Functional analysis of relaxin and INSL3 receptors

Grant number: 628427 | Funding period: 2010 - 2012

Completed

Abstract

The peptide hormone relaxin is currently in clinical trials to treat acute heart failure. The related hormone INSL3 has important roles in fertility. We will continue our previously successful approaches to study the interaction of relaxin and INSL3 with their cell surface receptors and the mechanisms by which the receptors function. The knowledge gained will aid in the design of smaller, more potent and orally active forms of relaxin and INSL3 for future clinical applications.

Related publications (11)

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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

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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

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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

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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

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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

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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

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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

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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..

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RELAXIN FAMILY PEPTIDES AND THEIR RECEPTORS

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

2013-01-01

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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

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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..