Structure-based discovery of beta2-adrenergic receptor ligands.

  title={Structure-based discovery of beta2-adrenergic receptor ligands.},
  author={Peter Kolb and Daniel M Rosenbaum and John J. Irwin and Juan Jos{\'e} Fung and Brian K. Kobilka and Brian K. Shoichet},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  volume={106 16},
Aminergic G protein-coupled receptors (GPCRs) have been a major focus of pharmaceutical research for many years. Due partly to the lack of reliable receptor structures, drug discovery efforts have been largely ligand-based. The recently determined X-ray structure of the beta(2)-adrenergic receptor offers an opportunity to investigate the advantages and limitations inherent in a structure-based approach to ligand discovery against this and related GPCR targets. Approximately 1 million… CONTINUE READING