Substrates and inhibitors for prenyl cysteine...

C - Chemistry – Metallurgy – 12 – Q

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C12Q 1/48 (2006.01) C07C 323/41 (2006.01) C07C 323/59 (2006.01)

Patent

CA 2084505

2084505 9117261 PCTABS00008 Compounds of formula (I), in which R1 is alkyl of 1 to 3 carbon atoms; R2 is -COX, wherein X is hydroxy, methyl, amino, thio, H-N-(alkyl of 1 to 3 carbon atoms), N-(alkyl of 1 to 3 carbon atoms)2, or halogen; R3 is a straight or branched chain alkyl of 10 to 25 carbon atoms, or a straight or branched chain alkene including polyunsaturated alkenes of 10 to 25 carbon atoms; and the alkali metal, alkaline earth metal, ammonium, and substituted ammonium salts thereof when R2 is -COOH, are substrates and/or inhibitors specifically for prenyl cysteine methyltransferase enzymes which catalyze the methyl transfer from S-adenosylmethionine to the C-termini of proteins and peptides with prenylated cysteine residues at their C-termini. The compounds, as substrates, are particularly suitable for use in assays for qualitatively or quantitatively detecting the farnesyl cysteine methyltransferase enzymes.

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