Danesi R, McLellan C A, Myers C E
Division of Hematology/Oncology, University of Virginia, Charlottesville 22908.
Biochem Biophys Res Commun. 1995 Jan 17;206(2):637-43. doi: 10.1006/bbrc.1995.1090.
Specific labeling of either farnesylated or geranylgeranylated proteins in human PC-3 prostate cancer cell line was obtained by suppression of mevalonic acid biosynthesis with lovastatin, 50 microM, followed by supplementation of cell culture medium with either [3H]farnesyl- or [3H]geranylgeranyl-pyrophosphate. The immunoprecipitation of either a farnesylated (p21 ras) or geranylgeranylated (p21 rap 1) protein demonstrated that labeling was specific since proteins were detected only if the appropriate isoprenoid was added to the culture medium. TLC analysis indicated that no conversion of one isoprenoid to the other occurred in these conditions. The selective labeling of either farnesylated or geranylgeranylated proteins may be a valuable tool for the development of inhibitors of isoprenoid transferases as a potential new class of antitumor agents.
通过用50微摩尔洛伐他汀抑制甲羟戊酸生物合成，然后用[3H]法尼基焦磷酸或[3H]香叶基香叶基焦磷酸补充细胞培养基，在人PC-3前列腺癌细胞系中获得了法尼基化或香叶基香叶基化蛋白的特异性标记。对法尼基化（p21 ras）或香叶基香叶基化（p21 rap 1）蛋白的免疫沉淀表明标记是特异性的，因为只有在向培养基中添加适当的类异戊二烯时才能检测到蛋白质。薄层色谱分析表明，在这些条件下没有发生一种类异戊二烯向另一种类异戊二烯的转化。法尼基化或香叶基香叶基化蛋白的选择性标记可能是开发类异戊二烯转移酶抑制剂作为潜在新型抗肿瘤药物的有价值工具。
