Methyl ester of N-formylmethionyl-leucyl-phenylalanine: chemotactic responses of human blood monocytes and inhibition of gold compounds.
N-formylmethionyl-leucyl-phenylalanine, a potent hemotactic peptide for human polymorphonuclear leukocytes, is less chemotactic for human blood monocytes. Esterification of the N-formylated tripeptide enhances its chemotactic activity for monocytes by more than 4 logs, whereas a decrease by 3 logs is observed for polymorphonuclear leukocytes. These results indicate the participation of the C-terminal carboxyl group in chemotaxis of different cell types. We have also observed the selective inhibition of chemotactic responsiveness of human blood monocytes by a clinically useful antirheumatic drug, sodium aurothiomalate. Since this is the first in vitro cell migration model of inflammation in which gold compounds have demonstrated activity in micromolar concentrations, it suggests a site of action for this antirheumatic drug.
D002634:Chemotaxis, Leukocyte / Q000187:drug effects*; D006052:Gold Sodium Thiomalate / Q000494:pharmacology*; D006801:Humans; D008715:Methionine / Q000031:analogs & derivatives*; D009000:Monocytes / Q000502:physiology*; D009239:N-Formylmethionine / Q000031:analogs & derivatives* / Q000494:pharmacology; D009504:Neutrophils / Q000502:physiology; D009842:Oligopeptides / Q000494:pharmacology*
D009842:Oligopeptides; D006052:Gold Sodium Thiomalate; D009239:N-Formylmethionine; D008715:Methionine