Synthesis of GTP-derived Ras ligands

Laurent Soulère, Courtney Aldrich, Oliver Daumke, Robert Gail, Lars Kissau, Alfred Wittinghofer, Herbert Waldmann

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

A practical and convenient method for the synthesis of acid- and base-sensitive GTP analogues carrying a further substituent at the terminal phosphate has been developed. Key to the successful synthesis of these potential ligands of the Ras protein is the use of Pd0-sensitive allyl protecting groups in a one-pot synthesis that avoids evaporation steps. Initial biochemical analysis of a representative compound revealed that such GTP analogues can bind to Ras and might open up the possibility of developing small molecules that can act as deactivators of oncogenic Ras.

Original languageEnglish (US)
Pages (from-to)1448-1453
Number of pages6
JournalChemBioChem
Volume5
Issue number10
DOIs
StatePublished - Oct 4 2004

Keywords

  • Bioorganic chemistry
  • Nucleotides
  • Protecting groups
  • Ras protein
  • Signal transduction

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