Synthesis and anti-aggregatory activity of linear retro-inverso RGD peptides.
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.
Dal Pozzo
A
A
G. Ronzoni Institute of Chemical and Biochemical Research, Milan, Italy. dalpozzo@ronzoni.it
Fagnoni
M
M
Bergonzi
R
R
Vanini
L
L
de Castiglione
R
R
Aglio
C
C
Colli
S
S
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
D000577:Amides; D009842:Oligopeptides; D010975:Platelet Aggregation Inhibitors; C047981:arginyl-glycyl-aspartic acid