Literature DB >> 15956730

Responses of GPCR135 to human gene 3 (H3) relaxin in CHO-K1 cells determined by microphysiometry.

Emma T Van der Westhuizen1, Patrick M Sexton, Ross A D Bathgate, Roger J Summers.   

Abstract

This study examined the functional response to human relaxin 2 (H2 relaxin), human relaxin 3 (H3 relaxin), 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 assessed. Saturation studies of [125I] H3 relaxin binding to GPCR135 in these cells gave a Bmax of 32.61 +/- 6.5 fmol/mg protein and Kd of 0.12 +/- 0.08 nM. The functional response to H3 relaxin and other relaxin/insulin peptides of GPCR135 expressed in CHO-K1 cells was measured in the cytosensor microphysiometer and analyzed using inhibitors of signal transduction proteins.

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Year:  2005        PMID： 15956730     DOI： 10.1196/annals.1282.053

Source DB:  PubMed          Journal:  Ann N Y Acad Sci        ISSN： 0077-8923            Impact factor:   5.691


  9 in total

1.  Orthosteric, Allosteric and Biased Signalling at the Relaxin-3 Receptor RXFP3.

Authors:  Martina Kocan; Sheng Yu Ang; Roger J Summers
Journal:  Neurochem Res       Date:  2015-08-21       Impact factor: 3.996

Review 2.  Relaxin family peptide receptors--former orphans reunite with their parent ligands to activate multiple signalling pathways.

Authors:  M L Halls; E T van der Westhuizen; R A D Bathgate; R J Summers
Journal:  Br J Pharmacol       Date:  2007-02-12       Impact factor: 8.739

3.  Binding conformation and determinants of a single-chain peptide antagonist at the relaxin-3 receptor RXFP3.

Authors:  Linda M Haugaard-Kedström; Han Siean Lee; Maryon V Jones; Angela Song; Vishaal Rathod; Mohammed Akhter Hossain; Ross A D Bathgate; K Johan Rosengren
Journal:  J Biol Chem       Date:  2018-08-21       Impact factor: 5.157

Review 4.  International Union of Basic and Clinical Pharmacology. XCV. Recent advances in the understanding of the pharmacology and biological roles of relaxin family peptide receptors 1-4, the receptors for relaxin family peptides.

Authors:  Michelle L Halls; Ross A D Bathgate; Steve W Sutton; Thomas B Dschietzig; Roger J Summers
Journal:  Pharmacol Rev       Date:  2015       Impact factor: 25.468

5.  In vitro pharmacological characterization of RXFP3 allosterism: an example of probe dependency.

Authors:  Lily Alvarez-Jaimes; Steven W Sutton; Diane Nepomuceno; S Timothy Motley; Miroslav Cik; Emily Stocking; James Shoblock; Pascal Bonaventure
Journal:  PLoS One       Date:  2012-02-07       Impact factor: 3.240

6.  GABAergic Neurons in the Rat Medial Septal Complex Express Relaxin-3 Receptor (RXFP3) mRNA.

Authors:  Hector Albert-Gascó; Sherie Ma; Francisco Ros-Bernal; Ana M Sánchez-Pérez; Andrew L Gundlach; Francisco E Olucha-Bordonau
Journal:  Front Neuroanat       Date:  2018-01-17       Impact factor: 3.856

7.  Involvement of the Nucleus Incertus and Relaxin-3/RXFP3 Signaling System in Explicit and Implicit Memory.

Authors:  Isis Gil-Miravet; Aroa Mañas-Ojeda; Francisco Ros-Bernal; Esther Castillo-Gómez; Hector Albert-Gascó; Andrew L Gundlach; Francisco E Olucha-Bordonau
Journal:  Front Neuroanat       Date:  2021-03-18       Impact factor: 3.856

8.  Targeted viral vector transduction of relaxin-3 neurons in the rat nucleus incertus using a novel cell-type specific promoter.

Authors:  Alexander D Wykes; Sherie Ma; Ross A D Bathgate; Andrew L Gundlach
Journal:  IBRO Rep       Date:  2019-12-13

9.  High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist.

Authors:  Guangyao Lin; Yang Feng; Xiaoqing Cai; Caihong Zhou; Lijun Shao; Yan Chen; Linhai Chen; Qing Liu; Qingtong Zhou; Ross A D Bathgate; Dehua Yang; Ming-Wei Wang
Journal:  Molecules       Date:  2021-12-11       Impact factor: 4.411
  9 in total

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