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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:19

Article

Palmioli, Alessandro¹  Sacco, Elena¹  Abraham, Sherwin³  Thomas, Celestine J.²  Di Domizio, Alessandro¹  De Gioia, Luca¹  Gaponenko, Vadim³  Vanoni, Marco¹  Peri, Francesco¹ 

[1] Univ Milano Bicocca, Dept Biosci & Biotechnol, Piazza Sci 2, I-20126 Milan, Italy

[2] Univ Montana, CBSD, Missoula, MT 59812 USA

[3] Univ Illinois, Dept Biochem & Mol Genet, Chicago, IL 60607 USA

关键词: Ras protein;    Sugars;    Synthesis;    Anticancer agents;    NMR;    Molecular modeling;   

DOI  :  10.1016/j.bmcl.2009.05.107

来源: Elsevier

【 摘 要 】

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 N-15-edited HSQC NMR experiment the ligand-Ras binding interface. (C) 2009 Elsevier Ltd. All rights reserved.

【 授权许可】

Free