Journal
NATURE COMMUNICATIONS
Volume 4, Issue -, Pages -Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/ncomms2953
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Funding
- Molecular Libraries Initiative of the NIH Roadmap for Medical Research [U54MH084681, R03MH085705]
- Intramural Research Program of the National Human Genome Research Institute (NHGRI)
- National Center for Advancing Translational Sciences (NCATS)
- National Institutes of Health (NIH)
- Faculty Research Support Program of the Florida International University
- NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES [ZIBTR000002] Funding Source: NIH RePORTER
- NATIONAL HUMAN GENOME RESEARCH INSTITUTE [Z01HG200319] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF MENTAL HEALTH [R03MH085705] Funding Source: NIH RePORTER
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The anti-fibrotic, vasodilatory and pro-angiogenic therapeutic properties of recombinant relaxin peptide hormone have been investigated in several diseases, and recent clinical trial data has shown benefit in treating acute heart failure. However, the remodelling capacity of these peptide hormones is difficult to study in chronic settings because of their short half-life and the need for intravenous administration. Here we present the first small-molecule series of human relaxin/insulin-like family peptide receptor 1 agonists. These molecules display similar efficacy as the natural hormone in several functional assays. Mutagenesis studies indicate that the small molecules activate relaxin receptor through an allosteric site. These compounds have excellent physical and in vivo pharmacokinetic properties to support further investigation of relaxin biology and animal efficacy studies of the therapeutic benefits of relaxin/insulin-like family peptide receptor 1 activation.
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