Camp L A, Hofmann S L
Department of Internal Medicine, University of Texas Southwestern Medical Center, Dallas 75235.
J Biol Chem. 1993 Oct 25;268(30):22566-74.
H-Ras, the protein product of the cellular homologue of the Harvey ras oncogene, undergoes a complex series of post-translational modifications that include C-terminal isoprenylation, proteolysis, methylation, and palmitoylation. Palmitoylation has been shown to enhance the transformation efficiency of H-Ras about 10-fold in vivo. A recent study (Magee, A. I., Gutierrez, L., McKay, I. A., Marshall, C. J., and Hall, A. (1987) EMBO J. 6, 3353-3357) has provided strong evidence that the palmitate undergoes a dynamic acylation-deacylation cycle, but details concerning the enzymology of this process and its regulation are lacking. To begin to dissect this event, we have developed an assay for the enzymatic removal of palmitate from [3H]palmitate-labeled H-Ras. This substrate was produced in a baculovirus expression system and was used to purify to homogeneity a novel 37-kDa enzyme from bovine brain cytosol that removes the radiolabeled palmitate. The purified enzyme is sensitive to diethyl pyrocarbonate and insensitive to phenylmethylsulfonyl fluoride and N-ethylmaleimide. Interestingly, the thioesterase recognizes H-Ras as a substrate only when H-Ras is in its native conformation (bound to Mg2+ and guanine nucleotide). The palmitoylated alpha subunits of the heterotrimeric G proteins are also substrates for the enzyme.
H-Ras是哈维ras癌基因细胞同源物的蛋白质产物,会经历一系列复杂的翻译后修饰,包括C末端异戊二烯化、蛋白水解、甲基化和棕榈酰化。已证明棕榈酰化在体内可使H-Ras的转化效率提高约10倍。最近一项研究(Magee, A. I., Gutierrez, L., McKay, I. A., Marshall, C. J., and Hall, A. (1987) EMBO J. 6, 3353 - 3357)提供了强有力的证据,表明棕榈酸经历动态酰化-去酰化循环,但该过程的酶学及其调控的细节尚不清楚。为了开始剖析这一事件,我们开发了一种从[3H]棕榈酸标记的H-Ras中酶促去除棕榈酸的测定方法。该底物在杆状病毒表达系统中产生,并用于从牛脑细胞质中纯化出一种新型的37 kDa酶,该酶可去除放射性标记的棕榈酸。纯化后的酶对焦碳酸二乙酯敏感,对苯甲基磺酰氟和N-乙基马来酰亚胺不敏感。有趣的是,硫酯酶仅在H-Ras处于其天然构象(与Mg2+和鸟嘌呤核苷酸结合)时才将其识别为底物。异源三聚体G蛋白的棕榈酰化α亚基也是该酶的底物。