Determining modes of binding and activation of complex G-protein coupled receptor targets
Grant number: 1043750 | Funding period: 2013 - 2015
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)
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
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..