Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimetics.
In this paper, we describe the synthesis of a selected library of heterochiral d-Pro-containing RGD-peptidomimetics (RpD) and we investigate the biological activity as inhibitors of fibronectin adhesion to SK-MEL-24 tumor cells. In particular, peptides 4 and 8 showed an IC(50) in the 10(-8)M range. Despite the linear structure, the peptides tend to adopt a folded conformation in a polar environment.
Gentilucci
Luca
L
Department of Chemistry G. Ciamician, Università degli Studi di Bologna, Via Selmi 2, 40126 Bologna, Italy. luca.gentilucci@ciam.unibo.it
Cardillo
Giuliana
G
Squassabia
Federico
F
Tolomelli
Alessandra
A
Spampinato
Santi
S
Sparta
Antonino
A
Baiula
Monica
M
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002448:Cell Adhesion / Q000187:drug effects*; D045744:Cell Line, Tumor; D005353:Fibronectins / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D018716:Molecular Mimicry; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology*; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology*; D019151:Peptide Library; D011392:Proline; D011487:Protein Conformation; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D005353:Fibronectins; D009842:Oligopeptides; D019151:Peptide Library; C047981:arginyl-glycyl-aspartic acid; D011392:Proline