From pure FPP to mixed FPP and CAAX competitive inhibitors of farnesyl protein transferase |
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| Authors: | Lannuzel Marc Lamothe Marie Schambel Philippe Etiévant Chantal Hill Bridget Perez Michel |
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| Affiliation: | Department of Medicinal Chemistry 4, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin, 81106 Castres Cedex, France. |
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| Abstract: | 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. |
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