title: First experimental identification of Ras-inhibitor binding interface using a water-soluble Ras ligand.
abstract: 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 (15)N-edited HSQC NMR experiment the ligand-Ras binding interface.
authors.affiliation: Department of Biotechnology and Biosciences, University of Milano-Bicocca, Piazza della Scienza, 2, 20126 Milano, Italy.
authors.forename: Alessandro
authors.initials: A
authors.lastname: Palmioli
authors.forename: Elena
authors.initials: E
authors.lastname: Sacco
authors.forename: Sherwin
authors.initials: S
authors.lastname: Abraham
authors.forename: Celestine J
authors.initials: CJ
authors.lastname: Thomas
authors.forename: Alessandro
authors.initials: A
authors.lastname: Di Domizio
authors.forename: Luca
authors.initials: L
authors.lastname: De Gioia
authors.forename: Vadim
authors.initials: V
authors.lastname: Gaponenko
authors.forename: Marco
authors.initials: M
authors.lastname: Vanoni
authors.forename: Francesco
authors.initials: F
authors.lastname: Peri
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D005960:Glucosides / Q000138:chemical synthesis* / Q000494:pharmacology; D006147:Guanine / Q000737:chemistry; D006801:Humans; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D051379:Mice; D008958:Models, Molecular; D008968:Molecular Conformation; D041681:NIH 3T3 Cells; D011485:Protein Binding; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology; D018631:ras Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D005960:Glucosides; D008024:Ligands; C107861:SCH 54292; D013449:Sulfonamides; D006147:Guanine; D018631:ras Proteins