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1 ion and reduced contractility in response to relaxin.
2 distal actions of low circulating levels of relaxin.
3 pression of LGR7, the cognate receptor of H2 relaxin.
4 at perfectly matches the binding cassette of relaxin.
5 nancy and its use in defining the actions of relaxin.
6 GPCR135 and GPCR142 by its high affinity for relaxin.
7 ndent activation of PPARgamma in response to relaxin.
8 d diffusive transport induced by the hormone relaxin.
9 NA diminished the regulation of PPARgamma by relaxin.
10 glucose production are corrected by chronic relaxin.
11 ion of ML290 increased p-ERK1/2 responses to relaxin.
12 bit collagen deposition similar to native H2 relaxin.
15 chimeric peptides indicates the A-chain from relaxin-1, relaxin-2, insulin-like peptide (INSL)3, and
16 -h intravenous infusion of placebo (n=62) or relaxin 10 microg/kg (n=40), 30 microg/kg (n=43), 100 mi
17 ere assessed in the placebo group, 40 in the relaxin 10 microg/kg per day group, 42 in the relaxin 30
18 (dcSSc) were administered recombinant human relaxin (10 microg/kg/day or 25 microg/kg/day) or placeb
19 elaxin 30 microg/kg per day group, 37 in the relaxin 100 microg/kg per day group, and 49 in the relax
20 ive rats (SHRs), and SHRs treated with human relaxin 2 for 14 d (4 mug/h; n=8/group) and studied usin
21 or renal failure at day 60 was reduced with relaxin (2.6% [95% CI 0.4-16.8] vs 17.2% [9.6-29.6]; p=0
26 ptides indicates the A-chain from relaxin-1, relaxin-2, insulin-like peptide (INSL)3, and INSL6 does
27 m of the naturally occurring peptide hormone relaxin-2, is a pleiotropic vasodilating hormone that ha
29 dy, serelaxin, the recombinant form of human relaxin-2, reduced post-discharge mortality at 180 days
33 recently identified the insulin-like peptide relaxin-3 (aka INSL7) as the endogenous ligand for an or
35 tudy undertook to develop analogues of human relaxin-3 (H3 relaxin) that can selectively bind and act
36 one (GnRH), a G-protein-coupled receptor for relaxin-3 (RXFP3) and a functional cyclic nucleotide-gat
42 gonist, R3(BDelta23-27)R/I5, consists of the relaxin-3 B-chain with a replacement of Gly23 to Arg, a
45 was activated by nanomolar concentrations of relaxin-3 but was completely unresponsive to all other k
50 s, we have characterized the distribution of relaxin-3 fibers/terminals in relation to different sept
52 eptides that consist of the B-chain of human relaxin-3 in combination with various A-chains from othe
59 relaxin-3, and pharmacological modulation of relaxin-3 receptors in medial septum alters hippocampal
61 ojected to hippocampus, and contacts between relaxin-3 terminals and calbindin- and calretinin-positi
62 Human INSL5 displaces the binding of (125)I-relaxin-3 to GPCR142 with a high affinity (K(i) = 1.5 nM
63 f a very hydrophobic peptide (the A-chain of relaxin-3) with a very hydrophilic peptide (the A-chain
64 neurons express the relaxin-family peptide, relaxin-3, and pharmacological modulation of relaxin-3 r
65 euroanatomical colocalization of GPCR135 and relaxin-3, coupled with a clear high affinity interactio
66 eptor for the highly conserved neuropeptide, relaxin-3, decreased self-administration of alcohol in a
68 companying article, we present the case that relaxin-3, which has previously been shown to bind to th
75 The mechanisms underlying the involvement of relaxin-3/GPCR135 in the regulation of stress, feeding,
77 A-chain from INSL5), the radiolabeled (125)I-relaxin-3/INSL5 chimera is a suitable ligand (high-affin
82 elaxin 10 microg/kg per day group, 42 in the relaxin 30 microg/kg per day group, 37 in the relaxin 10
98 osophila insulin-like peptide 8 (Dilp8) as a relaxin and insulin-like molecule secreted from growing
100 er there is local expression and function of relaxin and relaxin receptor in arteries of nonpregnant
101 in that the secondary interaction between H2 relaxin and RXFP1 is not driven by any single amino acid
102 vercome the many challenges of investigating relaxin and the LDLa module interactions with the ELs, w
103 interaction that involves the A-chain of H2 relaxin and transmembrane exoloops of the receptors.
104 suggest that urotensin II, apelin, ghrelin, relaxin and urocortins, together with the trace amine ty
108 90 did not directly compete with orthosteric relaxin binding and did not affect binding kinetics, but
109 model explains the exquisite sensitivity of relaxin binding avidity to minute changes in the disposi
112 utated in RXFP1, and changes in function and relaxin binding were assessed alongside the RXFP1 agonis
113 rich G-protein-coupled receptor 7 supports a relaxin-binding group of amino acids that perfectly matc
115 operties to support further investigation of relaxin biology and animal efficacy studies of the thera
116 d no effect on increased distensibility with relaxin, but caused outward hypertrophic remodeling of P
117 a reporter gene assay to demonstrate that H2 relaxin can induce the expression of prostate-specific a
118 e have previously demonstrated that human H2-relaxin can mediate androgen-independent growth of LNCaP
120 Growing evidence indicates that circulating relaxin causes vasodilatation and increases in arterial
123 f the secondary structure to the extent that relaxin cross-reacts with the LGR8, the RLF receptor.
127 rthermore, nonreplicating viruses expressing relaxin did not increase metastases, suggesting that hig
128 Taken together, these results indicate that relaxin effects BMDEC function through the RXFP1 recepto
132 ccupied by STAT3 on day 6 of pregnancy, when relaxin expression is minimal; on day 15, when expressio
136 acterization of contemporary and resurrected relaxin family hormones, we show that derivation of INSL
137 that the A-chains among some of the insulin/relaxin family members are pharmacologically exchangeabl
139 al administration of peptide antagonists for relaxin family peptide 3 receptor (RXFP3), the cognate r
140 tment for acute heart failure, activates the relaxin family peptide receptor (RXFP1), which is a clas
141 tions through the G protein-coupled receptor relaxin family peptide receptor 1 (RXFP1), little is kno
142 nalosome, that couples the relaxin receptor, relaxin family peptide receptor 1 (RXFP1), to cAMP follo
143 and vasoprotective properties that binds to relaxin family peptide receptor-1 (RXFP1) and has been s
145 , a member of the highly conserved family of relaxin family peptide receptors (RXFPs), mediates the c
146 ies demonstrated that two of the seven human relaxin family peptides, relaxin H2 (RLN2) and INSL3, si
148 t drivers of the affinity and activity of H2 relaxin for RXFP2 with additional minor contributions fr
149 t for 13 weeks and continuously treated with relaxin for the final 3 weeks of the diet exhibited decr
151 In the RELAX-AHF (Efficacy and Safety of Relaxin for the Treatment of Acute Heart Failure) study,
153 g that oncolytic adenoviruses expressing the relaxin gene and containing an Ad5/Ad35 chimeric fiber s
154 g/day and 25 microg/kg/day recombinant human relaxin, given for 24 weeks in patients with stable, dif
156 of the seven human relaxin family peptides, relaxin H2 (RLN2) and INSL3, signal exclusively through
159 is directly (bosentan, interferon gamma, and relaxin) have been disappointing but new strategies agai
161 on in various mammalian species, the role of relaxin in human reproduction is poorly understood, larg
162 er, the molecular and cellular mechanisms of relaxin in regulating both myogenic cell differentiation
163 documented importance of the protein hormone relaxin in reproduction in various mammalian species, th
164 ese results revealed the multiple effects of relaxin in systematically improving muscle healing as we
165 ty are consistent with a significant role of relaxin in the establishment and/or maintenance of early
168 We show that the matrix-modifying hormone relaxin increased tumor-associated fibroblast (TAF) inte
169 re not detected in cerebral vasculature, but relaxin increased vascular endothelial growth factor (VE
176 e 5 (INSL5) is a peptide that belongs to the relaxin/insulin family, and its receptor has not been id
177 in-3, the most recently identified member of relaxin/insulin family, is an agonist for leucine-rich r
179 in-like peptide 3 (INSL3) is a member of the relaxin/insulin superfamily and is expressed in testicul
181 icacy studies of the therapeutic benefits of relaxin/insulin-like family peptide receptor 1 activatio
182 ent the first small-molecule series of human relaxin/insulin-like family peptide receptor 1 agonists.
185 function in adult males via interaction with relaxin/insulin-like family peptide receptor 2 (RXFP2).
186 d reduction in expression of INSL3 receptor, relaxin/insulin-like family peptide receptor 2 (RXFP2).
188 candidate genes, such as insulin-like 3 and relaxin/insulin-like family peptide receptor 2, in cases
191 tudies identify a novel antifibrotic role of relaxin involving the inhibition of the contractile phen
199 vessel disease (SVD), and determined whether relaxin is a treatment for SVD during hypertension.
200 dition, our previous study demonstrated that relaxin is beneficial to skeletal muscle healing by both
212 ivation interaction of RXFP1 and RXFP2 by H2 relaxin, leading to a potent and RXFP1-selective analog,
213 , these findings reveal an arterial-derived, relaxin ligand-receptor system that acts locally to regu
218 uggest that the receptor-binding site of the relaxin-like factor (RLF) is located in the flexible C-t
223 vered the signal initiation structure of the relaxin-like factor and shown its function to be indepen
224 s small protein permits one to study how the relaxin-like factor initiates the signal on the receptor
226 t targeting myofibroblast contractility with relaxin-like peptides may be of therapeutic benefit in t
231 t pathway, using LY294002, prevented both H2-relaxin-mediated phosphorylation of Akt and GSK-3beta an
233 lve parallel from the B-chain alpha-helix of relaxin, neutralize the charge repulsion of the juxta-po
234 ogenic therapeutic properties of recombinant relaxin peptide hormone have been investigated in severa
236 ed with relaxin (4 mug/h, osmotic minipump), relaxin plus PPARgamma inhibitor GW9662 (10 mg/kg/d), or
240 strate that p53(R273H) binds directly to the relaxin promoter, further confirming a role for H2 relax
242 eptor, formyl peptide receptor-2 (FPR2), the relaxin receptor (LGR7), G-proteins (Galpha(q/11/o/13)),
244 local expression and function of relaxin and relaxin receptor in arteries of nonpregnant females and
245 ich has previously been shown to bind to the relaxin receptor LGR7, is most likely the endogenous lig
248 ly active GPCR signalosome, that couples the relaxin receptor, relaxin family peptide receptor 1 (RXF
253 zation of the signaling pathway reveals that relaxin regulates MLC(20) dephosphorylation and lung myo
254 cells stably expressing RXFP1, we found that relaxin regulation of PPARgamma activity requires accumu
258 w that inducible, intratumoral expression of relaxin (Rlx) either by transplanting tumor cells that c
260 tools to study the physiological roles of H3 relaxin/RXFP3 systems in the brain and important leads f
263 were explored to assess whether intravenous relaxin should be pursued in larger studies of acute hea
269 udy was to elucidate the mechanisms by which relaxin stimulates the endothelial ETB receptor/NO vasod
271 omized controlled trial of recombinant human relaxin suggested that a dosage of 25 microg/kg/day was
274 to develop analogues of human relaxin-3 (H3 relaxin) that can selectively bind and activate its rece
275 hypertension) in 7 patients who had received relaxin therapy but in none who had received placebo.
276 ccompanied by decreases in the ability of H3 relaxin to compete for (33)P-relaxin binding to the chim
277 nd primary human myoblasts were treated with relaxin to investigate its potential effect in vitro; re
282 MMP-2 activity in small renal arteries from relaxin-treated nonpregnant and midterm pregnant rats re
283 genic reactivity of these blood vessels from relaxin-treated nonpregnant and midterm pregnant rats wa
284 enic reactivity of small renal arteries from relaxin-treated nonpregnant and midterm pregnant rats.
285 enic reactivity of small renal arteries from relaxin-treated nonpregnant rats was absent in ETB recep
286 Length of stay was 10.2 days (SD 6.1) for relaxin-treated patients versus 12.0 days (7.3) for thos
289 21.0 in the D-Pen Trial cohort, 27.3 in the Relaxin Trial cohort, and 26.1 in the Collagen Trial coh
290 ), recombinant human relaxin versus placebo (Relaxin Trial), and oral bovine type I collagen versus p
291 nicillamine (D-Pen Trial), recombinant human relaxin versus placebo (Relaxin Trial), and oral bovine
292 o investigate its potential effect in vitro; relaxin was also injected intramuscularly into the injur
293 lure and normal-to-increased blood pressure, relaxin was associated with favourable relief of dyspnoe
298 dies for rat and mouse Lgr7 receptor and rat relaxin, we also identified protein expression in arteri
299 s, such as urotensin-II, ghrelin, apelin and relaxin, which are most likely to provide novel targets
300 es, suggesting that high level expression of relaxin will not enhance metastatic spread of tumors.
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