title: Synthesis and anti-aggregatory activity of linear retro-inverso RGD peptides.
abstract: Six retro-inverso tri- and tetrapeptide analogues of RGD were prepared and their anti-aggregatory activity was determined by platelet aggregation tests in comparison with the corresponding parent peptides. An efficient method for the introduction of a malonyl-aspartic residue into a peptide chain is described for the first time. A 2-3-fold decrease in potency or total loss of bioactivity was observed with the new peptides; structure-activity relationships are discussed.
authors.affiliation: G. Ronzoni Institute of Chemical and Biochemical Research, Milan, Italy. dalpozzo@ronzoni.it
authors.forename: A
authors.initials: A
authors.lastname: Dal Pozzo
authors.forename: M
authors.initials: M
authors.lastname: Fagnoni
authors.forename: R
authors.initials: R
authors.lastname: Bergonzi
authors.forename: L
authors.initials: L
authors.lastname: Vanini
authors.forename: R
authors.initials: R
authors.lastname: de Castiglione
authors.forename: C
authors.initials: C
authors.lastname: Aglio
authors.forename: S
authors.initials: S
authors.lastname: Colli
mesh_terms: D000577:Amides / Q000737:chemistry; D006801:Humans; D006860:Hydrogen Bonding; D015394:Molecular Structure; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011487:Protein Conformation; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D009842:Oligopeptides; D010975:Platelet Aggregation Inhibitors; C047981:arginyl-glycyl-aspartic acid