Gillette William K, Esposito Dominic, Abreu Blanco Maria, Alexander Patrick, Bindu Lakshman, Bittner Cammi, Chertov Oleg, Frank Peter H, Grose Carissa, Jones Jane E, Meng Zhaojing, Perkins Shelley, Van Que, Ghirlando Rodolfo, Fivash Matthew, Nissley Dwight V, McCormick Frank, Holderfield Matthew, Stephen Andrew G
Cancer Research Technology Program, Frederick National Laboratory for Cancer Research, Leidos Biomedical Research, Inc. PO Box B, Frederick, MD 21702.
Laboratory of Molecular Biology, National Institute of Diabetes and Digestive and Kidney Diseases, 5 Memorial Drive, Bethesda MD 20892.
Sci Rep. 2015 Nov 2;5:15916. doi: 10.1038/srep15916.
Prenylated proteins play key roles in several human diseases including cancer, atherosclerosis and Alzheimer's disease. KRAS4b, which is frequently mutated in pancreatic, colon and lung cancers, is processed by farnesylation, proteolytic cleavage and carboxymethylation at the C-terminus. Plasma membrane localization of KRAS4b requires this processing as does KRAS4b-dependent RAF kinase activation. Previous attempts to produce modified KRAS have relied on protein engineering approaches or in vitro farnesylation of bacterially expressed KRAS protein. The proteins produced by these methods do not accurately replicate the mature KRAS protein found in mammalian cells and the protein yield is typically low. We describe a protocol that yields 5-10 mg/L highly purified, farnesylated, and methylated KRAS4b from insect cells. Farnesylated and methylated KRAS4b is fully active in hydrolyzing GTP, binds RAF-RBD on lipid Nanodiscs and interacts with the known farnesyl-binding protein PDEδ.
异戊烯化蛋白在包括癌症、动脉粥样硬化和阿尔茨海默病在内的多种人类疾病中发挥关键作用。KRAS4b在胰腺癌、结肠癌和肺癌中经常发生突变,它通过法尼基化、蛋白水解切割以及C端的羧甲基化进行加工。KRAS4b的质膜定位需要这种加工过程,KRAS4b依赖的RAF激酶激活也需要该过程。此前生产修饰型KRAS的尝试依赖于蛋白质工程方法或对细菌表达的KRAS蛋白进行体外法尼基化。这些方法产生的蛋白质不能准确复制哺乳动物细胞中发现的成熟KRAS蛋白,并且蛋白质产量通常较低。我们描述了一种从昆虫细胞中产生5-10mg/L高度纯化、法尼基化和甲基化的KRAS4b的方案。法尼基化和甲基化的KRAS4b在水解GTP方面具有完全活性,可在脂质纳米盘上结合RAF-RBD,并与已知的法尼基结合蛋白PDEδ相互作用。