Liu Xiao-Hui, Prestwich Glenn D
Department of Medicinal Chemistry, The University of Utah, 419 Wakara Way, Suite 205, Salt Lake City, UT 84108-1257, USA.
Bioorg Med Chem Lett. 2004 May 3;14(9):2137-40. doi: 10.1016/j.bmcl.2004.02.077.
Didehydrofarnesyl diphosphate (delta delta FPP), a fluorescent pentaene analogue of farnesyl diphosphate (FPP), was synthesized using stereoselective Wittig reactions. Although delta delta FPP was not an alternative substrate for yeast protein farnesyltransferase (FTase), the fluorescent analogue was a potent competitive inhibitor with a K(i) value of 8.8 microM (K (m) (FPP) = 27 microM).
利用立体选择性维蒂希反应合成了法尼基二磷酸（FPP）的荧光戊二烯类似物二脱氢法尼基二磷酸（δδFPP）。尽管δδFPP不是酵母蛋白法尼基转移酶（FTase）的替代底物，但该荧光类似物是一种强效竞争性抑制剂，其抑制常数（Ki）值为8.8微摩尔（FPP的米氏常数（Km）=27微摩尔）。
