Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity
DR March, LM Proctor, MJ Stoermer, R Sbaglia… - Molecular …, 2004 - Elsevier
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 for small molecule antagonists has …
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 for small molecule antagonists has …
