Functional analysis of relaxin and INSL3 receptors
Grant number: 628427 | Funding period: 2010 - 2012
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 (15)
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
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
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
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
The inhibition of the G protein-coupled receptor, relaxin family peptide receptor 1 (RXFP1), by a small LDLa protein may be a pote..
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
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
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
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
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
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
Relaxin-3 is a highly conserved neuropeptide in vertebrate species and binds to the Class A G protein-coupled receptor (GPCR) RXFP..