870526-97-9Relevant academic research and scientific papers
From pure FPP to mixed FPP and CAAX competitive inhibitors of farnesyl protein transferase
Lannuzel, Marc,Lamothe, Marie,Schambel, Philippe,Etievant, Chantal,Hill, Bridget,Perez, Michel
, p. 1459 - 1462 (2003)
Starting from a FPP analogue with nanomolar inhibitory activity against isolated FPTase, yet lacking activity in cellular assays, structural modifications were performed to enhance cellular activity by removing all acidic functionalities. Overall, these changes resulted in the transformation of a pure FPP to a mixed FPP and CAAX competitive inhibitor with nanomolar activity on isolated FPTase and micromolar inhibitory activity in the farnesylation of H-Ras in cultured DLD-1 cells.
Synthesis of desthio prenylcysteine analogs: Sulfur is important for biological activity
Henriksen, Brian S.,Anderson, Jessica L.,Hrycyna, Christine A.,Gibbs, Richard A.
, p. 5080 - 5083 (2007/10/03)
N-Acetyl-S-farnesyl cysteine (AFC) is the minimal synthetic substrate for the enzyme Icmt, which methylates prenylated proteins. The desthio-AFC isostere 2 has been synthesized in racemic form. This analog was not an Icmt substrate, but instead a weak inh
