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.
Synthesis and anti-aggregatory activity of linear retro-inverso RGD peptides / A. Dal Pozzo, M. Fagnoni, R. Bergonzi, L. Vanini, R. de Castiglione, C. Aglio, S. Colli. - In: JOURNAL OF PEPTIDE RESEARCH. - ISSN 1397-002X. - 55:6(2000 Jun), pp. 447-454. [10.1034/j.1399-3011.2000.00713.x]
Synthesis and anti-aggregatory activity of linear retro-inverso RGD peptides
S. ColliUltimo
2000
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.Pubblicazioni consigliate
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