Structure-activity relationship of for-L-Met L-Leu-L-Phe-OMe analogues in human neutrophils.
Neutrophils constitute the first line of defence against bacterial invasion. They migrate to infected tissues along a concentration gradient of chemoattractant molecules, the most important of which is for-Met-Leu-Phe-OH (fMLP). Different responses arise from formylpeptides binding to different isoforms of the specific receptor. The aim of the studies reported herein was to clarify (i) the role of fMLP-OMe amide bonds in receptor-ligand cross-linking, (ii) the nature of the group occupying the N- and C-terminal positions, (iii) the features peculiar to the Met, Leu, and Phe receptor pockets, and (iv) the features which determine the specific neutrophil response.
Cavicchioni
Giorgio
G
Department of Pharmaceutical Sciences, University of Ferrara, 44100 Ferrara, Italy. g5z@unife.it
Fraulini
Anna
A
Falzarano
Sofia
S
Spisani
Susanna
S
D002630:Chemotactic Factors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D002634:Chemotaxis, Leukocyte / Q000187:drug effects; D006801:Humans; D015394:Molecular Structure; D009240:N-Formylmethionine Leucyl-Phenylalanine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology*; D009504:Neutrophils / Q000187:drug effects*; D011485:Protein Binding; D044042:Receptors, Formyl Peptide / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship
D002630:Chemotactic Factors; D044042:Receptors, Formyl Peptide; D009240:N-Formylmethionine Leucyl-Phenylalanine