RGDechi-hCit 对恶性黑素瘤细胞的 αvβ3 整合素拮抗作用的体外研究。

In vitro activity of the αvβ3 integrin antagonist RGDechi-hCit on malignant melanoma cells.

机构信息

Istituto di Chimica Biomolecolare-CNR, Traversa La Crucca 3, 07100 Sassari, Italy.

出版信息

Anticancer Res. 2013 Mar;33(3):871-9.

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.

MATERIALS AND 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.

CONCLUSION

The data demonstrate anti-adhesion and anti-migration, but not antiproliferative, activities of RGDechi-hCit against MM cells.

摘要

背景

在恶性黑色素瘤（MM）中，αvβ3 整联蛋白的过表达与更具转移性的表型相关。开发能够对抗黑色素瘤进展的抗αvβ3 药物将有助于疾病的治疗。一种新的 αvβ3 选择性配体 RGDechi-hCit，在动物血管生成模型中具有抗内皮细胞的抗血管生成特性。本研究旨在评估 RGDechi-hCit 肽在七种 MM 细胞系中的体外作用。