| Abstract
| - Eleven farnesyl diphosphate analogues, which contained ω-azide or alkyne substituents suitable forbioorthogonal Staudinger and Huisgen [3 + 2] cycloaddition coupling reactions, were synthesized. Theanalogues were evaluated as substrates for the alkylation of peptide cosubstrates by yeast protein farnesyltransferase. Five of the diphosphates were good alternative substrates for farnesyl diphosphate (FPP).Steady-state kinetic constants were measured for the active compounds, and the products were characterizedby HPLC and LC-MS. Two of the analogues gave steady-state kinetic parameters (kcat and Km) verysimilar to those of the natural substrate.
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