title: In vitro activity of the αvβ3 integrin antagonist RGDechi-hCit on malignant melanoma cells.
abstract: BACKGROUND
  In malignant melanoma (MM), overexpression of αvβ3 integrin is linked to a more metastatic phenotype. Development of anti-αvβ3 agents able to counteract melanoma progression would be helpful for disease treatment. A new selective ligand of αvβ3, RGDechi-hCit, has anti-angiogenic properties against endothelial cells in animal angiogenesis models. The aim of this study was to evaluate the in vitro effects of the RGDechi-hCit peptide on MM cell lines.
  
  
  METHODS
  Cytofluorimetric analysis characterized the cell surface expression of αvβ3 integrin on seven MM cell lines: A375, WM266-4, SK-Mel-28, Sbcl2, LB24Dagi, PR-Mel and PNP-Mel. Cell proliferation, adhesion, and migration assays were carried out using the αvβ3-antagonist RGDechi-hCit.
  
  
  RESULTS
  Proliferation was not significantly inhibited by RGDechi-hCit, although striking morphological changes were detected in MM cell lines highly expressing αvβ3. Conversely, assays on fibronectin-coated plates showed a significant RGDechi-hCit dose-dependent inhibitory effect on both adhesion and migration.
  
  
  CONCLUSIONS
  The data demonstrate anti-adhesion and anti-migration, but not antiproliferative, activities of RGDechi-hCit against MM cells.
authors.affiliation: Istituto di Chimica Biomolecolare-CNR, Traversa La Crucca 3, 07100 Sassari, Italy. marina.pisano@icb.cnr.it
authors.forename: Marina
authors.initials: M
authors.lastname: Pisano
authors.forename: Ivan
authors.initials: I
authors.lastname: DE Paola
authors.forename: Valentina
authors.initials: V
authors.lastname: Nieddu
authors.forename: Ilaria
authors.initials: I
authors.lastname: Sassu
authors.forename: Sara
authors.initials: S
authors.lastname: Cossu
authors.forename: Grazia
authors.initials: G
authors.lastname: Galleri
authors.forename: Annarita
authors.initials: A
authors.lastname: Del Gatto
authors.forename: Mario
authors.initials: M
authors.lastname: Budroni
authors.forename: Antonio
authors.initials: A
authors.lastname: Cossu
authors.forename: Michele
authors.initials: M
authors.lastname: Saviano
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Palmieri
authors.forename: Laura
authors.initials: L
authors.lastname: Zaccaro
authors.forename: Carla
authors.initials: C
authors.lastname: Rozzo
mesh_terms: D020533:Angiogenesis Inhibitors / Q000494:pharmacology*; D002448:Cell Adhesion / Q000187:drug effects; D045744:Cell Line, Tumor; D002465:Cell Movement / Q000187:drug effects; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000032:analysis / Q000037:antagonists & inhibitors*; D008545:Melanoma / Q000188:drug therapy* / Q000473:pathology / Q000556:secondary; D010455:Peptides / Q000494:pharmacology*
chemical_list: D020533:Angiogenesis Inhibitors; D039302:Integrin alphaVbeta3; D010455:Peptides; C581099:RGDechi-hCit peptide