| Characterization of a new potent and long-lasting single chain peptide agonist of RXFP1 in cells and in vivo translational models. | Characterization of a new potent and long-lasting single chain peptide agonist of RXFP1 in cells and in vivo translational models.
Illiano S, Poirier B, Minoletti C, Pasquier O, Riva L, Chenede X, Menguy I, Guillotel M, Prigent P, Le Claire S, Gillot F, Thill G, Lo Presti F, Corbier A, Le Bail JC, Grailhe P, Monteagudo E, Ingenito R, Bianchi E, Philippo C, Duclos O, Mallart S, Bathgate R, Janiak P., Free PMC Article | 12/10/2022 |
| Identification of a distal RXFP1 gene enhancer with differential activity in fibrotic lung fibroblasts involving AP-1. | Identification of a distal RXFP1 gene enhancer with differential activity in fibrotic lung fibroblasts involving AP-1.
Chen TY, Li X, Goobie GC, Hung CH, Hung TK, Hamilton K, Bahudhanapati H, Tan J, Kass DJ, Zhang Y., Free PMC Article | 01/15/2022 |
| Structural Insights into the Unique Modes of Relaxin-Binding and Tethered-Agonist Mediated Activation of RXFP1 and RXFP2. | Structural Insights into the Unique Modes of Relaxin-Binding and Tethered-Agonist Mediated Activation of RXFP1 and RXFP2.
Sethi A, Bruell S, Ryan T, Yan F, Tanipour MH, Mok YF, Draper-Joyce C, Khandokar Y, Metcalfe RD, Griffin MDW, Scott DJ, Hossain MA, Petrie EJ, Bathgate RAD, Gooley PR. | 11/27/2021 |
| The anti-fibrotic actions of relaxin are mediated through AT2 R-associated protein phosphatases via RXFP1-AT2 R functional crosstalk in human cardiac myofibroblasts. | The anti-fibrotic actions of relaxin are mediated through AT(2) R-associated protein phosphatases via RXFP1-AT(2) R functional crosstalk in human cardiac myofibroblasts.
Wang C, Pinar AA, Widdop RE, Hossain MA, Bathgate RAD, Denton KM, Kemp-Harper BK, Samuel CS. | 01/16/2021 |
| In mice expressing human RXFP1 gene treated with carbon tetrachloride, ML290 significantly reduced collagen content, alpha-smooth muscle actin expression, and cell proliferation around portal ducts. | Therapeutic effects of a small molecule agonist of the relaxin receptor ML290 in liver fibrosis.
Kaftanovskaya EM, Ng HH, Soula M, Rivas B, Myhr C, Ho BA, Cervantes BA, Shupe TD, Devarasetty M, Hu X, Xu X, Patnaik S, Wilson KJ, Barnaeva E, Ferrer M, Southall NT, Marugan JJ, Bishop CE, Agoulnik IU, Agoulnik AI., Free PMC Article | 05/30/2020 |
| Idiopathic pulmonary fibrosis lung fibroblasts transfected with anti-miR-144-3p had increased RXFP1 expression and reduced alpha-smooth muscle actin expression. | MicroRNA-144-3p targets relaxin/insulin-like family peptide receptor 1 (RXFP1) expression in lung fibroblasts from patients with idiopathic pulmonary fibrosis.
Bahudhanapati H, Tan J, Dutta JA, Strock SB, Sembrat J, Àlvarez D, Rojas M, Jäger B, Prasse A, Zhang Y, Kass DJ., Free PMC Article | 10/19/2019 |
| Binding of relaxin to RXFP1 recruits G proteins with subsequent activation of adenylyl cyclase and elevation of cAMP. | Expression of RXFP1 Is Decreased in Idiopathic Pulmonary Fibrosis. Implications for Relaxin-based Therapies.
Tan J, Tedrow JR, Dutta JA, Juan-Guardela B, Nouraie M, Chu Y, Trejo Bittar H, Ramani K, Biswas PS, Veraldi KL, Kaminski N, Zhang Y, Kass DJ., Free PMC Article | 07/22/2017 |
| 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. | Endometrial LGR7 expression and implantation failure.
Campitiello MR, Caprio F, Mele D, D'eufemia D, Colacurci N, De Franciscis P. | 04/15/2017 |
| Hormone receptor expression was concentrated in the fibroblasts, and RXFP1 was also evident in blood vessels and nerves | Hormone receptor expression in human fascial tissue.
Fede C, Albertin G, Petrelli L, Sfriso MM, Biz C, De Caro R, Stecco C., Free PMC Article | 02/18/2017 |
| The complex binding mode of the peptide hormone H2 relaxin to its receptor RXFP1 has been deciphered. | The complex binding mode of the peptide hormone H2 relaxin to its receptor RXFP1.
Sethi A, Bruell S, Patil N, Hossain MA, Scott DJ, Petrie EJ, Bathgate RAD, Gooley PR., Free PMC Article | 09/10/2016 |
| RXFP1 gene expression was dysregulated in the anterior cingulate of bipolar patients. | Transcriptome sequencing of the anterior cingulate in bipolar disorder: dysregulation of G protein-coupled receptors.
Cruceanu C, Tan PP, Rogic S, Lopez JP, Torres-Platas SG, Gigek CO, Alda M, Rouleau GA, Pavlidis P, Turecki G. | 03/12/2016 |
| H2 relaxin amide is fully active at the relaxin receptor RXFP1 and thus dimerization is not required for biological activity. | Solution structure, aggregation behavior, and flexibility of human relaxin-2.
Haugaard-Kedström LM, Hossain MA, Daly NL, Bathgate RA, Rinderknecht E, Wade JD, Craik DJ, Rosengren KJ. | 12/12/2015 |
| Synthetic covalently linked dimeric form of H2 relaxin retains native RXFP1 activity and has improved in vitro serum stability. | Synthetic covalently linked dimeric form of H2 relaxin retains native RXFP1 activity and has improved in vitro serum stability.
Nair VB, Bathgate RA, Separovic F, Samuel CS, Hossain MA, Wade JD., Free PMC Article | 11/7/2015 |
| 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). | Relaxin activates peroxisome proliferator-activated receptor γ (PPARγ) through a pathway involving PPARγ coactivator 1α (PGC1α).
Singh S, Simpson RL, Bennett RG., Free PMC Article | 04/25/2015 |
| 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. | Detection of relaxin receptor in the dorsoradial ligament, synovium, and articular cartilage of the trapeziometacarpal joint.
Clifton KB, Rodner C, Wolf JM. | 09/6/2014 |
| We have developed and assessed four microRNA against human RXFP1. | Development of human cells with RXFP1 knockdown using retroviral delivery of microRNA against human RXFP1.
Yong KL, Callander GE, Bergin R, Samuel CS, Bathgate RA. | 05/3/2014 |
| 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. | Recombinant RXFP1-LDL-A module does not form dimers.
Petrie EJ, Periguini MA, Bathgate RA, Gooley PR. | 05/3/2014 |
| To create a tool to investigate the low-affinity interaction, a protein scaffold system displaying exoloops 1 and 2 from RXFP1 was designed. | Development of a scaffold displaying exoloops of RXFP1.
Diepenhorst NA, Gooley PR, Stone MJ, Bathgate RA. | 05/3/2014 |
| The development of a quantitative high-throughput platform for an RXFP1 agonist screen. | Identification of small-molecule agonists of human relaxin family receptor 1 (RXFP1) by using a homogenous cell-based cAMP assay.
Chen CZ, Southall N, Xiao J, Marugan JJ, Ferrer M, Hu X, Jones RE, Feng S, Agoulnik IU, Zheng W, Agoulnik AI., Free PMC Article | 02/22/2014 |
| Report increased expression of RXFP1 in placenta of patients with placenta accreta. | Relaxin, its receptor (RXFP1), and insulin-like peptide 4 expression through gestation and in placenta accreta.
Goh W, Yamamoto SY, Thompson KS, Bryant-Greenwood GD., Free PMC Article | 01/11/2014 |
| the RXFP1 receptor lacking the LDLa module binds ligand normally but cannot signal through any characterized G protein-coupled receptor signaling pathway | The relaxin receptor (RXFP1) utilizes hydrophobic moieties on a signaling surface of its N-terminal low density lipoprotein class A module to mediate receptor activation.
Kong RC, Petrie EJ, Mohanty B, Ling J, Lee JC, Gooley PR, Bathgate RA., Free PMC Article | 12/28/2013 |
| These results provide new mechanistic insights into the binding and activation events of RXFP1 and RXFP2 by their native hormone ligands. | The different ligand-binding modes of relaxin family peptide receptors RXFP1 and RXFP2.
Scott DJ, Rosengren KJ, Bathgate RA., Free PMC Article | 04/20/2013 |
| Identification of key residues essential for the structural fold and receptor selectivity within the A-chain of human gene-2 (H2) relaxin | Identification of key residues essential for the structural fold and receptor selectivity within the A-chain of human gene-2 (H2) relaxin.
Chan LJ, Rosengren KJ, Layfield SL, Bathgate RA, Separovic F, Samuel CS, Hossain MA, Wade JD., Free PMC Article | 02/9/2013 |
| 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. | Expression of RXFP1 in skin of scleroderma patients and control subjects.
Giordano N, Volpi N, Franci D, Corallo C, Fioravanti A, Papakostas P, Montella A, Biagioli M, Fimiani M, Grasso G, Muscettola MM, Guerranti R, Vannoni D, Galeazzi M, Nuti R. | 01/12/2013 |
| relaxin-2 and its receptors RXFP1 and RXFP2 are expressed in GSV and their expression is significantly decreased in varicose GSV | A novel role for relaxin-2 in the pathogenesis of primary varicosis.
Adams J, Schott S, Bern A, Renz M, Ikenberg K, Garbe C, Busch C., Free PMC Article | 12/22/2012 |