Species selectivity of small-molecular antagonists for the CCR5 chemokine receptor.

  title={Species selectivity of small-molecular antagonists for the CCR5 chemokine receptor.},
  author={Yuji Saita and Mitsuhiro Kondo and Yasuaki Shimizu},
  journal={International immunopharmacology},
  volume={7 12},
The species selectivity of four structurally different compounds, SCH-351125, E-913, TAK-779 and UK-427857 has been examined using cloned human, rhesus, and mouse CCR5 receptors. SCH-351125 and E-913 potently inhibited the binding of [125I]-CCL3 to human CCR5, but their inhibitory activities against rhesus CCR5 were more than 10-fold weaker. In contrast, TAK-779 and UK-427857 inhibited binding to human and rhesus CCR5 with similar potency. The inhibitory activities of all four compounds against… CONTINUE READING

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