Engineering a CD4 mimetic inhibiting the binding of the human immunodeficiency virus-1 (HIV-1) envelope glycoprotein gp120 to human lymphocyte CD4 by the transfer of a CD4 functional site to a small natural scaffold

被引：16
|
作者：
Drakopoulou, E [1 ]
Vizzavona, J [1 ]
Vita, C [1 ]
机构：
[1] CEA, Dept Ingn & Etud Prot, CE Saclay, F-91190 Gif Sur Yvette, France
来源：
LETTERS IN PEPTIDE SCIENCE | 1998年 / 5卷 / 2-3期
关键词：
active site transfer; chimeric mini-protein; drug lead; HIV inhibitor;
D O I：
10.1023/A:1008837427367
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The solvent-exposed CDR2-like region of human CD4 was transferred to the structural scaffold of scorpion charybdotoxin, as a means to reproduce that site in a native-like conformation. The chimeric mini-protein (33 amino acids long), obtained by solid-phase synthesis, is able to specifically prevent the interaction of HIV-1 gp120 with CD4. This CD4 mimetic may represent a valuable tool in the study of the HIV-cell interactions and as a lead in the development of antiviral drugs.
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页码：241 / 245
页数：5
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