title: Conformational aspects of human formyl-peptide receptor agonists.
abstract: The conformation of several Met-Ile-Phe-Leu analogues was analyzed using circular dichroism and infra-red absorption. Their effect on human neutrophils was verified by receptor binding assays and measurements of lysozyme release. The results demonstrate that in amphipatic environments the compounds examined can be highly and weakly ordered in beta-turn structures, in dependence on their N-terminal substituents. The ability of the compounds to evoke neutrophil functions appears strongly and weakly influenced by N- and C-terminal modification, respectively.
authors.affiliation: Department of Pharmaceutical Sciences, Ferrara University, Ferrara, Italy. dla@dns.unife.it
authors.forename: Alessandro
authors.initials: A
authors.lastname: Dalpiaz
authors.forename: Gianni
authors.initials: G
authors.lastname: Vertuani
authors.forename: Angelo
authors.initials: A
authors.lastname: Scatturin
authors.forename: Federica
authors.initials: F
authors.lastname: Vitali
authors.forename: Katia
authors.initials: K
authors.lastname: Varani
authors.forename: Susanna
authors.initials: S
authors.lastname: Spisani
mesh_terms: D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002942:Circular Dichroism; D003594:Cytoplasmic Granules / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D066298:In Vitro Techniques; D008247:Lysosomes / Q000187:drug effects / Q000378:metabolism; D008968:Molecular Conformation; D009113:Muramidase / Q000187:drug effects / Q000378:metabolism; D009504:Neutrophils / Q000187:drug effects / Q000378:metabolism; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D044042:Receptors, Formyl Peptide / Q000819:agonists*; D012997:Solvents; D017550:Spectroscopy, Fourier Transform Infrared; D013329:Structure-Activity Relationship
chemical_list: C480200:Met-Ile-Phe-Leu; D009842:Oligopeptides; D044042:Receptors, Formyl Peptide; D012997:Solvents; D009113:Muramidase