Kumar Sujeet, Sharma Rajendra K
Department of Pathology and Laboratory Medicine, University of Saskatchewan, Saskatoon, SK, S7N 0W8, Canada,
Mol Cell Biochem. 2014 Jul;392(1-2):175-86. doi: 10.1007/s11010-014-2029-z. Epub 2014 Mar 26.
N-myristoyltransferase (NMT) is an indispensible enzyme, which exists as two isoforms (NMT1 and NMT2) in humans and has proven roles in development of cancerous states. It is thus a target for novel anti-cancer drug design, but understanding of the biochemical and functional differences of these isozymes is not fully deciphered. A soluble expression under the T7 promoter for human NMT1 was achieved in E. coli BL21 (DE3) cells, devoid of any isopropyl β-D-1-thiogalactopyranoside-based induction. The identity of expressed protein was confirmed by matrix-assisted laser desorption ionization mass spectrometry peptide-fingerprint analysis and a two-step purification protocol yielded homogeneous enzyme. The intact mass of the purified protein was verified by electrospray ionization mass spectrometry and found to be in agreement with the theoretical mass (48.141 vs. 48.140 kDa). The fluorescence spectrophotometric analyses of the ligand binding and enzyme activity demonstrated that the recombinant form is functional. The yield of purified protein was ~8-10 mg/L culture (batch to batch variation) with a specific activity value of 18,500 ± 513 U/mg of protein under the experimental conditions used. The final verification of the myristoylation was demonstrated by mass spectrometry analysis of reaction product. The described approach could be readily adapted for production of human NMT1, with high yields of pure enzyme preparations, which should aid in downstream applications involving inhibitor design and structure-function studies of NMT's.
N-肉豆蔻酰转移酶(NMT)是一种不可或缺的酶,在人类中以两种同工型(NMT1和NMT2)存在,并且已被证明在癌症状态的发展中起作用。因此,它是新型抗癌药物设计的一个靶点,但对这些同工酶的生化和功能差异的理解尚未完全阐明。在大肠杆菌BL21(DE3)细胞中实现了人NMT1在T7启动子下的可溶性表达,无需任何基于异丙基β-D-1-硫代半乳糖苷的诱导。通过基质辅助激光解吸电离质谱肽指纹分析确认了表达蛋白的身份,两步纯化方案得到了均一的酶。通过电喷雾电离质谱验证了纯化蛋白的完整质量,发现与理论质量一致(48.141对48.140 kDa)。配体结合和酶活性的荧光分光光度分析表明重组形式具有功能。在所用实验条件下,纯化蛋白的产量约为8 - 10 mg/L培养物(批次间变化),比活性值为18,500±513 U/mg蛋白。通过反应产物的质谱分析证明了肉豆蔻酰化的最终验证。所描述的方法可以很容易地适用于人NMT1的生产,得到高产量的纯酶制剂,这将有助于涉及NMT抑制剂设计和结构 - 功能研究的下游应用。