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  • Title: Farnesyl-derived inhibitors of ras farnesyl transferase.
    Author: Kang MS, Stemerick DM, Zwolshen JH, Harry BS, Sunkara PS, Harrison BL.
    Journal: Biochem Biophys Res Commun; 1995 Dec 05; 217(1):245-9. PubMed ID: 8526918.
    Abstract:
    The synthesis and evaluation of farnesyl-derived inhibitors of ras farnesyl transferase are presented. Evaluation of inhibitors of farnesyl transferase and comparison with the previously described inhibitor was accomplished using purified enzyme and Amersham's Farnesyl:Transferase enzyme assay kit. These results show an order of magnitude increase in inhibitory activity for beta-ketophosphonic acid over beta-hydroxyphosphonic acid. Incorporation of fluorines in alpha-position, led to an increase in inhibitory activity over the nonfluorinated analogues.
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