Sandberg B E
Int J Pept Protein Res. 1979 Mar;13(3):327-33. doi: 10.1111/j.1399-3011.1979.tb01887.x.
In order to study the importance of arginine residues 13 and 14 in apamin, the bee venom neurotoxin, four analogues, [Lys13]-apamin, [Lys14]-apamin, [Har4, Har13]-apamin and [Har4, har14]-apamin were synthesized and tested with respect to their neurotoxicity. The two lysine-apamins were prepared by the solid phase method on benzhydrylamine resins. Before oxidation to disulphides, the (S-Acm)4-peptides were isolated and characterized. Portions of the purified lysin peptides were converted to homoarginine analogues by guanidination. The four apamin analogues were lethal, but the lethal doses differed significantly. The results demonstrate that the arginine residue at position 14 is more important for the high toxicity than is the one at position 13. The circular dichroism (CD) spectrum of [Lys13]-apamin was identical with that of apamin itself, whereas the spectrum of [Lys14]-apamin showed certain deviations.
为了研究蜂毒神经毒素蜂毒明肽中精氨酸残基13和14的重要性，合成了四种类似物，即[赖氨酸13] -蜂毒明肽、[赖氨酸14] -蜂毒明肽、[高精氨酸4，高精氨酸13] -蜂毒明肽和[高精氨酸4，高精氨酸14] -蜂毒明肽，并对它们的神经毒性进行了测试。两种赖氨酸 - 蜂毒明肽是在二苯甲基胺树脂上通过固相法制备的。在氧化成二硫化物之前，分离并表征了（S - 乙酰巯基甲基）4 - 肽。将部分纯化的赖氨酸肽通过胍基化转化为高精氨酸类似物。这四种蜂毒明肽类似物都具有致死性，但致死剂量有显著差异。结果表明，第14位的精氨酸残基对高毒性的重要性高于第13位的精氨酸残基。[赖氨酸13] -蜂毒明肽的圆二色性（CD）光谱与蜂毒明肽本身的相同，而[赖氨酸14] -蜂毒明肽的光谱则显示出一定的偏差。
