Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity.

@article{March2004PotentCA,
  title={Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity.},
  author={Darren R March and Lavinia M Proctor and Martin J. Stoermer and Robert Sbaglia and Giovanni Abbenante and Robert C Reid and Trent M Woodruff and Khemar Wadi and Natalii J. Paczkowski and Joel D A Tyndall and Stephen M. Taylor and David P. Fairlie},
  journal={Molecular pharmacology},
  year={2004},
  volume={65 4},
  pages={868-79}
}
Human C5a is a plasma protein with potent chemoattractant and pro-inflammatory properties, and its overexpression correlates with severity of inflammatory diseases. C5a binds to its G protein-coupled receptor (C5aR) on polymorphonuclear leukocytes (PMNLs) through a high-affinity helical bundle and a low-affinity C terminus, the latter being solely responsible for receptor activation. Potent and selective C5a antagonists are predicted to be effective anti-inflammatory drugs, but no pharmacophore… CONTINUE READING
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