The Anticancer Activity of Organotelluranes: Potential Role in Integrin Inactivation. (25th April 2016)

• Record Type: Journal Article
• Authors: Silberman, Alon; Kalechman, Yona; Hirsch, Shira; Erlich, Ziv; Sredni, Benjamin; Albeck, Amnon
• Is Part Of: Chembiochem. Volume 17:Number 10(2016)
• Page Start: 918
• Page End: 927
• Publication Date: 2016-04-25
• Subjects: cancer -- inhibitors -- integrins -- labile ligands -- organotelluranes -- VLA-4; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1002/cbic.201500614
• Languages: English
• ISSNs: 1439-4227

Abstract

Abstract: Organic Te IV compounds (organotelluranes) differing in their labile ligands exhibited anti‐integrin activities in vitro and anti‐metastatic properties in vivo. They underwent ligand substitution withl ‐cysteine, as a thiol model compound. Unlike inorganic Te IV compounds, the organotelluranes did not form a stable complex with cysteine, but rather immediately oxidized it. The organotelluranes inhibited integrin functions, such as adhesion, migration, and metalloproteinase secretion mediation in B16F10 murine melanoma cells. In comparison, a reduced derivative with no labile ligand inhibited adhesion of B16F10 cells to a significantly lower extent, thus pointing to the importance of the labile ligands of the Te IV atom. One of the organotelluranes inhibited circulating cancer cells in vivo, possibly by integrin inhibition. Our results extend the current knowledge on the reactivity and mechanism of organotelluranes with different labile ligands and highlight their clinical potential. Abstract : Organotellurium compounds differing in their functional groups inhibit integrin functions as adhesion, migration, and metalloproteinase secretion mediators in murine melanoma cells. One of the compounds inhibits circulating cancer cells in vivo, possibly by integrin inhibition.