C5a mutants are potent antagonists of the C5a receptor (CD88) and of C5L2: position 69 is the locus that determines agonism or antagonism
M Otto, H Hawlisch, PN Monk, M Muller, A Klos… - Journal of Biological …, 2004 - ASBMB
The anaphylatoxin C5a exerts a plethora of biologic activities critical in the pathogenesis of
systemic inflammatory diseases. Recently, we reported on a C5a mutant, jun/fos-A8, as a
potent antagonist for the human and mouse C5a receptor (CD88). Addressing the molecular
mechanism accounting for CD88 receptor antagonism by site-directed mutagenesis, we
found that a positively charged amino acid at position 69 is crucial. Replacements by either
hydrophobic or negatively charged amino acids switched the CD88 antagonist jun/fos-A8 to …
systemic inflammatory diseases. Recently, we reported on a C5a mutant, jun/fos-A8, as a
potent antagonist for the human and mouse C5a receptor (CD88). Addressing the molecular
mechanism accounting for CD88 receptor antagonism by site-directed mutagenesis, we
found that a positively charged amino acid at position 69 is crucial. Replacements by either
hydrophobic or negatively charged amino acids switched the CD88 antagonist jun/fos-A8 to …
