Polymeric analogues of N-formyl peptides are potent activators of degranulation and superoxide production by human neutrophils.
Analogues of N-formyl methionyl leucyl phenylalanine possessing three and four peptide units grafted onto an inert carbon skeleton were tested as activators of human polymorphonuclear leukocytes. For the two responses studied, degranulation and respiratory burst, the polymeric analogues showed two maxima of activity, one at the same concentration as the monomer, the other one at a concentration 100- to 1000-fold lower. The potency of the polymers with respect to the monomer is discussed in terms of receptor clustering. The similarity of the dose-response curves for superoxide production and lysozyme secretion indicates that the early transmembrane signalling events are identical for the two responses studied.
Ravel
P
P
INSERM U25, CNRS UA 122, Hôpital Necker, Paris, France.
Kraus
J L
JL
Lederer
F
F
D015550:Cell Degranulation / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D066298:In Vitro Techniques; D009113:Muramidase / Q000378:metabolism; D009240:N-Formylmethionine Leucyl-Phenylalanine / Q000494:pharmacology*; D009504:Neutrophils / Q000502:physiology*; D013329:Structure-Activity Relationship; D013481:Superoxides / Q000378:metabolism*
D013481:Superoxides; D009240:N-Formylmethionine Leucyl-Phenylalanine; D009113:Muramidase