Determining modes of binding and activation of complex G-protein coupled receptor targets

Grant number: 1043750 | Funding period: 2013 - 2015

Completed

Abstract

The peptide hormones relaxin is currently in a Phase III trial for the treatment of heart failure. However the peptide is not a good drug as it can't be taken orally and is very expensive to produce. We will study the interaction of relaxin and the related peptide 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 which will be able to be used as drugs for the treatment of heart failure.

Related publications (6)

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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..