title: New chemotactic peptide analogs with high biological activity for human neutrophils.
abstract: As a part of a research programme aimed at studying structure activity relationships in the field of chemotactic peptides, modified analogs of the chemoattractant N-formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP) were examined for their capacity to activate several functions of human neutrophils. 4-Aminotetrahydrothiopyran-4carboxylic acid (Thp) and 2-aminoindane-2-carboxylic acid (Ain) were chosen as achiral, conformationally restricted amino acids suitable for mimicking the external Met and Phe residues of FMLP-OMe. The replacement of both produces a high locomotion activity, greater than the parent peptide; in contrast, the two Thp-containing analogs induce neither superoxide production nor lysozyme release. From these results we can hypothesize two different signal transduction systems: one which provides for movement, the other for superoxide generation and granule enzyme release.
authors.affiliation: Istituto di Chimica Biologica, Università degli Studi di Ferrara, Italy.
authors.forename: S
authors.initials: S
authors.lastname: Spisani
authors.forename: S
authors.initials: S
authors.lastname: Traniello
authors.forename: A L
authors.initials: AL
authors.lastname: Giuliani
authors.forename: I
authors.initials: I
authors.lastname: Torrini
authors.forename: G
authors.initials: G
authors.lastname: Pagani Zecchini
authors.forename: M
authors.initials: M
authors.lastname: Paglialunga Paradisi
authors.forename: E
authors.initials: E
authors.lastname: Gavuzzo
authors.forename: F
authors.initials: F
authors.lastname: Mazza
authors.forename: G
authors.initials: G
authors.lastname: Pochetti
authors.forename: G
authors.initials: G
authors.lastname: Lucente
mesh_terms: D000595:Amino Acid Sequence; D002634:Chemotaxis, Leukocyte / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D008969:Molecular Sequence Data; D015394:Molecular Structure; D009113:Muramidase / Q000378:metabolism; D009240:N-Formylmethionine Leucyl-Phenylalanine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D009504:Neutrophils / Q000187:drug effects* / Q000502:physiology; D011487:Protein Conformation; D044042:Receptors, Formyl Peptide; D011971:Receptors, Immunologic / Q000187:drug effects / Q000502:physiology; D015398:Signal Transduction / Q000187:drug effects; D013481:Superoxides / Q000378:metabolism
chemical_list: D044042:Receptors, Formyl Peptide; D011971:Receptors, Immunologic; D013481:Superoxides; D009240:N-Formylmethionine Leucyl-Phenylalanine; D009113:Muramidase