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Issue 5, 2011
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Binding properties and biological characterization of new sugar-derived Ras ligands

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Abstract

Since mutations of Ras genes have a great incidence in human tumours, Ras oncoproteins are a major clinical target for the development of anticancer agents. We have developed synthetic molecules able to inhibit Ras activation. Here we present new, water-soluble Ras inhibitors composed by an aromatic pharmacofore moiety covalently linked to different sugars. New glycosylated compounds bind to Switch 2 region of Ras, also involved in effector binding, inhibit GEF-catalyzed nucleotide exchange on Ras in vitro, and reduce Ras-dependent proliferation of murine fibroblasts. The influence of the sugar unit on Ras binding affinity and on the biological activity of Ras inhibitors has been investigated.

Graphical abstract: Binding properties and biological characterization of new sugar-derived Ras ligands

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Publication details

The article was received on 16 Dec 2010, accepted on 15 Feb 2011 and first published on 07 Mar 2011


Article type: Concise Article
DOI: 10.1039/C0MD00264J
Med. Chem. Commun., 2011,2, 396-401

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    Binding properties and biological characterization of new sugar-derived Ras ligands

    E. Sacco, S. J. Abraham, A. Palmioli, G. Damore, A. Bargna, E. Mazzoleni, V. Gaponenko, M. Vanoni and F. Peri, Med. Chem. Commun., 2011, 2, 396
    DOI: 10.1039/C0MD00264J

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