Kumagai K, Tokunaga K, Tsutsumi M, Ikuta K
Institute of Immunological Science, Hokkaido University, Sapporo, Japan.
FEBS Lett. 1993 Sep 13;330(2):117-21. doi: 10.1016/0014-5793(93)80255-s.
We recently showed that S1, a sequence-scrambled form of CD4 CDR3-related synthetic peptide, has more potent inhibitory activities on HIV-1 replication and HIV-1-induced syncytium formation than the original form. In this study, a series of derivatives of S1 were synthesized and their anti-HIV-1 activities were evaluated. A D-isomer was as potent as S1, and a homodimer was 10- to 18-fold more potent than S1. The increased antiviral activity of the dimer peptide was related to alpha-helix formation, as detected by circular dichroism.
我们最近发现，S1是一种与CD4互补决定区3（CDR3）相关的合成肽的序列打乱形式，它对HIV-1复制和HIV-1诱导的合胞体形成具有比原始形式更强的抑制活性。在本研究中，合成了一系列S1的衍生物，并评估了它们的抗HIV-1活性。一种D-异构体与S1的活性相当，而一种同二聚体的活性比S1强10至18倍。通过圆二色性检测发现，二聚体肽抗病毒活性的增强与α-螺旋的形成有关。
