Lobl T J, Renis H E, Epand R M, Maggiora L L, Wathen M W
Biopolymer Chemistry Research, Upjohn Company, Kalamazoo, MI.
Int J Pept Protein Res. 1988 Nov;32(5):326-30.
Five carbobenzoxylated and D-amino acid containing-peptide analogs of the respiratory syncytial virus (RSV) F1 glycoprotein amino terminus were chemically synthesized by solution and FMOC-solid phase peptide synthesis methods. Several of these peptides, ranging from 3 to 6 residues in length, raised the bilayer to hexagonal phase transition temperature of dielaidoylphosphatidylethanolamine. None of these peptides were specific inhibitors of RSV or herpes simplex virus infection. Two of the series, CBZ-D-Phe-L-Leu-Gly-D-Phe-D-Leu-D-Leu and CBZ-D-Phe-L-Leu-Gly-D-Phe-D-Leu-D-Leu-Gly, were active in reducing measles virus-induced cytopathic effect at 62 micrograms/mL. Others in the series showed some activity at higher doses or activity simultaneously with some cell toxicity. These results support the view that membrane-stabilizing agents may have non-specific effects on membranes which are responsible for their antimeasles activity.
通过溶液法和FMOC-固相肽合成法，化学合成了呼吸道合胞病毒（RSV）F1糖蛋白氨基末端的5种含苄氧羰基化和D-氨基酸的肽类似物。这些肽中有几种长度为3至6个残基，提高了二油酰磷脂酰乙醇胺从双层到六方相的转变温度。这些肽均不是RSV或单纯疱疹病毒感染的特异性抑制剂。其中两个系列，CBZ-D-苯丙氨酸-L-亮氨酸-甘氨酸-D-苯丙氨酸-D-亮氨酸-D-亮氨酸和CBZ-D-苯丙氨酸-L-亮氨酸-甘氨酸-D-苯丙氨酸-D-亮氨酸-D-亮氨酸-甘氨酸，在浓度为62微克/毫升时能有效减轻麻疹病毒诱导的细胞病变效应。该系列中的其他肽在较高剂量时表现出一些活性，或在具有一定细胞毒性的同时表现出活性。这些结果支持这样一种观点，即膜稳定剂可能对膜具有非特异性作用，这是它们抗麻疹活性的原因。
