Zanotti G, Wieland T, D'Auria G, Paolillo L, Trivellone E
CNR, Department of Pharmaceutical Sciences, University La Sapienza, Rome, Italy.
Int J Pept Protein Res. 1990 Mar;35(3):263-70. doi: 10.1111/j.1399-3011.1990.tb00947.x.
The title compound 3, an amatoxin analogue containing L-alpha-aminobutyric acid instead of L-asparagine in position 1, as in natural toad stool peptides, has been synthesized. It does not inhibit the eukaryotic DNA-dependent RNA polymerase form II (or B) in concentrations up to 10(-4)M, whereas 50% inhibition is exerted in 10(-6)M solution by the corresponding Asn-analogue S-deoxo-Ile3-amaninamide 2. The striking difference seems to be due to a relatively small variation of the conformation recognized by sensitive NMR spectroscopic methods.
已合成标题化合物3，它是一种鹅膏毒素类似物，在第1位含有L-α-氨基丁酸而非天然蟾蜍粪便肽中的L-天冬酰胺。在浓度高达10⁻⁴M时，它不抑制真核生物依赖DNA的RNA聚合酶II型（或B型），而相应的天冬酰胺类似物S-脱氧异亮氨酸3-鹅膏酰胺2在10⁻⁶M溶液中可产生50%的抑制作用。这种显著差异似乎是由于通过灵敏的核磁共振光谱法识别的构象变化相对较小。
