Ligand chain length drives activation of lipid G protein-coupled receptors

  title={Ligand chain length drives activation of lipid G protein-coupled receptors},
  author={Anastassia Troupiotis-Tsa{\"i}laki and Julian Zachmann and In{\'e}s Gonz{\'a}lez-Gil and {\'A}ngel Gonz{\'a}lez and Silvia Ortega-Guti{\'e}rrez and Mar{\'i}a L. L{\'o}pez-Rodr{\'i}guez and Leonardo Pardo and C{\'e}dric Govaerts},
  booktitle={Scientific Reports},
Sphingosine-1-phosphate (S1P) is a lipid mediator that can activate five cell membrane G protein-coupled receptors (GPCRs) which carry a variety of essential functions and are promising drug targets. S1P is composed of a polar zwitterionic head-group and a hydrophobic alkyl chain. This implies an activation mechanism of its cognate receptor that must be significantly different from what is known for prototypical GPCRs (ie receptor to small hydrophilic ligands). Here we aim to identify the… CONTINUE READING
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