Title of article
From pure FPP to mixed FPP and CAAX competitive inhibitors of farnesyl protein transferase
Author/Authors
Marc Lannuzel، نويسنده , , Marie Lamothe، نويسنده , , Philippe Schambel، نويسنده , , Chantal Etiévant، نويسنده , , Bridget Hill، نويسنده , , Michel Pérez، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
4
From page
1459
To page
1462
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793163
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