Pong S S, Nuss D L, Koch G
J Biol Chem. 1975 Jan 10;250(1):240-5.
Incorporation of amino acids into proteins in HeLa cells, virus-transformed 3T3 mouse fibroblasts, and mouse plasmacytoma cells is inhibited after the addition of L-1-tosylamido-2-phenylethyl chloromethyl ketone, an alkylating agent and chymotrypsin-specific protease inhibitor. Addition of this drug to tissue culture cells at concentrations of 20 to 30 mug per ml results in an irreversible inhibition of the incorporation of amino acids into cellular proteins, and a rapid and complete breakdown of polyribosomes. A comparative study examining the effects of L-1-tosylamido-2-phenylethyl chloromethyl ketone and several known inhibitors of in vivo protein synthesis, with known mechanisms of action, revealed that an optimal concentration of L-1-tosylamido-2-phenylethyl chloromethyl ketone: (a) immediately and selectively inhibits initiation of protein synthesis, (b) does not significantly affect normal elongation rates, and (c) does not promote a premature release of nascent peptides. L-1-Tosylamido-2-phenylethyl chloromenthyl ketone may prove to be a useful tool in investigating the initiatior of protein synthesis in eukaryotic cells.
在加入L-1-甲苯磺酰氨基-2-苯乙基氯甲基酮（一种烷基化剂和胰凝乳蛋白酶特异性蛋白酶抑制剂）后，HeLa细胞、病毒转化的3T3小鼠成纤维细胞和小鼠浆细胞瘤细胞中氨基酸掺入蛋白质的过程受到抑制。以每毫升20至30微克的浓度将这种药物添加到组织培养细胞中，会导致氨基酸掺入细胞蛋白质的过程受到不可逆的抑制，以及多核糖体迅速且完全分解。一项比较研究考察了L-1-甲苯磺酰氨基-2-苯乙基氯甲基酮和几种已知的体内蛋白质合成抑制剂（其作用机制已知）的效果，结果显示L-1-甲苯磺酰氨基-2-苯乙基氯甲基酮的最佳浓度：（a）立即且选择性地抑制蛋白质合成的起始；（b）对正常的延伸速率没有显著影响；（c）不会促进新生肽的过早释放。L-1-甲苯磺酰氨基-2-苯乙基氯甲基酮可能被证明是研究真核细胞中蛋白质合成起始的一种有用工具。
