Bioorganic & medicinal chemistry letters

Didehydrofarnesyl diphosphate: an intrinsically fluorescent inhibitor of protein farnesyltransferase

X Liu, GD Prestwich

文献索引：Liu, Xiao-Hui; Prestwich, Glenn D. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 9 p. 2137 - 2140

全文：HTML全文

被引用次数: 13

摘要

Didehydrofarnesyl diphosphate (ΔΔFPP), a fluorescent pentaene analogue of farnesyl diphosphate (FPP), was synthesized using stereoselective Wittig reactions. Although ΔΔFPP was not an alternative substrate for yeast protein farnesyltransferase (FTase), the fluorescent analogue was a potent competitive inhibitor with a Ki value of 8.8 μM (K m (FPP)= 27 μM).