In this communication the ability of new compound to inhibit nucleotide exchange on human Ras through STD NMR experiments is presented. Interestingly, the Surface Plasmon Resonance (SPR) studies reported here demonstrate for the first time that both glucose-derived and arabinose-derived compounds inhibit the interaction between Ras and the Guanine nucleotide Exchange Factor protein (C-Cdc25). This experimental evidence contributes to explain at a molecular level the mode of action of our inhibitors. Too complex to change. New glucose-derived phenylhydroxylamines inhibit nucleotide exchange on human Ras. NMR and SPR experiments indicated that the Ras-GEF interaction is inhibited when the Ras-ligand complex is formed. (Chemical Equation Presented). © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.

Airoldi, C., Palmioli, A., D'Urzo, A., Colombo, S., Vanoni, M., Martegani, E., et al. (2007). Glucose-derived Ras pathway inhibitors: evidence of Ras-ligand binding and Ras-GEF (Cdc25) interaction inhibition. CHEMBIOCHEM, 2007(8), 1376-1379 [10.1002/cbic.200700185].

Glucose-derived Ras pathway inhibitors: evidence of Ras-ligand binding and Ras-GEF (Cdc25) interaction inhibition

AIROLDI, CRISTINA;PALMIOLI, ALESSANDRO;D'URZO, ANNALISA;COLOMBO, SONIA;VANONI, MARCO ERCOLE;MARTEGANI, ENZO;PERI, FRANCESCO
2007

Abstract

In this communication the ability of new compound to inhibit nucleotide exchange on human Ras through STD NMR experiments is presented. Interestingly, the Surface Plasmon Resonance (SPR) studies reported here demonstrate for the first time that both glucose-derived and arabinose-derived compounds inhibit the interaction between Ras and the Guanine nucleotide Exchange Factor protein (C-Cdc25). This experimental evidence contributes to explain at a molecular level the mode of action of our inhibitors. Too complex to change. New glucose-derived phenylhydroxylamines inhibit nucleotide exchange on human Ras. NMR and SPR experiments indicated that the Ras-GEF interaction is inhibited when the Ras-ligand complex is formed. (Chemical Equation Presented). © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.
Articolo in rivista - Articolo scientifico
Ras, sugar, Gef
English
1376
1379
4
Airoldi, C., Palmioli, A., D'Urzo, A., Colombo, S., Vanoni, M., Martegani, E., et al. (2007). Glucose-derived Ras pathway inhibitors: evidence of Ras-ligand binding and Ras-GEF (Cdc25) interaction inhibition. CHEMBIOCHEM, 2007(8), 1376-1379 [10.1002/cbic.200700185].
Airoldi, C; Palmioli, A; D'Urzo, A; Colombo, S; Vanoni, M; Martegani, E; Peri, F
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/10281/6099
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