Structural Determinants of A3 Adenosine Receptor Activation: Nucleoside Ligands at the Agonist/Antagonist Boundary

@article{Gao2002StructuralDO,
  title={Structural Determinants of A3 Adenosine Receptor Activation: Nucleoside Ligands at the Agonist/Antagonist Boundary},
  author={Zhang-Guo Gao and Soo-Kyung Kim and Thibaud Biadatti and Wangzhong Chen and Kyeong Lee and D. Barak and S. G. Kim and Carl R. Johnson and K. Jacobson},
  journal={Journal of Medicinal Chemistry},
  year={2002},
  volume={45},
  pages={4471-4484}
}
Mutagenesis of the human A3 adenosine receptor (AR) suggested that certain amino acid residues contributed differently to ligand binding and activation processes. Here we demonstrated that various adenosine modifications, including adenine substitution and ribose ring constraints, also contributed differentially to these processes. The ligand effects on cyclic AMP production in intact CHO cells expressing the A3AR and in receptor binding were compared. Notably, the simple 2-fluoro group alone… Expand
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