Zalacaín M, Zaera E, Vázquez D, Jiménez A
FEBS Lett. 1982 Nov 1;148(1):95-7. doi: 10.1016/0014-5793(82)81250-7.
Bouvardin is an antitumor drug that inhibits protein synthesis in intact eukaryotic cells and cell-free systems. Our present studies have shown that bouvardin acts at the level of the 80 S ribosome in a site somehow involved with the interaction of EF1 and EF2. Indeed bouvardin inhibits EF1-dependent binding of aminoacyl-tRNA and EF2-dependent translocation of peptidyl-tRNA but does not affect the nonenzymic translocation since this reaction does not require EF2. The site of the 80 S ribosome involved in the interaction with bouvardin appears to be independent from the cycloheximide and the cryptopleurine binding sites since yeast mutants resistant to cycloheximide or cryptopleurine are sensitive to bouvardin.
布伐迪因是一种抗肿瘤药物，它能抑制完整真核细胞和无细胞系统中的蛋白质合成。我们目前的研究表明，布伐迪因作用于80S核糖体水平，作用位点与EF1和EF2的相互作用有关。实际上，布伐迪因抑制氨酰基-tRNA的EF1依赖性结合和肽基-tRNA的EF2依赖性转位，但不影响非酶促转位，因为该反应不需要EF2。80S核糖体中与布伐迪因相互作用的位点似乎独立于环己酰亚胺和隐丹参酮结合位点，因为对环己酰亚胺或隐丹参酮耐药的酵母突变体对布伐迪因敏感。
