Identification and optimization of small-molecule agonists of the human relaxin hormone receptor RXFP1.

@article{Xiao2013IdentificationAO,
  title={Identification and optimization of small-molecule agonists of the human relaxin hormone receptor RXFP1.},
  author={Jingbo Xiao and Zaohua Huang and Catherine Z. Chen and Irina U Agoulnik and Noel Southall and Xin Hu and Raisa E Jones and Marc Ferrer and Wei Zheng and Alexander I. Agoulnik and Juan Jose Marugan},
  journal={Nature communications},
  year={2013},
  volume={4},
  pages={1953}
}
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… CONTINUE READING
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