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 language | English (US) |
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Pages (from-to) | 1448-1453 |
Number of pages | 6 |
Journal | ChemBioChem |
Volume | 5 |
Issue number | 10 |
DOIs | |
State | Published - Oct 4 2004 |
Keywords
- Bioorganic chemistry
- Nucleotides
- Protecting groups
- Ras protein
- Signal transduction