Title of article
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases
Author/Authors
Thomas J. Tucker، نويسنده , , Marc T. Abrams، نويسنده , , Carolyn A. Buser، نويسنده , , Joseph P. Davide، نويسنده , , Michelle Ellis-Hutchings، نويسنده , , Christine Fernandes، نويسنده , , Jackson B. Gibbs، نويسنده , , Samuel L. Graham، نويسنده , , George D. Hartman، نويسنده , , Hans E. Huber، نويسنده , , Dongming Liu، نويسنده , , Robert B. Lobell، نويسنده , , William C. Lumma، نويسنده , , Ronald G. Robinson، نويسنده , , John T. Sisko، نويسنده , , Anthony M. Smith، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
4
From page
2027
To page
2030
Abstract
We have prepared a series of potent, dual inhibitors of the prenyl transferases farnesyl protein transferase (FPTase) and geranyl-geranyl protein transferase I (GGPTase). The compounds were shown to possess potent activity against both enzymes in cell culture. Mechanistic analysis has shown that the compounds are CAAX competitive for FPTase inhibition but geranyl-geranyl pyrophosphate (GGPP) competitive for GGPTase inhibiton.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792368
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