title: Identification of a receptor-binding region in the core segment of the human anaphylatoxin C5a.
abstract: In order to identify regions of C5a that contribute to receptor binding and functional activity of the anaphylatoxin, a series of peptides was synthesized in which core segments have been attached to C-terminal segments via native peptidic or disulfide bonds. It has been found that residues Arg40 and Arg46 in the loop-3 region of the core induce a 1000-fold increase in the affinity of the disordered C-terminal segment of C5a. The results obtained from this work lead to the conclusion that the loop-3 region is most likely the core binding site of C5a.
authors.affiliation: CIBA-GEIGY Corporation, Research Department, Summit, New Jersey 07901.
authors.forename: I
authors.initials: I
authors.lastname: Vlattas
authors.forename: I I
authors.initials: II
authors.lastname: Sytwu
authors.forename: J
authors.initials: J
authors.lastname: Dellureficio
authors.forename: J
authors.initials: J
authors.lastname: Stanton
authors.forename: A F
authors.initials: AF
authors.lastname: Braunwalder
authors.forename: N
authors.initials: N
authors.lastname: Galakatos
authors.forename: R
authors.initials: R
authors.lastname: Kramer
authors.forename: B
authors.initials: B
authors.lastname: Seligmann
authors.forename: M A
authors.initials: MA
authors.lastname: Sills
authors.forename: J
authors.initials: J
authors.lastname: Wasvary
mesh_terms: D000595:Amino Acid Sequence; D001120:Arginine; D001665:Binding Sites; D002462:Cell Membrane / Q000378:metabolism; D015936:Complement C5a / Q000737:chemistry / Q000378:metabolism*; D004220:Disulfides; D006801:Humans; D007700:Kinetics; D008961:Models, Structural; D008969:Molecular Sequence Data; D009504:Neutrophils / Q000378:metabolism; D010455:Peptides / Q000138:chemical synthesis* / Q000378:metabolism; D010456:Peptides, Cyclic / Q000138:chemical synthesis / Q000378:metabolism; D017433:Protein Structure, Secondary; D044087:Receptor, Anaphylatoxin C5a; D011951:Receptors, Complement / Q000378:metabolism*
chemical_list: D004220:Disulfides; D010455:Peptides; D010456:Peptides, Cyclic; D044087:Receptor, Anaphylatoxin C5a; D011951:Receptors, Complement; D015936:Complement C5a; D001120:Arginine