4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 15, Pages 4217-4222

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.05.107

Keywords

Ras protein; Sugars; Synthesis; Anticancer agents; NMR; Molecular modeling

Funding

  1. NIDDK NIH HHS [DK46371] Funding Source: Medline

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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.

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