linda M Haugaard-Jönsson
    School of Pure and Applied Natural Sciences, University of Kalmar, Kalmar, Sweden
    Ann N Y Acad Sci 1160:27-30. 2009
  9. ncbi De novo design and synthesis of cyclic and linear peptides to mimic the binding cassette of human relaxin
    Mohammed Akhter Hossain
    Howard Florey Institute, University of Melbourne, Parkville, Victoria, Australia
    Ann N Y Acad Sci 1160:16-9. 2009
  10. ncbi Structure and activity in the relaxin family of peptides
    Geoffrey 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

Research Grants

  1. PHYSIOLOGY OF RELAXIN-INSULIN-LIKE FACTORS
    Sheau Yu Hsu; Fiscal Year: 2002
  2. Identification of Relaxin Receptor Antagonists
    Sheau Yu Hsu; Fiscal Year: 2005
  3. Role of RAMPs in Intermedin Signaling
    Sheau Yu Hsu; Fiscal Year: 2009
  4. Role of RAMPs in Intermedin Signaling
    Sheau Yu Teddy Hsu; Fiscal Year: 2010

Scientific Experts

  • B C Wilson
  • Changlu Liu
  • Steven W Sutton
  • Andrew L Gundlach
  • S Ma
  • K Johan Rosengren
  • Thomas Dschietzig
  • Masaki Tanaka
  • Irina N Bespalova
  • Mitsuyuki Matsumoto
  • R J Summers
  • John D Wade
  • SHEAU-YU T HSU
  • Mohammed Akhter Hossain
  • Ross A D Bathgate
  • Emma T Van der Westhuizen
  • Geoffrey W Tregear
  • Craig M Smith
  • Linda M Haugaard-Jönsson
  • Philip J Ryan
  • Fazel Shabanpoor
  • Suode Zhang
  • Chrishan S Samuel
  • Patrick M Sexton
  • Pascal Bonaventure
  • B M McGowan
  • Feng Lin
  • Chester Kuei
  • Ross A Bathgate
  • David J Craik
  • Norelle L Daly
  • Katrin Boels
  • Jessica Zhu
  • M L Halls
  • E T van der Westhuizen
  • S A Stanley
  • J V Gardiner
  • S R Bloom
  • Timothy W Lovenberg
  • M A Ghatei
  • E L Thompson
  • Jingcai Chen
  • Linda M Haugaard-Kedström
  • Roy C K Kong
  • Xiao Luo
  • Yi Wen Huang
  • Pei Juan Shen
  • Sharon Layfield
  • Barbara M C McGowan
  • Chongxin Zhao
  • M Patterson
  • John Atack
  • Fredrik Kamme
  • J Donovan
  • Tracey N Wilkinson
  • R A D Bathgate
  • Tania Ferraro
  • K G Murphy
  • Diane Nepomuceno
  • N E White
  • K L Smith
  • O David Sherwood
  • Richard Ivell
  • Barbara M Sanborn
  • Stefanie Ortinau
  • Tanya C D Burazin
  • B M C McGowan
  • H Chica Schaller
  • Francisco E Olucha-Bordonau
  • Richard J Clark
  • Qi Xu
  • Ihaia T Hosken
  • Xiao Jun Du
  • Bryna Chow Suet Man
  • Tim H M Huang
  • Paul R Gooley
  • Xiao Xia Shao
  • David S Miller
  • David G Mutch
  • Jingqin Luo
  • Derek K Lobb
  • Avantika Banerjee
  • Paul J Goodfellow
  • Yu I Weng
  • Ya Li Liu
  • Arthur Christopoulos
  • Patrick J Shilling
  • Zhan Yun Guo
  • Geoffery Tregear
  • Andrea J Robinson

Detail Information

Publications63

  1. ncbi 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 processing
    Steven W Sutton
    Neuroscience Group, Johnson and Johnson Pharmaceutical Research and Development, LLC, 3210 Merryfield Row, San Diego, CA 92121, USA
    Neuroendocrinology 80:298-307. 2004
    G-protein-coupled receptor 135 (GPCR135), a former orphan GPCR also known as SALPR, has recently been shown to be modulated by relaxin-3 (R3)...
  2. ncbi Relaxin-3: improved synthesis strategy and demonstration of its high-affinity interaction with the relaxin receptor LGR7 both in vitro and in vivo
    Ross 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 ..
  3. ncbi Roles of the receptor, the ligand, and the cell in the signal transduction pathways utilized by the relaxin family peptide receptors 1-3
    Roger 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...
  4. ncbi Relaxin receptors--new drug targets for multiple disease states
    E 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 ..
  5. ncbi Relaxin-3 systems in the brain--the first 10 years
    Craig 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 ..
  6. ncbi Addition of a carboxy-terminal green fluorescent protein does not alter the binding and signaling properties of relaxin family Peptide receptor 3
    Emma 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. 2009
    The relaxin family peptide receptor 3 (RXFP3) is the cognate receptor for the neuropeptide relaxin-3...
  7. ncbi Probing the functional domains of relaxin-3 and the creation of a selective antagonist for RXFP3/GPCR135 over relaxin receptor RXFP1/LGR7
    Changlu Liu
    Johnson and Johnson Pharmaceutical Research and Development, LLC, San Diego, California 92121, USA
    Ann N Y Acad Sci 1160:31-7. 2009
    Both 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...
  8. ncbi Structural properties of relaxin chimeras
    Linda M Haugaard-Jönsson
    School of Pure and Applied Natural Sciences, University of Kalmar, Kalmar, Sweden
    Ann N Y Acad Sci 1160:27-30. 2009
    Relaxin-3 interacts with high potency with three relaxin family peptide receptors (RXFP1, RXFP3, and RXFP4)...
  9. ncbi De novo design and synthesis of cyclic and linear peptides to mimic the binding cassette of human relaxin
    Mohammed 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 ..
  10. ncbi Structure and activity in the relaxin family of peptides
    Geoffrey 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 ..
  11. ncbi Solid phase synthesis and structural analysis of novel A-chain dicarba analogs of human relaxin-3 (INSL7) that exhibit full biological activity
    Mohammed 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...
  12. ncbi The structural and functional role of the B-chain C-terminal arginine in the relaxin-3 peptide antagonist, R3(BDelta23-27)R/I5
    Mohammed 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 ..
  13. ncbi Relaxin-3 and RXFP3 expression, and steroidogenic actions in the ovary of teleost fish
    Brian 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...
  14. ncbi Relaxin family peptide receptors--from orphans to therapeutic targets
    Emma 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)...
  15. ncbi 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. 2008
    Relaxin-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...
  16. ncbi Structure of the R3/I5 chimeric relaxin peptide, a selective GPCR135 and GPCR142 agonist
    Linda 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...
  17. ncbi 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...
  18. ncbi Relaxin family peptides and receptors in mammalian brain
    Andrew 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 ..
  19. ncbi Metabolic and neuroendocrine responses to RXFP3 modulation in the central nervous system
    Steven 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...
  20. ncbi Design, synthesis, and characterization of a single-chain peptide antagonist for the relaxin-3 receptor RXFP3
    Linda 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...
  21. ncbi Nucleus incertus--an emerging modulatory role in arousal, stress and memory
    Philip 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...
  22. ncbi The roles of the A- and B-chains of human relaxin-2 and -3 on their biological activity
    Mohammed 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...
  23. ncbi H3 relaxin demonstrates antifibrotic properties via the RXFP1 receptor
    Mohammed 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...
  24. ncbi Relaxin-3/insulin-like peptide 7, a neuropeptide involved in the stress response and food intake
    Masaki 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 ..
  25. ncbi Distribution of relaxin-3 and RXFP3 within arousal, stress, affective, and cognitive circuits of mouse brain
    Craig M Smith
    Florey Neuroscience Institutes, The University of Melbourne, Victoria 3010, Australia
    J Comp Neurol 518:4016-45. 2010
    Relaxin-3 (RLN3) and its native receptor, relaxin family peptide 3 receptor (RXFP3), constitute a newly identified neuropeptide system enriched in mammalian brain...
  26. ncbi A simple approach for the preparation of mature human relaxin-3
    Xiao 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...
  27. ncbi Promoter hypermethylation of CIDEA, HAAO and RXFP3 associated with microsatellite instability in endometrial carcinomas
    Yi 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...
  28. ncbi 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. 2010
    Relaxin 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...
  29. ncbi Membrane receptors: structure and function of the relaxin family peptide receptors
    Roy 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...
  30. ncbi Localization of relaxin-3 in brain of Macaca fascicularis: identification of a nucleus incertus in primate
    Sherie 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...
  31. ncbi Verification of a relaxin-3 knockout/LacZ reporter mouse as a model of relaxin-3 deficiency
    Craig 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 ..
  32. ncbi Distribution of relaxin-3 mRNA and immunoreactivity and RXFP3-binding sites in the brain of the macaque, Macaca fascicularis
    Sherie Ma
    Howard Florey Institute, University of Melbourne, Victoria, Australia
    Ann N Y Acad Sci 1160:256-8. 2009
    This study examined the presence and distribution of relaxin-3 (RLN3) and its receptor, RXFP3, throughout the brain of Macaca fascicularis...
  33. ncbi Relaxin-3 and its role in neuroendocrine function
    Barbara 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...
  34. ncbi Relaxin-3 stimulates the hypothalamic-pituitary-gonadal axis
    B 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...
  35. ncbi The A-chain of human relaxin family peptides has distinct roles in the binding and activation of the different relaxin family peptide receptors
    Mohammed 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...
  36. ncbi Insulin-relaxin family peptide signaling and receptors in mouse brain membranes and neuronal cells
    Stefanie Ortinau
    Howard Florey Institute of Experimental Physiology and Medicine, The University of Melbourne, Victoria 3010, Australia
    Ann N Y Acad Sci 1041:211-5. 2005
    Several 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 ..
  37. ncbi Localization of LGR7 (relaxin receptor) mRNA and protein in rat forebrain: correlation with relaxin binding site distribution
    Tanya 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...
  38. ncbi Receptors for relaxin family peptides
    Ross 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 ..
  39. ncbi Recent progress in relaxin-3-related research
    Changlu 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...
  40. ncbi Central relaxin-3 administration causes hyperphagia in male Wistar rats
    B 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 ..
  41. ncbi 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...
  42. ncbi 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
    Changlu 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...
  43. ncbi Pharmacological characterization of relaxin-3/INSL7 receptors GPCR135 and GPCR142 from different mammalian species
    Jingcai 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. 2005
    Relaxin-3 has recently been identified as a ligand for two structurally related G-protein-coupled receptors, human GPCR135 and GPCR142...
  44. ncbi Identification of a mouse orthologue of the G-protein-coupled receptor SALPR and its expression in adult mouse brain and during development
    Katrin Boels
    Zentrum für Molekulare Neurobiologie, Universitat Hamburg, Martinistrasse 52, 20246 Hamburg, Germany
    Brain Res Dev Brain Res 152:265-8. 2004
    The mouse orthologue of somatostatin and angiotensin-like peptide receptor (SALPR) was amplified from cDNA of the hippocampal cell line HT22...
  45. ncbi Identification and characterisation of GPR100 as a novel human G-protein-coupled bradykinin receptor
    Katrin Boels
    Zentrum für Molekulare Neurobiologie, Universitat Hamburg, Martinistrasse 52, Hamburg 20246, Germany
    Br J Pharmacol 140:932-8. 2003
    ....
  46. ncbi Identification of relaxin-3/INSL7 as an endogenous ligand for the orphan G-protein-coupled receptor GPCR135
    Changlu Liu
    Johnson and Johnson Pharmaceutical Research and Development, L L C, San Diego, California 92121, USA
    J Biol Chem 278:50754-64. 2003
    b>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...
  47. ncbi Identification of relaxin-3/INSL7 as a ligand for GPCR142
    Changlu 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)...
  48. ncbi Responses of GPCR135 to human gene 3 (H3) relaxin in CHO-K1 cells determined by microphysiometry
    Emma 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 ..
  49. ncbi Evolution of the signaling system in relaxin-family peptides
    Sheau 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...
  50. ncbi Fine mapping of the 5p13 locus linked to schizophrenia and schizotypal personality disorder in a Puerto Rican family
    Irina 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...
  51. ncbi Relaxin-3, INSL5, and their receptors
    Changlu 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...
  52. ncbi Relaxin-family peptide and receptor systems in brain: insights from recent anatomical and functional studies
    Sherie 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/..
  53. ncbi The evolution of the relaxin peptide family and their receptors
    Tracey 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...
  54. ncbi R3(BDelta23 27)R/I5 chimeric peptide, a selective antagonist for GPCR135 and GPCR142 over relaxin receptor LGR7: in vitro and in vivo characterization
    Chester Kuei
    Johnson and Johnson Pharmaceutical Research and Development, LLC, San Diego, California 92121, USA
    J Biol Chem 282:25425-35. 2007
    Both relaxin-3 and its receptor (GPCR135) are expressed predominantly in brain regions known to play important roles in processing sensory signals...
  55. ncbi The relaxin family peptide receptor 3 activates extracellular signal-regulated kinase 1/2 through a protein kinase C-dependent mechanism
    Emma 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 ..
  56. ncbi Relaxin family peptide receptors--former orphans reunite with their parent ligands to activate multiple signalling pathways
    M 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, ..
  57. ncbi Hypothalamic mapping of orexigenic action and Fos-like immunoreactivity following relaxin-3 administration in male Wistar rats
    B 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...
  58. ncbi Relaxin-3 in GABA projection neurons of nucleus incertus suggests widespread influence on forebrain circuits via G-protein-coupled receptor-135 in the rat
    S 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)...
  59. ncbi 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 GPCR135
    Steven 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...
  60. ncbi Relaxin-a pleiotropic hormone and its emerging role for experimental and clinical therapeutics
    Thomas 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...
  61. ncbi International Union of Pharmacology LVII: recommendations for the nomenclature of receptors for relaxin family peptides
    Ross 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)...
  62. ncbi Solution structure and novel insights into the determinants of the receptor specificity of human relaxin-3
    K 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.
  63. ncbi The novel G-protein coupled receptor SALPR shares sequence similarity with somatostatin and angiotensin receptors
    M 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 Grants9

  1. PHYSIOLOGY OF RELAXIN-INSULIN-LIKE FACTORS
    Sheau 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. ..
  2. Identification of Relaxin Receptor Antagonists
    Sheau 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. ..
  3. Role of RAMPs in Intermedin Signaling
    Sheau Yu Hsu; Fiscal Year: 2009
    ....
  4. Role of RAMPs in Intermedin Signaling
    Sheau Yu Teddy Hsu; Fiscal Year: 2010
    ....