Discovery and Cardioprotective Effects of the First Non-Peptide Agonists of the G Protein-Coupled Prokineticin Receptor-1

@inproceedings{Gasser2015DiscoveryAC,
  title={Discovery and Cardioprotective Effects of the First Non-Peptide Agonists of the G Protein-Coupled Prokineticin Receptor-1},
  author={Adeline Gasser and Simone Brogi and Kyoji Urayama and Toshishide Nishi and Hitoshi Kurose and Andrea Tafi and Nigel Ribeiro and Laurent D{\'e}saubry and Canan G Nebigil},
  booktitle={PloS one},
  year={2015}
}
Prokineticins are angiogenic hormones that activate two G protein-coupled receptors: PKR1 and PKR2. PKR1 has emerged as a critical mediator of cardiovascular homeostasis and cardioprotection. Identification of non-peptide PKR1 agonists that contribute to myocardial repair and collateral vessel growth hold promises for treatment of heart diseases. Through a combination of in silico studies, medicinal chemistry, and pharmacological profiling approaches, we designed, synthesized, and characterized… CONTINUE READING
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