First experimental identification of Ras-inhibitor binding interface using a water-soluble Ras ligand

By combining in the same molecule Ras-interacting aromatic moieties and a sugar, we prepared a water-soluble Ras ligand that binds Ras and inhibits guanine nucleotide exchange. With this compound it was possible to determine experimentally by a 15N-edited HSQC NMR experiment the ligand-Ras binding i...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-08, Vol.19 (15), p.4217-4222
Hauptverfasser:	Palmioli, Alessandro, Sacco, Elena, Abraham, Sherwin, Thomas, Celestine J., Domizio, Alessandro Di, Gioia, Luca De, Gaponenko, Vadim, Vanoni, Marco, Peri, Francesco
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anticancer agents Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Biological and medical sciences Chemistry, Pharmaceutical - methods Drug Design General aspects Glucosides - chemical synthesis Glucosides - pharmacology Guanine - chemistry Humans Ligands Magnetic Resonance Spectroscopy - methods Medical sciences Mice Models, Molecular Molecular Conformation Molecular modeling NIH 3T3 Cells NMR Pharmacology. Drug treatments Protein Binding Ras protein ras Proteins - antagonists & inhibitors ras Proteins - metabolism Sugars Sulfonamides - chemical synthesis Sulfonamides - pharmacology Synthesis
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Zusammenfassung:	By combining in the same molecule Ras-interacting aromatic moieties and a sugar, we prepared a water-soluble Ras ligand that binds Ras and inhibits guanine nucleotide exchange. With this compound it was possible to determine experimentally by a 15N-edited HSQC NMR experiment the ligand-Ras binding interface.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.05.107