Development of a selective agonist for relaxin family peptide receptor 3

@inproceedings{Wei2017DevelopmentOA,
  title={Development of a selective agonist for relaxin family peptide receptor 3},
  author={Dian Wei and Meng-Jun Hu and Xiao-xia Shao and J H Wang and Wei-Han Nie and Ya-li Liu and Zeng-guang Xu and Zhan-yun Guo},
  booktitle={Scientific Reports},
  year={2017}
}
Relaxin family peptides perform a variety of biological functions by activating four G protein-coupled receptors, namely RXFP1–4. Among these receptors, RXFP3 lacks a specific natural or synthetic agonist at present. A previously designed chimeric R3/I5 peptide, consisting of the B-chain of relaxin-3 and the A-chain of INSL5, displays equal activity towards the homologous RXFP3 and RXFP4. To increase its selectivity towards RXFP3, in the present study we conducted extensive mutagenesis around… CONTINUE READING