1.
Bioorg Med Chem Lett
; 12(15): 2027-30, 2002 Aug 05.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12113834
RESUMO
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.