Functional analysis of relaxin and INSL3 receptors

The relaxin receptor as a therapeutic target - perspectives from evolution Cheek for updates and drug targeting

Ross AD Bathgate, Martina Kocan, Daniel J Scott, M Akhter Hossain, Sara V Good, Sergey Yegorov, Jan Bogerd, Paul R Gooley

2018-07-01

The peptide relaxin was first identified as an important circulating hormone during pregnancy over 90 years ago. Research over man..

ML290 is a biased allosteric agonist at the relaxin receptor RXFP1

Martina Kocan, Mohsin Sarwar, Sheng Y Ang, Jingbo Xiao, Juan J Marugan, Mohammed A Hossain, Chao Wang, Dana S Hutchinson, Chrishan S Samuel, Alexander I Agoulnik, Ross AD Bathgate, Roger J Summers

2017-06-07

Activation of the relaxin receptor RXFP1 has been associated with improved survival in acute heart failure. ML290 is a small molec..

The complex binding mode of the peptide hormone H2 relaxin to its receptor RXFP1

Ashish Sethi, Shoni Bruell, Nitin Patil, Mohammed Akhter Hossain, Daniel J Scott, Emma J Petrie, Ross AD Bathgate, Paul R Gooley

2016-04-01

H2 relaxin activates the relaxin family peptide receptor-1 (RXFP1), a class A G-protein coupled receptor, by a poorly understood m..

Native Chemical Ligation to Minimize Aspartimide Formation during Chemical Synthesis of Small LDLa Protein

Julien Tailhades, Ashish Sethi, Emma J Petrie, Paul R Gooley, Ross A Bathgate, John D Wade, Mohammed A Hossain

2016-01-18

The inhibition of the G protein-coupled receptor, relaxin family peptide receptor 1 (RXFP1), by a small LDLa protein may be a pote..

In a class of their own-RXFP1 and RXFP2 are unique members of the LGR family

Emma J Petrie, Samantha Lagaida, Ashish Sethi, Ross AD Bathgate, Paul R Gooley

2015-09-07

The leucine-rich repeat-containing G protein-coupled receptors (LGRs) family consists of three groups: types A, B, and C and all c..

Activation of relaxin family receptor 1 from different mammalian species by relaxin peptide and small-molecule agonist ML290

Zaohua Huang, Courtney Myhr, Ross AD Bathgate, Brian A Ho, Amaya Bueno, Xin Hu, Jingbo Xiao, Noel Southall, Elena Barnaeva, Irina U Agoulnik, Juan J Marugan, Marc Ferrer, Alexander I Agoulnik

2015-08-17

Relaxin peptide (RLN), which signals through the relaxin family peptide 1 (RXFP1) GPCR receptor, has shown therapeutic effects in ..

Investigation of Interactions at the Extracellular Loops of the Relaxin Family Peptide Receptor 1 (RXFP1)

Natalie A Diepenhorst, Emma J Petrie, Catherine Z Chen, Amy Wang, Mohammed Akhter Hossain, Ross AD Bathgate, Paul R Gooley

2014-12-12

Relaxin, an emerging pharmaceutical treatment for acute heart failure, activates the relaxin family peptide receptor (RXFP1), whic..

Mapping Key Regions of the RXFP2 Low-Density Lipoprotein Class-A Module That Are Involved in Signal Activation

Roy CK Kong, Ross AD Bathgate, Shoni Bruell, John D Wade, Paul R Gooley, Emma J Petrie

2014-07-22

The peptide hormone INSL3 and its receptor, RXFP2, have co-evolved alongside relaxin and its receptor, RXFP1. Both RXFP1 and RXFP2..

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

Roy CK Kong, Emma J Petrie, Biswaranjan Mohanty, Jason Ling, Jeremy CY Lee, Paul R Gooley, Ross AD Bathgate

2013-09-27

The peptide hormone relaxin is showing potential as a treatment for acute heart failure. Although it is known that relaxin mediate..

Chimeric RXFP1 and RXFP2 Receptors Highlight the Similar Mechanism of Activation Utilizing Their N-Terminal Low-Density Lipoprotein Class A Modules.

Shoni Bruell, Roy CK Kong, Emma J Petrie, Brad Hoare, John D Wade, Daniel J Scott, Paul R Gooley, Ross AD Bathgate

2013-01-01

Relaxin family peptide (RXFP) receptors 1 and 2 are unique G-protein coupled receptors in that they contain an N-terminal low-dens..

Elucidation of relaxin-3 binding interactions in the extracellular loops of RXFP3.

Ross AD Bathgate, Maria HY Oh, WJ Jason Ling, Quentin Kaas, M Akhter Hossain, Paul R Gooley, K Johan Rosengren

2013-01-01

Relaxin-3 is a highly conserved neuropeptide in vertebrate species and binds to the Class A G protein-coupled receptor (GPCR) RXFP..

RELAXIN FAMILY PEPTIDES AND THEIR RECEPTORS

RAD Bathgate, ML Halls, ET van der Westhuizen, GE Callander, M Kocan, RJ Summers

2013-01-01

There are seven relaxin family peptides that are all structurally related to insulin. Relaxin has many roles in female and male re..

The Different Ligand-Binding Modes of Relaxin Family Peptide Receptors RXFP1 and RXFP2

Daniel J Scott, K Johan Rosengren, Ross AD Bathgate

2012-11-01

Relaxin and insulin-like peptide 3 (INSL3) are peptide hormones with a number of important physiological roles in reproduction, re..

The structural determinants of insulin-like Peptide 3 activity.

Ross AD Bathgate, Soude Zhang, Richard A Hughes, K Johan Rosengren, John D Wade

2012-01-01

Insulin-like peptide 3 (INSL3) is a hormone and/or paracrine factor which is a member of the relaxin peptide family. It has key ro..

A novel protein engineering approach for investigating GPCR/ligand interactions

Natalie Anne Witteveen, Paul R Gooley, Martin J Stone, Ross AD Bathgate

2011-04-01