The relaxin family peptide receptor 1 (RXFP1): An emerging player in human health and disease [PDF]
Molecular Genetics & Genomic Medicine, 2020 Background Relaxin/relaxin family peptide receptor 1 (RXFP1) signaling is important for both normal physiology and disease. Strong preclinical evidence supports relaxin as a potent antifibrotic molecule.
Xiaoyun Li +2 more
exaly +3 more sources
Characterization of a new potent and long-lasting single chain peptide agonist of RXFP1 in cells and in vivo translational models [PDF]
Scientific Reports, 2022 Despite beneficial effects in acute heart failure, the full therapeutic potential of recombinant relaxin-2 has been hampered by its short half-life and the need for intravenous administration limiting its use to intensive care units.
Stephane Illiano +23 more
doaj +4 more sources
Identification of a distal RXFP1 gene enhancer with differential activity in fibrotic lung fibroblasts involving AP-1. [PDF]
PLoS ONE, 2021 Relaxin/insulin-like family peptide receptor 1 (RXFP1) mediates relaxin's antifibrotic effects and has reduced expression in the lung and skin of patients with fibrotic interstitial lung disease (fILD) including idiopathic pulmonary fibrosis (IPF) and ...
Ting-Yun Chen +9 more
doaj +3 more sources
Activation of Relaxin Family Receptor 1 from different mammalian species by relaxin peptide and small molecule agonist ML290 [PDF]
Frontiers in Endocrinology, 2015 Relaxin peptide (RLN), which signals through the relaxin family peptide 1 (RXFP1) GPCR receptor, has shown therapeutic effects in an acute heart failure clinical trial.
Zaohua eHuang +12 more
doaj +8 more sources
Multi-Component Mechanism of H2 Relaxin Binding to RXFP1 through NanoBRET Kinetic Analysis [PDF]
iScience, 2019 Summary: The peptide hormone H2 relaxin has demonstrated promise as a therapeutic, but mimetic development has been hindered by the poorly understood relaxin receptor RXFP1 activation mechanism.
Bradley L. Hoare +8 more
doaj +2 more sources
RXFP1 is targeted by complement C1q Tumor Necrosis Factor-related factor 8 (CTRP8) in brain cancer [PDF]
Frontiers in Endocrinology, 2015 The relaxin-like - RXFP1 ligand-receptor system has important functions in tumor growth and tissue invasion. Recently, we have identified the secreted protein, CTRP8, a member of the C1q/ Tumor Necrosis Factor-related protein (CTRP) family, as a novel ...
Thatchawan eThanasupawat +6 more
doaj +2 more sources
Targeted overexpression of relaxin receptor 1 (RXFP1) with chronic administration of relaxin as a novel inotropic approach for heart failure treatment [PDF]
, 2020 Despite advances in modern medicine, heart failure (HF) is one of the leading causes of death in developed countries. HF is a progressive condition that gradually affects the heart. It is a common end point for all heart diseases.
Sasipong, Nuttarak
core +2 more sources
ML290 is a biased allosteric agonist at the relaxin receptor RXFP1 [PDF]
Scientific Reports, 2017 Activation of the relaxin receptor RXFP1 has been associated with improved survival in acute heart failure. ML290 is a small molecule RXFP1 agonist with simple structure, long half-life and high stability.
Martina Kocan +11 more
doaj +2 more sources
Synthetic short-chain peptide analogues of H1 relaxin lack affinity for the RXFP1 receptor and relaxin-like bioactivity. Clues to a better understanding of relaxin agonist design [PDF]
Frontiers in Pharmacology, 2022 The peptide hormone relaxin (RLX), also available as clinical-grade recombinant protein (serelaxin), holds great promise as a cardiovascular and anti-fibrotic agent but is limited by the pharmacokinetic issues common to all peptide drugs.
Annunziata D'Ercole +12 more
doaj +3 more sources
Antioxidants, 2023 Due to the high incidence of diabetes mellitus (DM) and poor response to the first-line treatment of DM-induced erectile dysfunction (DMED), new therapeutic strategies for DMED are needed.
Taotao Sun, Wenchao Xu, Kang Liu
exaly +3 more sources