Increased anti‐HIV‐1 activity of CD4 CDR3‐related synthetic peptides by scrambling and further structural modifications, including d‐isomerization and dimerization

FEBS Letters

Kumagai, Kazuo¹  Tsutsumi, Masahiro²  Ikuta, Kazuyoshi¹  Tokunaga, Kenzo¹ 

[1] Institute of Immunological Science, Hokkaido University, Sapporo 060, Japan;Biotechnology Laboratory, Sumitomo Chemical Co., Takatsukasa, Takarazuka 665, Japan

关键词: HIV-1;    CD4;    Synthetic peptide;    Antiviral activity;    Circular dichroism;    HIV-1;    human immunodeficiency virus type 1;    CDR;    complementarity-determining region;    CD;    circular dichroism;    TCID;    tissue culture infectious dose;    PE;    phosphatidylethanolamine;    CPE;    cytopathic effect;   

DOI  :  10.1016/0014-5793(93)80255-S

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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 α-helix formation, as detected by circular dichroism.

【 授权许可】

Unknown