Chambers T J, Weir R C, Grakoui A, McCourt D W, Bazan J F, Fletterick R J, Rice C M
Department of Molecular Microbiology, Washington University School of Medicine, Saint Louis, MO 63110-1093.
Proc Natl Acad Sci U S A. 1990 Nov;87(22):8898-902. doi: 10.1073/pnas.87.22.8898.
Sequence homology and molecular modeling studies have suggested that the N-terminal one-third of the flavirvirus nonstructural protein NS3 functions as a trypsin-like serine protease. To examine the putative proteolytic activity of NS3, segments of the yellow fever virus genome were subcloned into plasmid transcription/translation vectors and cell-free translation products were characterized. The results suggest that a protease activity encoded within NS2B and the N-terminal one-third of yellow fever virus NS3 is capable of cis-acting site-specific proteolysis at the NS2B-NS3 cleavage site and dilution-insensitive cleavage of the NS2A-NS2B site. Site-directed mutagenesis of the His-53, Asp-77, and Ser-138 residues of NS3 that compose the proposed catalytic triad implicates this domain as a serine protease. Infectious virus was not recovered from mammalian cells transfected with RNAs transcribed from full-length yellow fever virus cDNA templates containing mutations at Ser-138 (which abolish or dramatically reduce protease activity in vitro), suggesting that the protease is required for viral replication.
序列同源性和分子建模研究表明,黄病毒非结构蛋白NS3的N端三分之一区域具有类胰蛋白酶丝氨酸蛋白酶的功能。为了检测NS3假定的蛋白水解活性,将黄热病毒基因组片段亚克隆到质粒转录/翻译载体中,并对无细胞翻译产物进行表征。结果表明,NS2B和黄热病毒NS3的N端三分之一区域编码的蛋白酶活性能够在NS2B-NS3裂解位点进行顺式作用的位点特异性蛋白水解,并能对NS2A-NS2B位点进行稀释不敏感的裂解。对构成假定催化三联体的NS3的His-53、Asp-77和Ser-138残基进行定点诱变,表明该结构域是一种丝氨酸蛋白酶。用含有Ser-138突变(在体外消除或显著降低蛋白酶活性)的全长黄热病毒cDNA模板转录的RNA转染哺乳动物细胞,未回收感染性病毒,这表明蛋白酶是病毒复制所必需的。